Document:

EX-4.2

 Exhibit 4.2 

NEITHER THIS SECURITY NOR THE SECURITIES FOR WHICH THIS SECURITY IS EXERCISABLE HAVE BEEN REGISTERED WITH THE SECURITIES AND EXCHANGE COMMISSION OR THE
SECURITIES COMMISSION OF ANY STATE IN RELIANCE UPON AN EXEMPTION FROM REGISTRATION UNDER THE SECURITIES ACT OF 1933, AS AMENDED (THE “SECURITIES ACT”), AND, ACCORDINGLY, MAY NOT BE OFFERED OR SOLD EXCEPT PURSUANT TO AN EFFECTIVE
REGISTRATION STATEMENT UNDER THE SECURITIES ACT OR PURSUANT TO AN AVAILABLE EXEMPTION FROM, OR IN A TRANSACTION NOT SUBJECT TO, THE REGISTRATION REQUIREMENTS OF THE SECURITIES ACT AND IN ACCORDANCE WITH APPLICABLE STATE SECURITIES LAWS. THIS
SECURITY AND THE SECURITIES ISSUABLE UPON EXERCISE OF THIS SECURITY MAY BE PLEDGED IN CONNECTION WITH A BONA FIDE MARGIN ACCOUNT OR OTHER LOAN SECURED BY SUCH SECURITIES. 
  

COMMON STOCK PURCHASE WARRANT 

REGULUS THERAPEUTICS INC. 
  

			
	Warrant Shares: [_______]	  	 Initial Exercise Date: [________]
 Issue Date:
[________]

 THIS COMMON STOCK PURCHASE WARRANT (the “Warrant”) certifies that, for value received,
[_____________] or its assigns (the “Holder”) is entitled, upon the terms and subject to the limitations on exercise and the conditions hereinafter set forth, at any time on or after the date hereof (the “Initial Exercise
Date”) and until 5:00 p.m. (New York City time) on [________]1 (the “Termination Date”) but not thereafter, to subscribe for and purchase from Regulus Therapeutics Inc.,
a Delaware corporation (the “Company”), up to [______] shares (as subject to adjustment hereunder, the “Warrant Shares”) of Common Stock. The purchase price of one share of Common Stock under this Warrant shall be
equal to the Exercise Price, as defined in Section 2(b). 
 Section 1. Definitions. In addition to the
terms defined elsewhere in this Warrant, the following terms have the meanings indicated in this Section 1: 

“Affiliate” means any Person that, directly or indirectly through one or more intermediaries, controls or is
controlled by or is under common control with a Person as such terms are used in and construed under Rule 405 under the Securities Act. 

“Bid Price” means, for any date, the price determined by the first of the following clauses that applies:
(a) if the Common Stock is then listed or quoted on a Trading Market, the bid price of the Common Stock for the time in question (or the nearest preceding date) on the Trading Market on which the Common Stock is then listed or quoted as
reported by Bloomberg L.P. (based on a Trading Day from 9:30 a.m. (New York City time) to 4:02 p.m. (New York City time)), (b) if OTCQB or OTCQX is not a 

 

	1 	 Fifth anniversary of the closing. 

  
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Trading Market, the volume weighted average price of the Common Stock for such date (or the nearest preceding date) on OTCQB or OTCQX as applicable, (c) if the Common Stock is not then
listed or quoted for trading on OTCQB or OTCQX and if prices for the Common Stock are then reported in the “Pink Sheets” published by OTC Markets Group, Inc. (or a similar organization or agency succeeding to its functions of reporting
prices), the most recent bid price per share of the Common Stock so reported, or (d) in all other cases, the fair market value of a share of Common Stock as determined by an independent appraiser selected in good faith by the Holders of a
majority in interest of the Warrants then outstanding and reasonably acceptable to the Company, the fees and expenses of which shall be paid by the Company.

“Business Day” means any day except any Saturday, any Sunday, any day which is a federal legal holiday in the
United States or any day on which banking institutions in the State of New York are authorized or required by law or other governmental action to close. 

“Commission” means the United States Securities and Exchange Commission. 

“Common Stock” means the common stock of the Company, par value $0.001 per share, and any other class of
securities into which such securities may hereafter be reclassified or changed. 
 “Common Stock
Equivalents” means any securities of the Company or any subsidiaries of the Company which would entitle the holder thereof to acquire at any time Common Stock, including, without limitation, any debt, preferred stock, right, option, warrant
or other instrument that is at any time convertible into or exercisable or exchangeable for, or otherwise entitles the holder thereof to receive, Common Stock. 

“Exchange Act” means the Securities Exchange Act of 1934, as amended, and the rules and regulations
promulgated thereunder. 
 “Person” means an individual or corporation, partnership, trust, incorporated or
unincorporated association, joint venture, limited liability company, joint stock company, government (or an agency or subdivision thereof) or other entity of any kind. 

“Purchase Agreement” means the Securities Purchase Agreement, dated November [__], 2020, by and among the
Company and the original Holder of this Warrant and the other parties named therein. 
 “Securities Act”
means the Securities Act of 1933, as amended, and the rules and regulations promulgated thereunder. 
 “Trading
Day” means a day on which the Common Stock is traded on a Trading Market. 
 “Trading Market” means
any of the following markets or exchanges on which the Common Stock is listed or quoted for trading on the date in question: the NYSE American, the Nasdaq Capital Market, the Nasdaq Global Market, the Nasdaq Global

  
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Select Market or the New York Stock Exchange (or any successors to any of the foregoing). 

“Transfer Agent” means Computershare, the current transfer agent of the Company, with a mailing address of 250
Royall Street, Canton, MA 02021, and any successor transfer agent of the Company. 
 “VWAP” means, for any
date, the price determined by the first of the following clauses that applies: (a) if the Common Stock is then listed or quoted on a Trading Market, the daily volume weighted average price of the Common Stock for such date (or the nearest
preceding date) on the Trading Market on which the Common Stock is then listed or quoted as reported by Bloomberg L.P. (based on a Trading Day from 9:30 a.m. (New York City time) to 4:02 p.m. (New York City time)), (b) if OTCQB or OTCQX is not
a Trading Market, the volume weighted average price of the Common Stock for such date (or the nearest preceding date) on OTCQB or OTCQX as applicable, (c) if the Common Stock is not then listed or quoted for trading on OTCQB or OTCQX and if
prices for the Common Stock are then reported in the “Pink Sheets” published by OTC Markets Group, Inc. (or a similar organization or agency succeeding to its functions of reporting prices), the most recent bid price per share of the
Common Stock so reported, or (d) in all other cases, the fair market value of a share of Common Stock as determined by an independent appraiser selected in good faith by the Holders of a majority in interest of the Warrants then outstanding and
reasonably acceptable to the Company, the fees and expenses of which shall be paid by the Company. 

“Warrants” means this Warrant and other warrants issued by the Company pursuant to the Purchase Agreement.

 Section 2.Exercise. 

a) Exercise of Warrants. Exercise of the purchase rights represented by this Warrant may be made, in whole or in part,
at any time or times on or after the Initial Exercise Date and on or before the Termination Date by delivery to the Company (or such other office or agency of the Company as it may designate by notice in writing to the registered Holder at the
address of the Holder appearing on the books of the Company) of a duly executed e-mail attachment of the Notice of Exercise in the form annexed hereto (the “Notice of Exercise”). Within the
earlier of (i) two (2) Trading Days and (ii) the number of Trading Days comprising the Standard Settlement Period (as defined in Section 2(d)(i) herein) following the date of exercise as aforesaid, the Holder shall deliver the
aggregate Exercise Price to the Company for the Warrant Shares specified in the applicable Notice of Exercise by wire transfer or cashier’s check drawn on a United States bank unless the cashless exercise procedure specified in
Section 2(c) below is specified in the applicable Notice of Exercise. No ink-original Notice of Exercise shall be required, nor shall any medallion guarantee (or other type of guarantee or
notarization) of any Notice of Exercise be required. Notwithstanding anything herein to the contrary, the Holder shall not be required to physically surrender this Warrant to the Company until the Holder has purchased all of the Warrant Shares
available hereunder and the Warrant has been exercised in full, in which case, the Holder shall 

  
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surrender this Warrant to the Company for cancellation within three (3) Trading Days of the date the final Notice of Exercise is delivered to the Company. Partial exercises of this Warrant
resulting in purchases of a portion of the total number of Warrant Shares available hereunder shall have the effect of lowering the outstanding number of Warrant Shares purchasable hereunder in an amount equal to the applicable number of Warrant
Shares purchased. The Holder and the Company shall maintain records showing the number of Warrant Shares purchased and the date of such purchases. The Company shall deliver any objection to any Notice of Exercise within one (1) Business Day of
receipt of such notice. The Holder and any assignee, by acceptance of this Warrant, acknowledge and agree that, by reason of the provisions of this paragraph, following the purchase of a portion of the Warrant Shares hereunder, the number of
Warrant Shares available for purchase hereunder at any given time may be less than the amount stated on the face hereof. 

b) Exercise Price. The exercise price per share of the Common Stock under this Warrant shall be $[__]2, subject to adjustment hereunder (the “Exercise Price”). 

c) Cashless Exercise. This Warrant may also be exercised, in whole or in part, at such time by means of a “cashless
exercise” in which the Holder shall be entitled to receive a number of Warrant Shares equal to the quotient obtained by dividing [(A-B) (X)] by (A), where: 

 

	 	(A) =	 as applicable: (i) the VWAP on the Trading Day immediately preceding the date of the applicable Notice of
Exercise if such Notice of Exercise is (1) both executed and delivered pursuant to Section 2(a) hereof on a day that is not a Trading Day or (2) both executed and delivered pursuant to Section 2(a) hereof on a Trading Day prior
to the opening of “regular trading hours” (as defined in Rule 600(b)(64) of Regulation NMS promulgated under the federal securities laws) on such Trading Day, (ii) at the option of the Holder, either (y) the VWAP on the Trading
Day immediately preceding the date of the applicable Notice of Exercise or (z) the Bid Price of the Common Stock on the principal Trading Market as reported by Bloomberg L.P. as of the time of the Holder’s execution of the applicable
Notice of Exercise if such Notice of Exercise is executed during “regular trading hours” on a Trading Day and is delivered within two (2) hours thereafter (including until two (2) hours after the close of “regular trading
hours” on a Trading Day) pursuant to Section 2(a) hereof or (iii) the VWAP on the date of the applicable Notice of Exercise if the date of such Notice of Exercise is a Trading Day and such Notice of Exercise is both executed and
delivered pursuant to Section 2(a) hereof after the close of “regular trading hours” on such Trading Day; 

  

	 	(B) =	 the Exercise Price of this Warrant, as adjusted hereunder; and 

 

	2 	 Equal to 120% of the purchase price of the shares (as-converted, if
applicable) at the closing. 

  
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	 	(X) =	 the number of Warrant Shares that would be issuable upon exercise of this Warrant in accordance with the terms
of this Warrant if such exercise were by means of a cash exercise rather than a cashless exercise. 

 If
Warrant Shares are issued in such a cashless exercise, the parties acknowledge and agree that in accordance with Section 3(a)(9) of the Securities Act, the Warrant Shares shall take on the registered characteristics of the Warrants being
exercised. The Company agrees not to take any position contrary to this Section 2(c). 
 d) Mechanics of
Exercise. 
 i. Delivery of Warrant Shares Upon Exercise. The Company shall cause the Warrant Shares purchased
hereunder to be transmitted by the Transfer Agent to the Holder by crediting the account of the Holder’s or its designee’s balance account with The Depository Trust Company through its Deposit or Withdrawal at Custodian system
(“DWAC”) if the Company is then a participant in such system and either (A) there is an effective registration statement permitting the issuance of the Warrant Shares to or resale of the Warrant Shares by the Holder or
(B) this Warrant is being exercised via cashless exercise, and otherwise by book-entry form or, if requested by the Holder, a physical delivery of a certificate, registered in the Company’s share register in the name of the Holder or its
designee, for the number of Warrant Shares to which the Holder is entitled pursuant to such exercise to the address specified by the Holder in the Notice of Exercise by the date that is the earlier of (i) the earlier of (A) two (2) Trading
Days after the delivery to the Company of the Notice of Exercise and (B) one (1) Trading Day after delivery of the aggregate Exercise Price to the Company and (ii) the number of Trading Days comprising the Standard Settlement Period after
the delivery to the Company of the Notice of Exercise (such date, the “Warrant Share Delivery Date”). Upon delivery of the Notice of Exercise, the Holder shall be deemed for all corporate purposes to have become the holder of record
of the Warrant Shares with respect to which this Warrant has been exercised, irrespective of the date of delivery of the Warrant Shares, provided that payment of the aggregate Exercise Price (other than in the case of a cashless exercise) is
received within the earlier of (i) two (2) Trading Days and (ii) the number of Trading Days comprising the Standard Settlement Period following delivery of the Notice of Exercise. The Company agrees to maintain a transfer agent that is a
participant in the FAST program so long as this Warrant remains outstanding and exercisable. As used herein, “Standard Settlement Period” means the standard settlement period, expressed in a number of Trading Days, on the
Company’s primary Trading Market with respect to the Common Stock as in effect on the date of delivery of the Notice of Exercise. 

ii. Delivery of New Warrants Upon Exercise. If this Warrant shall have been exercised in part, the Company shall, at
the request of a 

  
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Holder and upon surrender of this Warrant certificate, at the time of delivery of the Warrant Shares, deliver to the Holder a new Warrant evidencing the rights of the Holder to purchase the
unpurchased Warrant Shares called for by this Warrant, which new Warrant shall in all other respects be identical with this Warrant. 

iii. Compensation for Buy-In on Failure to Timely Deliver Warrant Shares Upon
Exercise. In addition to any other rights available to the Holder, if the Company fails to cause the Transfer Agent to transmit to the Holder the Warrant Shares in accordance with the provisions of Section 2(d)(i) above pursuant to an
exercise on or before the Warrant Share Delivery Date (other than a failure caused by incorrect or incomplete information provided by Holder to the Company), and if after such date the Holder is required to or otherwise purchases (in an open market
transaction or otherwise) shares of Common Stock to deliver in satisfaction of a sale by the Holder of the Warrant Shares which the Holder was entitled to receive upon the exercise relating to such Warrant Share Delivery Date (a “Buy-In”), then the Company shall (A) pay in cash to the Holder (in addition to any other remedies available to or elected by such Holder) the amount, if any, by which (x) the Holder’s total
purchase price (including brokerage commissions, if any) for the shares of Common Stock so purchased exceeds (y) the product of (1) the aggregate number of shares of Common Stock that the Holder was entitled to receive in connection with
the exercise at issue multiplied by (2) the actual sale price at which the sell order giving rise to such purchase obligation was executed (including any brokerage commissions), and (B) at the option of the Holder, either reinstate the
portion of the Warrant and equivalent number of Warrant Shares for which such exercise was not honored (in which case such exercise shall be deemed rescinded) or deliver to the Holder the number of shares of Common Stock that would have been issued
if the Company had timely complied with its exercise and delivery obligations requirements under Section 2(d)(i). For example, if the Holder purchases shares of Common Stock having a total purchase price of $11,000 to cover a Buy-In with respect to an attempted exercise of shares of Common Stock with respect to which the actual sale price (including any brokerage commissions) giving rise to such purchase obligation was a total of
$10,000, under clause (A) of the immediately preceding sentence the Company shall be required to pay the Holder $1,000. The Holder shall provide the Company written notice, within three (3) Trading Days after the occurrence of a Buy-In, indicating the amounts payable to the Holder in respect of the Buy-In together with applicable confirmations and other evidence reasonably requested by the Company.
Nothing herein shall limit a Holder’s right to pursue any other remedies available to it hereunder, at law or in equity including, without limitation, a decree of specific performance and/or injunctive relief with respect to the Company’s
failure to timely deliver shares of Common Stock upon exercise of the Warrant as required pursuant to the terms hereof; provided, 

  
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however, that the Holder shall not be entitled to both (i) require the Company to reinstate the portion of the Warrant and equivalent number of Warrant Shares for which such exercise was not
timely honored and (ii) receive the number of shares of Common Stock that would have been issued if the Company had timely complied with its delivery requirements under Section 2(d)(i). 

iv. No Fractional Shares or Scrip. No fractional shares or scrip representing fractional shares shall be issued upon
the exercise of this Warrant. As to any fraction of a share which the Holder would otherwise be entitled to purchase upon such exercise, the Company shall, at its election, either pay a cash adjustment in respect of such final fraction in an amount
equal to such fraction multiplied by the Exercise Price or round up to the next whole share. 
 v. Charges, Taxes and
Expenses. Issuance of Warrant Shares shall be made without charge to the Holder for any issue or transfer tax or other incidental expense in respect of the issuance of such Warrant Shares, all of which taxes and expenses shall be paid by the
Company, and such Warrant Shares shall be issued in the name of the Holder or in such name or names as may be directed by the Holder; provided, however, that in the event that Warrant Shares are to be issued in a name other than the
name of the Holder, this Warrant when surrendered for exercise shall be accompanied by the Assignment Form attached hereto duly executed by the Holder and the Company may require, as a condition thereto, the payment of a sum sufficient to reimburse
it for any transfer tax incidental thereto. The Company shall pay all Transfer Agent fees required for same-day processing of any Notice of Exercise and all fees to the Depository Trust Company (or another
established clearing corporation performing similar functions) required for same-day electronic delivery of the Warrant Shares. 

vi. Closing of Books. The Company will not close its stockholder books or records in any manner which prevents the
timely exercise of this Warrant, pursuant to the terms hereof. 
 e) Holder’s Exercise Limitations. The Company
shall not effect any exercise of this Warrant, and a Holder shall not have the right to exercise any portion of this Warrant, pursuant to Section 2 or otherwise, to the extent that after giving effect to such issuance after exercise as set
forth on the applicable Notice of Exercise, the Holder (together with the Holder’s Affiliates, and any other Persons acting as a group together with the Holder or any of the Holder’s Affiliates (such Persons, “Attribution
Parties”)), would beneficially own in excess of the Beneficial Ownership Limitation (as defined below). For purposes of the foregoing sentence, the number of shares of Common Stock beneficially owned by the Holder and its Affiliates
and Attribution Parties shall include the number of shares of Common Stock issuable upon exercise of this Warrant with respect to which such determination is being made, but shall exclude the number of

  
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shares of Common Stock which would be issuable upon (i) exercise of the remaining, nonexercised portion of this Warrant beneficially owned by the Holder or any of its Affiliates or
Attribution Parties and (ii) exercise or conversion of the unexercised or nonconverted portion of any other securities of the Company (including, without limitation, any other Common Stock Equivalents) subject to a limitation on conversion or
exercise analogous to the limitation contained herein beneficially owned by the Holder or any of its Affiliates or Attribution Parties. Except as set forth in the preceding sentence, for purposes of this Section 2(e), beneficial ownership
shall be calculated in accordance with Section 13(d) of the Exchange Act and the rules and regulations promulgated thereunder, it being acknowledged by the Holder that the Company is not representing to the Holder that such calculation is in
compliance with Section 13(d) of the Exchange Act and the Holder is solely responsible for any schedules required to be filed in accordance therewith. To the extent that the limitation contained in this Section 2(e) applies, the
determination of whether this Warrant is exercisable (in relation to other securities owned by the Holder together with any Affiliates and Attribution Parties) and of which portion of this Warrant is exercisable shall be in the sole discretion of
the Holder, and the submission of a Notice of Exercise shall be deemed to be the Holder’s determination of whether this Warrant is exercisable (in relation to other securities owned by the Holder together with any Affiliates and Attribution
Parties) and of which portion of this Warrant is exercisable, in each case subject to the Beneficial Ownership Limitation, and the Company shall have no obligation to verify or confirm the accuracy of such determination. In addition, a determination
as to any group status as contemplated above shall be determined in accordance with Section 13(d) of the Exchange Act and the rules and regulations promulgated thereunder. For purposes of this Section 2(e), in determining the number of
outstanding shares of Common Stock, a Holder may rely on the number of outstanding shares of Common Stock as reflected in (A) the Company’s most recent periodic or annual report filed with the Commission, as the case may be, (B) a
more recent public announcement by the Company or (C) a more recent written notice by the Company or the Transfer Agent setting forth the number of shares of Common Stock outstanding. Upon the written or oral request of a Holder, the
Company shall within one (1) Trading Day confirm orally and in writing to the Holder the number of shares of Common Stock then outstanding. In any case, the number of outstanding shares of Common Stock shall be determined after giving
effect to the conversion or exercise of securities of the Company, including this Warrant, by the Holder or its Affiliates or Attribution Parties since the date as of which such number of outstanding shares of Common Stock was reported. The
“Beneficial Ownership Limitation” shall initially be [9.99]%3 of the number of shares of the Common Stock outstanding immediately after giving effect to the issuance of shares of
Common Stock issuable upon exercise of this Warrant. The Holder, upon notice to the Company, may increase or decrease the Beneficial Ownership Limitation provisions of this Section 2(e), provided that the Beneficial Ownership Limitation in no
event exceeds [19.99]%4 of the number of shares of the Common Stock outstanding immediately after giving effect to the issuance of shares of Common Stock upon exercise of this Warrant held by the
Holder and the provisions of this Section 2(e) shall continue to apply. Any increase in 
  

	3 	 Each warrant to either reflect 4.99%, 9.99% or 19.99% based on particular investor’s preference.

	4 	 Each warrant to either reflect 9.99% or 19.99% based on particular investor’s preference.

  
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the Beneficial Ownership Limitation will not be effective until the 61st day after such notice is delivered to the Company. The provisions of
this paragraph shall be construed and implemented in a manner otherwise than in strict conformity with the terms of this Section 2(e) to correct this paragraph (or any portion hereof) which may be defective or inconsistent with the intended
Beneficial Ownership Limitation herein contained or to make changes or supplements necessary or desirable to properly give effect to such limitation. The limitations contained in this paragraph shall apply to a successor holder of this Warrant. 

Section 3. Certain Adjustments. 

a) Stock Dividends and Splits. If the Company, at any time while this Warrant is outstanding: (i) pays a stock
dividend or otherwise makes a distribution or distributions on shares of its Common Stock or any other equity or equity equivalent securities payable in shares of Common Stock (which, for avoidance of doubt, shall not include any shares of Common
Stock issued by the Company upon exercise of this Warrant), (ii) subdivides outstanding shares of Common Stock into a larger number of shares, (iii) combines (including by way of reverse stock split) outstanding shares of Common Stock into a
smaller number of shares, or (iv) issues by reclassification of shares of the Common Stock any shares of capital stock of the Company, then in each case on the effective date, the Exercise Price shall be multiplied by a fraction of which the
numerator shall be the number of shares of Common Stock (excluding treasury shares, if any) outstanding immediately before such event and of which the denominator shall be the number of shares of Common Stock outstanding immediately after such
event, and the number of shares issuable upon exercise of this Warrant shall be proportionately adjusted such that the aggregate Exercise Price of this Warrant shall remain unchanged. Any adjustment made pursuant to this Section 3(a) shall
become effective immediately after the record date for the determination of stockholders entitled to receive such dividend or distribution and shall become effective immediately after the effective date in the case of a subdivision, combination or re-classification. 
 b) Subsequent Rights Offerings. In addition to any adjustments
pursuant to Section 3(a) above, if at any time the Company grants, issues or sells any Common Stock Equivalents or rights to purchase stock, warrants, securities or other property pro rata to the record holders of any class of shares of Common
Stock (the “Purchase Rights”), then in each case on the effective date, the Holder will be entitled to acquire, upon the terms applicable to such Purchase Rights, the aggregate Purchase Rights which the Holder could have acquired if
the Holder had held the number of shares of Common Stock acquirable upon complete exercise of this Warrant (without regard to any limitations on exercise hereof, including without limitation, the Beneficial Ownership Limitation) immediately before
the date on which a record is taken for the grant, issuance or sale of such Purchase Rights, or, if no such record is taken, the date as of which the record holders of shares of Common Stock are to be determined for the grant, issue or sale of such
Purchase Rights (provided, however, to the extent that the Holder’s right to participate in any such Purchase Right would result in the Holder exceeding the Beneficial Ownership Limitation, then the Holder shall not be entitled to
participate in such Purchase Right to such extent (or beneficial ownership of such shares of Common 

  
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Stock as a result of such Purchase Right to such extent) and such Purchase Right to such extent shall be held in abeyance for the Holder until such time, if ever, as its right thereto would not
result in the Holder exceeding the Beneficial Ownership Limitation). 
 c) Pro Rata Distributions. During such time as
this Warrant is outstanding, if the Company shall declare or make any dividend or other distribution of its assets (or rights to acquire its assets) to holders of shares of Common Stock other than as set forth in Section 3(a), by way of return
of capital or otherwise (including, without limitation, any distribution of cash, stock or other securities, property or options by way of a dividend, spin off, reclassification, corporate rearrangement, scheme of arrangement or other similar
transaction) (a “Distribution”), at any time after the issuance of this Warrant, then, in each such case on the effective date, the Holder shall be entitled to participate in such Distribution to the same extent that the Holder
would have participated therein if the Holder had held the number of shares of Common Stock acquirable upon complete exercise of this Warrant (without regard to any limitations on exercise hereof, including without limitation, the Beneficial
Ownership Limitation) immediately before the date of which a record is taken for such Distribution, or, if no such record is taken, the date as of which the record holders of shares of Common Stock are to be determined for the participation in such
Distribution (provided, however, to the extent that the Holder’s right to participate in any such Distribution would result in the Holder exceeding the Beneficial Ownership Limitation, then the Holder shall not be entitled to
participate in such Distribution to such extent (or in the beneficial ownership of any shares of Common Stock as a result of such Distribution to such extent) and the portion of such Distribution shall be held in abeyance for the benefit of the
Holder until such time, if ever, as its right thereto would not result in the Holder exceeding the Beneficial Ownership Limitation). 

d) Fundamental Transaction. If, at any time while this Warrant is outstanding, (i) the Company, directly or
indirectly, in one or more related transactions effects any merger or consolidation of the Company with or into another Person, (ii) the Company, directly or indirectly, effects any sale, lease, license, assignment, transfer, conveyance or
other disposition of all or substantially all of its assets in one or a series of related transactions, (iii) any, direct or indirect, purchase offer, tender offer or exchange offer (whether by the Company or another Person) is completed
pursuant to which holders of Common Stock are permitted to sell, tender or exchange their shares for other securities, cash or property and has been accepted by the holders of 50% or more of the outstanding Common Stock, (iv) the Company,
directly or indirectly, in one or more related transactions effects any reclassification, reorganization or recapitalization of the Common Stock or any compulsory share exchange pursuant to which the Common Stock is effectively converted into or
exchanged for other securities, cash or property, or (v) the Company, directly or indirectly, in one or more related transactions consummates a stock or share purchase agreement or other business combination (including, without limitation, a
reorganization, recapitalization, spin-off or scheme of arrangement) with another Person or group of Persons whereby such other Person or group acquires more than 50% of the outstanding shares of Common Stock
(not including any shares of Common Stock held by the other Person or other Persons making or party to, or associated or affiliated with the other Persons making or party to, such stock or share purchase agreement or

  
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other business combination and excluding shares acquired upon conversion of any currently outstanding convertible securities in accordance with the terms thereof as in effect on the date hereof)
(each a “Fundamental Transaction”), then, upon any subsequent exercise of this Warrant, the Holder shall have the right to receive, for each Warrant Share that would have been issuable upon such exercise immediately prior to the
occurrence of such Fundamental Transaction (without regard to any limitation in Section 2(e) on the exercise of this Warrant), the number of shares of Common Stock of the successor or acquiring corporation or of the Company, if it is the
surviving corporation, and/or any additional or other consideration (the “Alternate Consideration”) as it would have been entitled to receive upon the occurrence of such Fundamental Transaction if it had been, immediately prior to
such Fundamental Transaction, the holder of one share of Common Stock (without regard to any limitation in Section 2(e) on the exercise of this Warrant). For purposes of any such exercise, the determination of the Exercise Price shall be
appropriately adjusted to apply to such Alternate Consideration based on the amount of Alternate Consideration issuable in respect of one share of Common Stock in such Fundamental Transaction, and the Company shall apportion the Exercise Price among
the Alternate Consideration in a reasonable manner reflecting the relative value of any different components of the Alternate Consideration. If holders of Common Stock are given any choice as to the securities, cash or property to be received in a
Fundamental Transaction, then the Holder shall be given the same choice as to the Alternate Consideration it receives upon any exercise of this Warrant following such Fundamental Transaction. The Company shall cause any successor entity in a
Fundamental Transaction in which the Company is not the survivor (the “Successor Entity”) to assume in writing all of the obligations of the Company under this Warrant in accordance with the provisions of this Section 3(d)
pursuant to written agreements in form and substance reasonably satisfactory to the Holder and reasonably approved by the Holder (without unreasonable delay) prior to such Fundamental Transaction and shall, at the option of the Holder and to the
extent applicable in light of the structure of the Fundamental Transaction, deliver to the Holder in exchange for this Warrant a security of the Successor Entity evidenced by a written instrument substantially similar in form and substance to this
Warrant which is exercisable for a corresponding number of shares of capital stock of such Successor Entity (or its parent entity) (only to the extent such capital stock is the form of consideration paid in the Fundamental Transaction) equivalent to
the shares of Common Stock acquirable and receivable upon exercise of this Warrant (without regard to any limitations on the exercise of this Warrant) prior to such Fundamental Transaction, and with an exercise price which applies the exercise price
hereunder to such shares of capital stock (but taking into account the relative value of the shares of Common Stock pursuant to such Fundamental Transaction and the value of such shares of capital stock, such number of shares of capital stock and
such exercise price being for the purpose of protecting the economic value of this Warrant immediately prior to the consummation of such Fundamental Transaction), and which is reasonably satisfactory in form and substance to the Holder. Upon the
occurrence of any such Fundamental Transaction, the Successor Entity shall succeed to, and be substituted for (so that from and after the date of such Fundamental Transaction, the provisions of this Warrant referring to the “Company” shall
refer instead to the Successor Entity), and may exercise every right and power of the Company and shall assume all of the obligations of 

  
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the Company under this Warrant with the same effect as if such Successor Entity had been named as the Company herein. 

e) Black Scholes Value. Notwithstanding anything to the contrary, in the event of a Fundamental Transaction, the Company
or any Successor Entity shall, at the Holder’s option, exercisable at any time concurrently with, or within 30 days after, the consummation of the Fundamental Transaction, purchase this Warrant from the Holder by paying to the Holder an amount
of cash equal to the Black Scholes Value of the remaining unexercised portion of this Warrant on the date of the consummation of such Fundamental Transaction; provided, however, if the Fundamental Transaction is not within the
Company’s control, including not approved by the Company’s Board of Directors, Holder shall only be entitled to receive from the Company or any Successor Entity, as of the date of consummation of such Fundamental Transaction, the same type
or form of consideration (and in the same proportion), at the Black Scholes Value (as defined below) of the unexercised portion of this Warrant, that is being offered and paid to the holders of Common Stock in connection with the Fundamental
Transaction, whether that consideration be in the form of cash, stock or any combination thereof, or whether the holders of Common Stock are given the choice to receive from among alternative forms of consideration in connection with the Fundamental
Transaction. “Black Scholes Value” means the value of this Warrant based on the Black and Scholes Option Pricing Model obtained from the “OV” function on Bloomberg, L.P. (“Bloomberg”) determined as of the
day of consummation of the applicable Fundamental Transaction for pricing purposes and reflecting (A) a risk-free interest rate corresponding to the U.S. Treasury rate for a period equal to the time between the date of the public announcement
of the applicable Fundamental Transaction and the Termination Date, (B) an expected volatility equal to the greater of 75% and the 100 day volatility obtained from the HVT function on Bloomberg as of the Trading Day immediately following the
public announcement of the applicable Fundamental Transaction, or, if the Fundamental Transaction is not publicly announced, the date the Fundamental Transaction is consummated, (C) the underlying price per share used in such calculation shall
be the sum of the price per share being offered in cash, if any, plus the value of any non-cash consideration, if any, being offered in such Fundamental Transaction, (D) a zero cost of borrow and
(E) a 360 day annualization factor. The payment of the Black Scholes Value will be made by wire transfer of immediately available funds within five Business Days of the Holder’s election (or, if later, on the effective date of the
Fundamental Transaction). 
 f) Calculations. All calculations under this Section 3 shall be made to the nearest
cent or the nearest 1/100th of a share, as the case may be. For purposes of this Section 3, the number of shares of Common Stock deemed to be issued and outstanding as of a given date shall be the sum of the number of shares of Common Stock
(excluding treasury shares, if any) issued and outstanding. 
 g) Notice to Holder. 

i. Adjustment to Exercise Price. Whenever the Exercise Price is adjusted pursuant to any provision of this
Section 3, the Company shall 

  
 12 

 
promptly deliver to the Holder by email a notice setting forth the Exercise Price after such adjustment and any resulting adjustment to the number of Warrant Shares and setting forth a brief
statement of the facts requiring such adjustment. 
 ii. Notice to Allow Exercise by Holder. If (A) the Company
shall declare a dividend (or any other distribution in whatever form) on the Common Stock, (B) the Company shall declare a special nonrecurring cash dividend on or a redemption of the Common Stock, (C) the Company shall authorize the
granting to all holders of the Common Stock rights or warrants to subscribe for or purchase any shares of capital stock of any class or of any rights, (D) the approval of any stockholders of the Company shall be required in connection with any
reclassification of the Common Stock, any consolidation or merger to which the Company is a party, any sale or transfer of all or substantially all of the assets of the Company, or any compulsory share exchange whereby the Common Stock is converted
into other securities, cash or property, or (E) the Company shall authorize the voluntary or involuntary dissolution, liquidation or winding up of the affairs of the Company, then, in each case, the Company shall cause to be delivered by email
to the Holder at its last email address as it shall appear upon the Warrant Register of the Company, at least 20 calendar days prior to the applicable record or effective date hereinafter specified, a notice stating (x) the date on which a
record is to be taken for the purpose of such dividend, distribution, redemption, rights or warrants, or if a record is not to be taken, the date as of which the holders of the Common Stock of record to be entitled to such dividend, distributions,
redemption, rights or warrants are to be determined or (y) the date on which such reclassification, consolidation, liquidation, merger, sale, transfer or share exchange is expected to become effective or close, and the date as of which it is
expected that holders of the Common Stock of record shall be entitled to exchange their shares of the Common Stock for securities, cash or other property deliverable upon such reclassification, consolidation, liquidation, merger, sale, transfer or
share exchange; provided that the failure to deliver such notice or any defect therein or in the delivery thereof shall not affect the validity of the corporate action required to be specified in such notice. To the extent that any notice provided
in this Warrant constitutes, or contains, material, non-public information regarding the Company or any subsidiaries of the Company, the Company shall simultaneously file such notice with the Commission
pursuant to a Current Report on Form 8-K. The Holder shall remain entitled to exercise this Warrant during the period commencing on the date of such notice to the effective date of the event triggering such
notice except as may otherwise be expressly set forth herein. 
 Section 4. Transfer of Warrant. 

  
 13 

 a) Transferability. This Warrant and all rights hereunder (including,
without limitation, any registration rights) are transferable, in whole or in part, upon surrender of this Warrant at the principal office of the Company or its designated agent, together with a written assignment of this Warrant substantially in
the form attached hereto duly executed by the Holder or its agent or attorney and funds sufficient to pay any transfer taxes payable upon the making of such transfer. Upon such surrender and, if required, such payment, the Company shall execute and
deliver a new Warrant or Warrants in the name of the assignee or assignees, as applicable, and in the denomination or denominations specified in such instrument of assignment, and shall issue to the assignor a new Warrant evidencing the portion of
this Warrant not so assigned, and this Warrant shall promptly be cancelled. Notwithstanding anything herein to the contrary, the Holder shall not be required to physically surrender this Warrant to the Company unless the Holder has assigned this
Warrant in full, in which case, the Holder shall surrender this Warrant to the Company within two (2) Trading Days of the date on which the Holder delivers an assignment form to the Company assigning this Warrant in full. The Warrant, if
properly assigned in accordance herewith, may be exercised by a new holder for the purchase of Warrant Shares without having a new Warrant issued. 

b) New Warrants. This Warrant may be divided or combined with other Warrants upon presentation hereof at the aforesaid
office of the Company, together with a written notice specifying the names and denominations in which new Warrants are to be issued, signed by the Holder or its agent or attorney. Subject to compliance with Section 4(a), as to any transfer
which may be involved in such division or combination, the Company shall execute and deliver a new Warrant or Warrants in exchange for the Warrant or Warrants to be divided or combined in accordance with such notice. All Warrants issued on transfers
or exchanges shall be dated the Issue Date of this Warrant and shall be identical with this Warrant except as to the number of Warrant Shares issuable pursuant thereto. 

c) Warrant Register. The Company shall register this Warrant, upon records to be maintained by the Company for that
purpose (the “Warrant Register”), in the name of the record Holder hereof from time to time. The Company may deem and treat the registered Holder of this Warrant as the absolute owner hereof for the purpose of any exercise hereof or
any distribution to the Holder, and for all other purposes, absent actual notice to the contrary. 
 d) Transfer
Restrictions. If, at the time of the surrender of this Warrant in connection with any transfer of this Warrant, the transfer of this Warrant shall not be either (i) registered pursuant to an effective registration statement under the
Securities Act and under applicable state securities or blue sky laws or (ii) eligible for resale pursuant to Rule 144, the Company may require, as a condition of allowing such transfer, that the Holder or transferee of this Warrant, as the
case may be, provide to the Company an opinion of counsel selected by the Holder and reasonably acceptable to the Company, the form and substance of which opinion shall be reasonably satisfactory to the Company, to the effect that such transfer does
not require registration of such transferred Warrant under the Securities Act. 

  
 14 

 e) Representation by the Holder. The Holder, by the acceptance
hereof, represents and warrants that it is acquiring this Warrant and, upon any exercise hereof, will acquire the Warrant Shares issuable upon such exercise, for its own account and not with a view to or for distributing or reselling such Warrant
Shares or any part thereof in violation of the Securities Act or any applicable state securities law, except pursuant to sales registered or exempted under the Securities Act. 

Section 5. Miscellaneous. 

a) No Rights as Stockholder Until Exercise; No Settlement in Cash. This Warrant does not entitle the Holder to any
voting rights, dividends or other rights as a stockholder of the Company prior to the exercise hereof as set forth in Section 2(d)(i), except as expressly set forth in Section 3. Without limiting the rights of a Holder to receive Warrant
Shares on a “cashless exercise,” in no event will the Company be required to net cash settle a Warrant exercise. 

b) Loss, Theft, Destruction or Mutilation of Warrant. The Company covenants that upon receipt by the Company of evidence
reasonably satisfactory to it of the loss, theft, destruction or mutilation of this Warrant or any stock certificate relating to the Warrant Shares, and in case of loss, theft or destruction, of indemnity or security reasonably satisfactory to it
(which, in the case of the Warrant, shall not include the posting of any bond), and upon surrender and cancellation of such Warrant or any stock certificate, if mutilated, the Company will make and deliver a new Warrant or issue stock (in
certificated or book entry form) of like tenor and dated as of such cancellation, in lieu of such Warrant or stock certificate. 

c) Saturdays, Sundays, Holidays, etc. If the last or appointed day for the taking of any action or the expiration of any
right required or granted herein shall not be a Business Day, then, such action may be taken or such right may be exercised on the next succeeding Business Day. 

d) Authorized Shares. 

The Company covenants that during the period the Warrant is outstanding, it will reserve from its authorized and unissued
Common Stock a sufficient number of shares to provide for the issuance of the Warrant Shares upon the exercise of any purchase rights under this Warrant. The Company further covenants that its issuance of this Warrant shall constitute full authority
to its officers who are charged with the duty of issuing the necessary Warrant Shares upon the exercise of the purchase rights under this Warrant. The Company will take all such reasonable action as may be necessary to assure that such Warrant
Shares may be issued as provided herein without violation of any applicable law or regulation, or of any requirements of the Trading Market upon which the Common Stock may be listed. The Company covenants that all Warrant Shares which may be issued
upon the exercise of the purchase rights represented by this Warrant will, upon exercise of the purchase rights represented by this Warrant and payment for such Warrant Shares in accordance herewith, be duly authorized,

  
 15 

 
validly issued, fully paid and nonassessable and free from all taxes, liens and charges created by the Company in respect of the issue thereof (other than taxes in respect of any transfer
occurring contemporaneously with such issue). 
 Except and to the extent as waived or consented to by the Holder, the
Company shall not by any action, including, without limitation, amending its certificate of incorporation or through any reorganization, transfer of assets, consolidation, merger, dissolution, issue or sale of securities or any other voluntary
action, avoid or seek to avoid the observance or performance of any of the terms of this Warrant, but will at all times in good faith assist in the carrying out of all such terms and in the taking of all such actions as may be necessary or
appropriate to protect the rights of Holder as set forth in this Warrant against impairment. Without limiting the generality of the foregoing, the Company will (i) not increase the par value of any Warrant Shares above the amount payable
therefor upon such exercise immediately prior to such increase in par value, (ii) take all such action as may be necessary or appropriate in order that the Company may validly and legally issue fully paid and nonassessable Warrant Shares upon
the exercise of this Warrant and (iii) use commercially reasonable efforts to obtain all such authorizations, exemptions or consents from any public regulatory body having jurisdiction thereof, as may be, necessary to enable the Company to
perform its obligations under this Warrant. 
 Before taking any action which would result in an adjustment in the number of
Warrant Shares for which this Warrant is exercisable or in the Exercise Price, the Company shall obtain all such authorizations or exemptions thereof, or consents thereto, as may be necessary from any public regulatory body or bodies having
jurisdiction thereof. 
 e) Jurisdiction. All questions concerning the construction, validity, enforcement and
interpretation of this Warrant shall be governed by and construed and enforced in accordance with the internal laws of the State of New York, without regard to the principles of conflicts of law thereof (whether of the State of New York or any other
jurisdiction) which would result in the application of the laws of any other jurisdiction. Each party agrees that all legal proceedings concerning the interpretations, enforcement and defense of the transactions contemplated by this Warrant (whether
brought against a party hereto or their respective affiliates, directors, officers, shareholders, partners, members, employees or agents) shall be commenced exclusively in the state and federal courts sitting in the City of New York. Each party
hereby irrevocably submits to the exclusive jurisdiction of the state and federal courts sitting in the City of New York, Borough of Manhattan for the adjudication of any dispute hereunder or in connection herewith or with any transaction
contemplated hereby or discussed herein, and hereby irrevocably waives, and agrees not to assert in any suit, action or proceeding, any claim that it is not personally subject to the jurisdiction of any such court, that such suit, action or
proceeding is improper or is an inconvenient venue for such proceeding. Each party hereby irrevocably waives personal service of process and consents to process being served in any such suit, action or proceeding by mailing a copy thereof via
registered or certified mail or overnight delivery (with evidence of delivery) to such party at the 

  
 16 

 
address in effect for notices to it under this Warrant and agrees that such service shall constitute good and sufficient service of process and notice thereof. Nothing contained herein shall be
deemed to limit in any way any right to serve process in any other manner permitted by law. If either party shall commence an action, suit or proceeding to enforce any provisions of this Warrant, the prevailing party in such action, suit or
proceeding shall be reimbursed by the other party for their reasonable attorneys’ fees and other costs and expenses incurred with the investigation, preparation and prosecution of such action or proceeding. 

f) Restrictions. The Holder acknowledges that the Warrant Shares acquired upon the exercise of this Warrant, if not
registered, and the Holder does not utilize cashless exercise, will have restrictions upon resale imposed by state and federal securities laws. 

g) Nonwaiver and Expenses. No course of dealing or any delay or failure to exercise any right hereunder on the part of
Holder shall operate as a waiver of such right or otherwise prejudice the Holder’s rights, powers or remedies. Without limiting any other provision of this Warrant or the Purchase Agreement pursuant to which this Warrant was issued, if the
Company willfully and knowingly fails to comply with any provision of this Warrant, which results in any material damages to the Holder, the Company shall pay to the Holder such amounts as shall be sufficient to cover any costs and expenses
including, but not limited to, reasonable attorneys’ fees, including those of appellate proceedings, incurred by the Holder in collecting any amounts due pursuant hereto or in otherwise enforcing any of its rights, powers or remedies hereunder.

 h) Notices. Any and all notices or other communications or deliveries to be provided by the Holders hereunder
including, without limitation, any Notice of Exercise, shall be in writing and delivered personally, by e-mail, or sent by a nationally recognized overnight courier service, addressed to the Company, at
Regulus Therapeutics Inc., 10628 Science Center Drive, Suite 225, San Diego, California 92121, Attention: Chief Financial Officer, email address: ccalsada@regulusrx.com, or such other email address or address as the Company may specify for such
purposes by notice to the Holders. Any and all notices or other communications or deliveries to be provided by the Company hereunder shall be in writing and delivered personally, by e-mail, or sent by a
nationally recognized overnight courier service addressed to each Holder at the e-mail address or address of such Holder appearing on the books of the Company. Any notice or other communication or deliveries
hereunder shall be deemed given and effective on the earliest of (i) the date of transmission, if such notice or communication is delivered via e-mail at the e-mail
address set forth in this Section prior to 5:30 p.m. (New York City time) on any date, (ii) the next Trading Day after the date of transmission, if such notice or communication is delivered via e-mail at
the e-mail address set forth in this Section on a day that is not a Trading Day or later than 5:30 p.m. (New York City time) on any Trading Day, (iii) the second Trading Day following the date of mailing,
if sent by U.S. nationally recognized overnight courier service, or (iv) upon actual receipt by the party to whom such notice is required to be given. To the extent that any notice provided hereunder constitutes, or contains, material, non-public information regarding the 

  
 17 

 
Company or any subsidiaries, the Company shall simultaneously file such notice with the Commission pursuant to a Current Report on Form 8-K. 

i) Limitation of Liability. No provision hereof, in the absence of any affirmative action by the Holder to exercise this
Warrant to purchase Warrant Shares, and no enumeration herein of the rights or privileges of the Holder, shall give rise to any liability of the Holder for the purchase price of any Common Stock or as a stockholder of the Company, whether such
liability is asserted by the Company or by creditors of the Company. 
 j) Remedies. The Holder, in addition to being
entitled to exercise all rights granted by law, including recovery of damages, will be entitled to specific performance of its rights under this Warrant. The Company agrees that monetary damages would not be adequate compensation for any loss
incurred by reason of a breach by it of the provisions of this Warrant and hereby agrees to waive and not to assert the defense in any action for specific performance that a remedy at law would be adequate. 

k) Successors and Assigns. Subject to applicable securities laws, this Warrant and the rights and obligations evidenced
hereby shall inure to the benefit of and be binding upon the successors and permitted assigns of the Company and the successors and permitted assigns of Holder. The provisions of this Warrant are intended to be for the benefit of any Holder from
time to time of this Warrant and shall be enforceable by the Holder or holder of Warrant Shares. 
 l) Amendment. This
Warrant may be modified or amended or the provisions hereof waived with the written consent of the Company and the Holder. 

m) Severability. Wherever possible, each provision of this Warrant shall be interpreted in such manner as to be
effective and valid under applicable law, but if any provision of this Warrant shall be prohibited by or invalid under applicable law, such provision shall be ineffective to the extent of such prohibition or invalidity, without invalidating the
remainder of such provisions or the remaining provisions of this Warrant. 
 n) Headings. The headings used in this
Warrant are for the convenience of reference only and shall not, for any purpose, be deemed a part of this Warrant. 
 ********************

 (Signature Page Follows) 

  
 18 

 IN WITNESS WHEREOF, the Company has caused this Warrant to be executed by its officer
thereunto duly authorized as of the date first above indicated. 
  

			
	 REGULUS THERAPEUTICS INC.

		
	By:	 	 
		 	 Name: Christopher R. Aker

		 	 Title: Senior Vice President and General Counsel

  
 19 

 NOTICE OF EXERCISE 

TO: REGULUS THERAPEUTICS INC. 
 (1) The
undersigned hereby elects to purchase                      Warrant Shares of the Company pursuant to the terms of the attached Warrant (only
if exercised in full), and tenders herewith payment of the exercise price in full, together with all applicable transfer taxes, if any. 

(2) Payment shall take the form of (check applicable box): 

[  ] in lawful money of the United States; or 

[  ] if permitted the cancellation of such number of Warrant Shares as is necessary, in accordance with the formula set forth in
subsection 2(c), to exercise this Warrant with respect to the maximum number of Warrant Shares purchasable pursuant to the cashless exercise procedure set forth in subsection 2(c). 

(3) Please issue said Warrant Shares in the name of the undersigned or in such other name as is specified below: 

 
  

The Warrant Shares shall be delivered to the following DWAC Account Number: 
  

 
  

 
  

 
 [SIGNATURE OF HOLDER] 

Name of Investing Entity: ________________________________________________________________________ 

Signature of Authorized Signatory of Investing Entity: _________________________________________________ 

Name of Authorized Signatory: ___________________________________________________________________ 

Title of Authorized Signatory: ____________________________________________________________________ 

Date: ________________________________________________________________________________________ 

 EXHIBIT B 

ASSIGNMENT FORM 
 (To assign
the foregoing Warrant, execute this form and supply required information. Do not use this form to purchase shares.) 
 FOR VALUE
RECEIVED, the foregoing Warrant and all rights evidenced thereby are hereby assigned to 
  

			
	 Name:
	  	 
	 	  	(Please Print)
		
	 Address:
	  	 
		  	(Please Print)
		
	 Phone Number:
	  	 
		
	 Email Address:
	  	
		
		  	  

		
	 Dated: _________ _____,______
	  	
		
	 Holder’s Signature:_________________
	  	
		
	 Holder’s Address:___________________EX-10.1

 Exhibit 10.1 

Execution Version 

SECURITIES PURCHASE AGREEMENT 

This SECURITIES PURCHASE AGREEMENT (this
“Agreement”), dated as of December 1, 2020, is made by and among REGULUS THERAPEUTICS INC., a Delaware corporation (the “Company”), and
the Purchasers listed on Exhibit A hereto, together with their permitted transferees (each, a “Purchaser” and collectively, the “Purchasers”). 

RECITALS: 
 A. The
Company and the Purchasers are executing and delivering this Agreement in reliance upon the exemption from securities registration afforded by Section 4(a)(2) of the Securities Act. 

B. The Purchasers desire to purchase and the Company desires to sell, upon the terms and conditions stated in this Agreement, shares of
Common Stock (the “Common Shares”), warrants to purchase Common Stock (“Warrants”) and shares of Class A-3 Convertible Preferred Stock (the
“Preferred Shares” and, together with the Common Shares, the “Shares”), having an aggregate purchase price of up to $19,383,036.94 as more fully described in this Agreement. 

C. The capitalized terms used herein and not otherwise defined have the meanings given them in Article 7. 

AGREEMENT 
 In
consideration of the premises and the mutual covenants contained herein and other good and valuable consideration, the receipt and sufficiency of which are hereby acknowledged, the Company and the Purchasers (severally and not jointly) hereby agree
as follows: 
 ARTICLE 1 

PURCHASE AND SALE OF SECURITIES 

1.1 Closing. 

(a) Purchase and Sale of Securities. At the closing of the transaction contemplated by this Agreement (the
“Closing”), the Company will sell and issue to each Purchaser, and each Purchaser will, severally and not jointly, purchase from the Company, (A) the number of Common Shares equal to (x) the dollar amount set forth
opposite such Purchaser’s name on Exhibit A hereto under the heading “Common Shares Subscription Amount” divided by (y) the Market Price, rounded down to the nearest whole share; provided, however, in the event the
number of Common Shares resulting from the foregoing calculation would result in such Purchaser, together with its Attribution Parties, beneficially owning in excess of the Beneficial Ownership Limitation of the outstanding Common Stock immediately
after the Closing, then (i) the number of Common Shares otherwise issuable to such Purchaser at the Closing will be reduced by the number (such number, the “Overage Number”) of Common Shares that would result in such
Purchaser beneficially owning, together with its Attribution Parties, no more than the Beneficial Ownership Limitation of the outstanding Common Stock immediately after the Closing, and (ii) the Company will issue to such Purchaser at the
Closing the maximum number of whole Preferred Shares which are convertible (in the aggregate and without regard to any conversion limitations) into a number of Preferred Conversion Shares that does not exceed the Overage Number; and (B) a
Warrant in the form attached hereto as Exhibit B exercisable for a number of shares of Common Stock equal to seventy-five percent of Common Shares purchased by the Purchaser at the Closing, rounded down to the nearest whole share, plus, if
applicable, seventy-five percent of the Preferred Conversion Shares issuable upon conversion of the Preferred Shares purchased by the Purchaser at the Closing, rounded down to the nearest whole share. The Common Shares, Warrants and Preferred Shares
to be issued in the Closing are collectively referred to herein as the “Securities”. 

 (b) Payment. At the Closing, each Purchaser will pay to the Escrow Agent, by
wire transfer of immediately available funds in accordance with the Escrow Agreement, the amount set forth opposite its name on Exhibit A hereto under the heading “Common Shares Subscription Amount” plus the product of (x) $0.125
multiplied by (y) each share of Common Stock issuable upon exercise of the Warrant (without regard to any exercise limitations set forth in the Warrant) to be issued to such Purchaser at the Closing (the “Warrant Subscription
Amount”). The Company will (i) instruct its transfer agent to credit each Purchaser the number of Common Shares purchased by the Purchaser pursuant to Section 1.1 hereof (and, upon request, will deliver stock certificates to
such Purchaser representing such Common Shares), (ii) deliver to each Purchaser the Warrant purchased by such Purchaser pursuant to Section 1.1 hereof and (iii) if applicable, issue a certificate evidencing the Preferred Shares purchased
by such Purchaser pursuant to Section 1.1 hereof. 
 (c) Closing Date. The Closing will take place as soon as reasonably
practicable after the date hereof but no later than December 4, 2020 (the date on which the Closing actually occurs, the “Closing Date”) and the Closing will be held remotely via the exchange of documents
and signatures, or at such other time and place as agreed upon by the Company and the Purchasers subscribing for a majority of the Securities to be sold and issued hereunder (the Preferred Shares to be counted on an as-converted-to-common-stock basis), based on the amounts set forth on Exhibit A hereto under the heading “Common Shares Subscription Amount”. 

ARTICLE 2 

REPRESENTATIONS AND WARRANTIES OF THE COMPANY 

Except as specifically contemplated by this Agreement, the Company hereby represents and warrants to the Purchasers and the Placement Agent as
of the date of this Agreement that: 
 2.1 Good Standing of the Company. The Company has been duly incorporated, is validly
existing as a corporation in good standing under the laws of the jurisdiction of its incorporation, has the corporate power and authority to own its property and to conduct its business as described in the reports, schedules, forms, statements and
other documents required to be filed by it with the SEC, pursuant to the reporting requirements of the Exchange Act (all of the foregoing filed prior to the date hereof and all exhibits included therein and financial statements and schedules thereto
and documents (other than exhibits) incorporated by reference therein, the “SEC Documents”) and is duly qualified to transact business and is in good standing in each jurisdiction in which the conduct of its business or its
ownership or leasing of property requires such qualification, except to the extent that the failure to be so qualified or be in good standing would not have a Material Adverse Effect on the Company. 

2.2 Authorization of Capital Stock. The authorized capital stock of the Company consists of 200,000,000 shares of Common Stock,
$0.001 par value per share, and 10,000,000 shares of Preferred Stock, $0.001 par value per share. As of September 30, 2020, 256,700 shares of Preferred Stock were designated Class A-1 Convertible
Preferred Stock and 1,639,515 shares were designated Class A-2 Convertible Preferred Stock. As of the Closing, 272,970 shares of Preferred Stock will be designated
Class A-3 Convertible Preferred Stock. As of September 30, 2020, 39,163,096 shares of Common Stock were issued and outstanding and 1,896,215 shares of Preferred Stock were issued and outstanding,
256,700 shares of which were Class A-1 Convertible Preferred Stock and 1,639,515 shares of which were Class A-2 Convertible Preferred Stock. No shares of Class A-3 Convertible Preferred Stock are issued and outstanding immediately prior to the Closing. The shares of capital stock of the Company, including the Common Stock outstanding prior to the issuance of the
Securities, have been duly authorized and are validly issued, fully paid and non-assessable and were not issued in violation of the preemptive or similar rights of any security holder of the Company. 

2.3 Authorization of Shares. The Shares of Common Stock issuable upon exercise of the Warrants (the “Warrant
Shares”) and the shares of Common Stock issuable upon conversion of the Class A-3 Convertible Preferred Stock (the “Preferred Conversion Shares” and, together with the
Warrant Shares, the “Conversion  

  
 2 

 
Shares”) have been duly authorized and, when issued and delivered in accordance with the terms of this Agreement (and, in the case of the Warrant Shares, the Warrants, and in
the case of the Preferred Conversion Shares, the Class A-3 Certificate of Designation), will be validly issued, fully paid and non-assessable, and the issuance of
such Shares and Conversion Shares will not be subject to any preemptive or similar rights of stockholders of the Company. 
 2.4
Private Placement. Neither the Company nor any of its Affiliates, nor any Person acting on its or their behalf, has, directly or indirectly, made any offers or sales of any security or solicited any offers to buy any security, under any
circumstances that would require registration of the Securities under the Securities Act. Assuming the accuracy of the representations and warranties of the Purchasers contained in Article 3 hereof, the issuance of the Securities and the Conversion
Shares are exempt from registration under the Securities Act. 
 2.5 Authorization and Execution of Agreement. This Agreement
has been duly authorized, executed and delivered by the Company. The Company has all requisite corporate power and authority to execute, deliver and perform its obligations under this Agreement. 

2.6 Absence of Defaults and Conflicts. Except as otherwise disclosed in the SEC Documents, the Company is not (i) in
violation of its charter, by-laws or similar incorporation or organizational documents or (ii) in violation or default in the performance or observance of any obligation, agreement, covenant or condition
contained in any contract, indenture, mortgage, deed of trust, loan or credit agreement, note, lease or other agreement or instrument to which the Company is a party or by which it may be bound, or to which any of the property or assets of the
Company is subject (collectively, “Agreements and Instruments”), except in the case of clause (ii), for such violations and defaults that would not result in a Material Adverse Effect on the Company; and the execution,
delivery and performance of this Agreement and the consummation of the transactions contemplated in this Agreement, and compliance by the Company with its obligations under this Agreement, do not and will not, whether with or without the giving of
notice or passage of time or both, conflict with or result in a breach of any of the terms and provisions of, or constitute a default or Repayment Event (as defined below) under, or result in the creation or imposition of any lien, charge or
encumbrance upon any property or assets of the Company pursuant to, the Agreements and Instruments, nor will such action result in any violation of the provisions of the charter, by-laws or similar
organizational documents of the Company or any applicable law, statute, rule, regulation, judgment, order, writ or decree of any government, government instrumentality or court, domestic or foreign, having jurisdiction over the Company or any of its
assets, properties or operations, except in each case (other than with respect to such charter, by-laws or similar organizational documents of the Company) for such conflicts, violations, breaches or defaults
which would not reasonably be expected to result in a Material Adverse Effect on the Company. As used herein, a “Repayment Event” means any event or condition which gives the holder of any note, debenture or other evidence of
indebtedness that is material to the operations or financial results of the Company (or any person acting on such holder’s behalf) the right to require the repurchase, redemption or repayment of all or a portion of such indebtedness by the
Company. 
 2.7 Absence of Further Requirements. No filing with, or authorization, approval, consent, license, order,
registration, exemption, qualification or decree of, any court or governmental authority or agency or any sub-division thereof is required for the performance by the Company of its obligations hereunder, in
connection with the offering, issuance or sale of the Securities and Conversion Shares under this Agreement or the consummation of the transactions contemplated by this Agreement, except such as have been already obtained or as may be required under
the Securities Act or the rules and regulations of the SEC thereunder, state securities or blue sky laws, the rules and regulations of the Financial Industry Regulatory Authority, Inc. (“FINRA”) or Nasdaq. 

2.8 No Material Adverse Effect. Except as otherwise disclosed in the SEC Documents, subsequent to the respective dates as of
which information is given in the SEC Documents: (a) the Company has not sustained 

  
 3 

 
any material loss or material interference with its business from fire, explosion, flood or other calamity, whether or not covered by insurance, or from any labor dispute or court or governmental
action, order or decree, (b) there has not been any change in the capital stock or increase in short-term or long-term debt of the Company, other than a change in the number of outstanding shares of Common Stock due to the issuance of shares
upon the exercise or settlement of outstanding options, warrants or restricted stock units as described in the SEC Documents, and (c) there has not occurred any Material Adverse Effect, or any development that would result in a prospective
Material Adverse Effect, in or affecting the condition, financial or otherwise, or in or affecting the revenues, business, assets, management, financial position, stockholders’ equity, operations or results of operations or prospects of the
Company. 
 2.9 Absence of Proceedings. There are no legal or governmental proceedings, inquiries or investigations pending
or, to the Company’s knowledge, threatened to which the Company is a party or to which any of the properties of the Company is subject, other than proceedings accurately described in all material respects in the SEC Documents or proceedings
that would not have a Material Adverse Effect on the Company, or on the power or ability of the Company to perform its obligations under this Agreement or to consummate the transactions contemplated by this Agreement. 

2.10 Investment Company Act of 1940. The Company is not, and after giving effect to the offering and sale of the Securities and
the application of the proceeds thereof as described herein will not be, required to register as an “investment company” as such term is defined in the Investment Company Act of 1940, as amended. 

2.11 Registration Rights. Except as described in the SEC Documents, there are no contracts, agreements or understandings between
the Company and any person granting such person the right to require the Company to file a registration statement under the Securities Act with respect to any securities of the Company or to require the Company to include such securities with the
Shares and Conversion Shares registered pursuant to a Registration Statement other than rights that have been validly waived. 
 2.12
Title to Real and Personal Property. Except as set forth in the SEC Documents, the Company has good and marketable title in fee simple to all real property and good and marketable title to all personal property owned by it which is material
to the business of the Company, in each case free and clear of all liens, encumbrances and defects, except such as are described in the SEC Documents or such as do not materially affect the value of such property and do not materially interfere with
the use made and proposed to be made of such property by the Company; and any real property and buildings held under lease by the Company are held by it under valid, subsisting and enforceable leases with such exceptions as are not material and do
not interfere with the use made and proposed to be made of such property and buildings by the Company. 
 2.13 Title to
Intellectual Property. Except as disclosed in the SEC Documents, the Company owns, possesses, licenses or has other rights to use all patents, patent applications, trade and service marks, trade and service mark registrations, trade names,
copyrights, licenses, inventions, trade secrets, technology, know-how and other intellectual property that, to the knowledge of the Company, is necessary for the conduct of the Company’s business as now
conducted (as described in the SEC Documents, collectively, the “Company Intellectual Property”), and, to the Company’s knowledge, the patents, trademarks, and copyrights included within the Company Intellectual Property
are valid, enforceable, and subsisting. Except as set forth in the SEC Documents or except in each case as would not reasonably be expected to have a Material Adverse Effect on the Company: (a) there are no material rights of third parties to
any such Company Intellectual Property; (b) to the Company’s knowledge, there is no material infringement by third parties of any such Company Intellectual Property; (c) there is no pending or, to the Company’s knowledge,
threatened action, suit, proceeding or claim by others challenging the Company’s rights in or to any such Company Intellectual Property; (d) there is no pending or, to the Company’s knowledge, threatened action, suit, proceeding or
claim by others challenging the validity or scope of 

  
 4 

 
any such Company Intellectual Property; (e) there is no pending or, to the Company’s knowledge, threatened action, suit, proceeding or claim by others that the Company infringes or
otherwise violates any patent, trademark, copyright, trade secret or other proprietary rights of others; (f) to the Company’s knowledge, there is no U.S. patent which contains claims that dominate any Company Intellectual Property
described in the SEC Documents or that interferes under 35 U.S.C. §102(g) with the pending claims of any Company Intellectual Property; (g) to the Company’s knowledge, there is no prior art of which the Company is aware that would
render any U.S. patent held by the Company invalid which has not been disclosed to the U.S. Patent and Trademark Office (the “PTO”); and (h) the Company is not obligated to pay a material royalty, grant a license, or
provide other material consideration to any third party in connection with the Company Intellectual Property. Except as otherwise disclosed in the SEC Documents, to the Company’s knowledge, all patents and patent applications owned by the
Company and filed with the PTO or any foreign or international patent authority (the “Company Patent Rights”) and all patents and patent applications in-licensed by the
Company and filed with the PTO or any foreign or international patent authority (the “In-licensed Patent Rights”) have been duly and properly filed; the Company has complied with their duty of candor and disclosure to the PTO
for the Company Patent Rights and, to the Company’s knowledge, the licensors of the In-licensed Patent Rights have complied with their duty of candor and disclosure to the PTO for the In-licensed Patent Rights. 
 2.14 Insurance. Except as set forth in the SEC Documents, the
Company is insured by insurers of recognized financial responsibility against such losses and risks and in such amounts as are prudent and customary in the business in which it is engaged; the Company has not been refused any coverage sought or
applied for; and the Company does not have any reason to believe that it will not be able to renew its existing insurance coverage as and when such coverage expires or to obtain similar coverage from similar insurers as may be necessary to continue
its business at a cost that would not have a Material Adverse Effect on the Company. 
 2.15 Licenses and Permits. Except as
set forth in the SEC Documents, the Company possesses all certificates, authorizations, consents, approvals, orders, licenses and permits issued by the appropriate federal, state or foreign regulatory authorities (collectively, the
“Permits”), including the FDA and any other state, federal or foreign agencies or bodies engaged in the regulation of pharmaceuticals or biohazardous materials, necessary to conduct its business as now conducted
and described in the SEC Documents, other than such certificates, authorizations, consents, approvals, orders, licenses and permits, the lack of which would not individually or in the aggregate have a Material Adverse Effect on the Company. Except
as otherwise disclosed in the SEC Documents, all of such Permits are valid and in full force and effect, except where the invalidity of such Permits or the failure to be in full force and effect, individually or in the aggregate, would not have a
Material Adverse Effect on the Company. Except as otherwise disclosed in the SEC Documents, there is no pending or, to the Company’s knowledge, threatened action, suit, proceeding or investigation that individually or in the aggregate would
reasonably be expected to lead to the revocation, modification, termination, suspension or any other impairment of the rights of the holder of any such Permit which revocation, modification, termination, suspension or other impairment would have a
Material Adverse Effect on the Company. 
 2.16 Accounting Controls. The Company has taken all actions reasonably necessary to
ensure that, within the time period required by applicable law, the Company will have established and will maintain a system of internal control over financial reporting (as such term is defined in Rule
13a-15(f) under the Exchange Act) sufficient to provide reasonable assurance regarding the reliability of financial reporting and the preparation of financial statements for external purposes in accordance
with United States generally accepted accounting principles (“U.S. GAAP”). Except as set forth in the SEC Documents, since the end of the Company’s most recent audited fiscal year, there has been (A) no material
weakness in the Company’s internal control over financial reporting (whether or not remediated) and (B) no change in the Company’s internal control over financial reporting that has materially affected, or is reasonably likely to
materially affect, the Company’s internal control over financial reporting. 

  
 5 

 2.17 Disclosure Controls. The Company maintains disclosure controls and
procedures (as such term is defined in Rule 13a-15(e) under the Exchange Act) that comply with the applicable requirements of the Exchange Act; and such disclosure controls and procedures have been designed to
ensure that material information relating to the Company is made known to the Company’s principal executive officer and principal financial officer by others within the Company. The Company has carried out evaluations of the effectiveness of
its disclosure controls and procedures as required by Rule 13a-15 of the Exchange Act. 

2.18 Independent Accountants. Ernst & Young LLP, who have certified the financial statements and supporting schedules
of the Company that are included in the SEC Documents and which will be included as a part of the Registration Statement, is an independent registered public accounting firm with respect to the Company as required by the Securities Act and the rules
and regulations of the SEC thereunder. 
 2.19 SEC Documents. The Company has timely filed the SEC Documents required to be
filed by it with the SEC since January 1, 2019, pursuant to the reporting requirements of the Exchange Act. As of their respective dates, the SEC Documents complied in all material respects with the requirements of the Exchange Act or the
Securities Act, as the case may be, and the rules and regulations of the SEC promulgated thereunder applicable to the SEC Documents, and none of the SEC Documents, at the time they were filed with the SEC, contained any untrue statement of a
material fact or omitted to state a material fact required to be stated therein or necessary in order to make the statements therein, in light of the circumstances under which they were made, not misleading. 

2.20 Financial Statements. (a) The financial statements included in the SEC Documents, together with the related schedules
and notes, present fairly, in all material respects, the financial position of the Company at the dates indicated and the statement of operations, stockholders’ equity and cash flows of the Company for the periods specified; said financial
statements have been prepared in conformity with U.S. GAAP applied on a consistent basis throughout the periods involved except, in the case of unaudited interim financial statements, for normal year-end audit
adjustments and the exclusion of footnotes. The selected financial data and the summary financial information included in the SEC Documents present fairly, in all material respects, the information shown therein and have been compiled on a basis
consistent in all material respects with that of the audited financial statements included in the SEC Documents. (b) Except as set forth in the SEC Documents, there are no off-balance sheet arrangements,
outstanding guarantees or other contingent obligations of the Company that would reasonably be expected to have a Material Adverse Effect on the Company. There are no transactions, arrangements or other relationships between and/or among the
Company, any of its affiliates (as such term is defined in Rule 405 of the Securities Act) and any unconsolidated entity, including, but not limited to, any structured finance, special purpose or limited purpose entity, that would reasonably be
expected to materially affect the Company’s liquidity or the availability of or requirements for its capital resources required to be described in SEC Documents which have not been described as required. 

2.21 Tax Liabilities and Reserves. Other than as set forth in the SEC Documents, any tax returns required to be filed by the
Company in any jurisdiction have been filed and any taxes, including any withholding taxes, excise taxes, penalties and interest, assessments and fees and other charges due or claimed to be due from the Company have been paid, other than any of
those being contested in good faith and for which adequate reserves have been provided or any of those currently payable without penalty or interest, except to the extent that the failure to so file or pay would not result in a Material Adverse
Effect on the Company. There is no material proposed tax deficiency, assessment, charge or levy against the Company, as to which a reserve would be required to be established under U.S. GAAP, that has not been so reserved or that should be disclosed
in the SEC Documents that has not been so disclosed, except for any such deficiency, assessment, charge or levy which, individually or in the aggregate, would not have a Material Adverse Effect on the Company. 

  
 6 

 2.22 Related Party Transactions. Except as described in the SEC Documents, no
relationship, direct or indirect, exists between or among the Company, on the one hand, and the directors, officers, stockholders, licensees, licensors or suppliers of the Company, on the other hand, that is required to be described in the SEC
Documents which is not so described. There are no outstanding loans, advances (except normal advances for business expense in the ordinary course of business) or guarantees of indebtedness by the Company, to or for the benefit of any of the officers
or directors of the Company or any of their respective family members, except as otherwise disclosed in the SEC Documents. 
 2.23
Commission Agreements. The Company is not a party to any contract, agreement or understanding with any person that would give rise to a valid claim against the Company or the Placement Agent for a brokerage commission, finder’s fee or
like payment in connection with any transaction contemplated by this Agreement, except for dealings with the Placement Agent, whose commissions and fees will be paid by the Company. 

2.24 Foreign Corrupt Practices Act. Except as otherwise disclosed in the SEC Documents, neither the Company nor, to the
Company’s knowledge, any of its affiliates, directors, officers, employees, agents or other person acting on behalf of the Company is aware of or has taken any action, directly or indirectly, that would result in a material violation by such
person of the Foreign Corrupt Practices Act of 1977, as amended, and the rules and regulations thereunder (the “FCPA”), including, without limitation, making use of the
mails or any means or instrumentality of interstate commerce corruptly in furtherance of an offer, payment, promise to pay or authorization of the payment of money, or other property, gift, promise to give, or authorization of the giving of anything
of value to any “foreign official” (as such term is defined in the FCPA) or any foreign political party or official thereof or any candidate for foreign political office, in contravention of the FCPA and the Company and, to the
Company’s knowledge, its affiliates have conducted their businesses in material compliance with the FCPA and have instituted and maintain policies and procedures designed to ensure, and which are reasonably expected to continue to ensure,
continued compliance therewith. 
 2.25 Use of Proceeds. The Company shall use the net proceeds of the sale of the Securities
hereunder for pre-clinical and clinical development, working capital and general corporate purposes. 

2.26 Acknowledgment Regarding Purchasers’ Purchase of Securities. The Company acknowledges and agrees that each of the
Purchasers is acting solely in the capacity of an arm’s length purchaser with respect to this Agreement and the transactions contemplated hereby. The Company further acknowledges that no Purchaser is acting as a financial advisor or fiduciary
of the Company (or in any similar capacity with respect to the Company) with respect to this Agreement and the transactions contemplated hereby and any advice given by any Purchaser or any of their respective representatives or agents to the Company
in connection with this Agreement and the transactions contemplated hereby is merely incidental to such Purchaser’s purchase of the Securities. The Company further represents to each Purchaser that the Company’s decision to enter into this
Agreement has been based on the independent evaluation of the transactions contemplated hereby by the Company and its representatives. 

2.27 No Reliance. The Company has not relied upon the Placement Agent or legal counsel for the Placement Agent for any legal,
tax or accounting advice in connection with the offering and sale of the Securities. 
 2.28 No Manipulation of Stock. The
Company has not taken, directly or indirectly, any action designed to stabilize or manipulate the price of the Common Stock or any security of the Company to facilitate the sale or resale of any of the Securities. 

2.29 The Nasdaq Capital Market. The Common Stock is listed on The Nasdaq Capital Market, and to the Company’s knowledge,
there are no proceedings to revoke or suspend such listing. Except as otherwise 

  
 7 

 
disclosed in the SEC Documents, the Company is in material compliance with the requirements of Nasdaq for continued listing of the Common Stock thereon and any other Nasdaq listing and
maintenance requirements. 
 Any certificate signed by an authorized officer of the Company and required to be delivered to the Placement Agent or to
counsel for the Placement Agent in connection with this Agreement shall be deemed to be a representation and warranty by the Company to the Placement Agent as to the matters set forth therein. 

ARTICLE 3 

PURCHASER’S REPRESENTATIONS AND WARRANTIES 

Each Purchaser represents and warrants to the Company and the Placement Agent, severally and not jointly, with respect to itself and its
purchase hereunder, that as of the Closing: 
 3.1 Investment Purpose. The Purchaser is purchasing the Securities for its own
account and not with a present view toward the public sale or distribution thereof and has no intention of selling or distributing any of such Securities or any arrangement or understanding with any other Persons regarding the sale or distribution
of such Securities except in accordance with the provisions of Article 6 and except as would not result in a violation of the Securities Act. The Purchaser will not, directly or indirectly, offer, sell, pledge, transfer or otherwise dispose of (or
solicit any offers to buy, purchase or otherwise acquire or take a pledge of) any of the Securities except in accordance with the provisions of Article 6 or pursuant to and in accordance with the Securities Act. 

3.2 Information. The Purchaser has been furnished with all relevant materials relating to the business, finances and operations
of the Company necessary to make an investment decision, and materials relating to the offer and sale of the Securities, that have been requested by the Purchaser, including, without limitation, the SEC Documents, and the Purchaser has had the
opportunity to review the SEC Documents. The Purchaser has been afforded the opportunity to ask questions of the Company. Neither such inquiries nor any other investigation conducted by or on behalf of such Purchaser or its representatives or
counsel shall modify, amend or affect such Purchaser’s right to rely on the truth, accuracy and completeness of the SEC Documents and the Company’s representations and warranties contained in the Agreement. The Purchaser specifically
understands and acknowledges that, on the date of this Agreement and on the Closing Date, the Company may have in its possession non-public information that could be material to the market price of the Shares.
The Purchaser hereby represents and warrants that, in entering into this Agreement and consummating the transactions contemplated hereby, it does not require the disclosure of such non-public information to it
by the Company in order to make an investment in the Securities, and hereby waives all present or future claims arising out of or relating to the Company’s failure to disclose such non-public information
to the Purchaser. The Purchaser also specifically acknowledges that the Company would not enter into this Agreement or any related documents in the absence of such Purchaser’s representations and acknowledgments set out in this Agreement, and
that this Agreement, including such representations and acknowledgments, are a fundamental inducement to the Company, and a substantial portion of the consideration provided by such Purchaser, in this transaction, and that the Company would not
enter into this transaction but for this inducement. 
 3.3 Acknowledgement of Risk. 

(a) The Purchaser acknowledges and understands that its investment in the Securities involves a significant degree of risk, including,
without limitation, (i) the Company remains a development stage business with limited operating history and requires substantial funds in addition to the proceeds from the sale of the Securities; (ii) an investment in the Company is
speculative, and only Purchasers who can afford the loss of their entire investment should consider investing in the Company and the Securities; (iii) the Purchaser may not be able to liquidate its investment; (iv) transferability of the
Securities is extremely limited; (v) in the event of a 

  
 8 

 
disposition of the Securities, the Purchaser could sustain the loss of its entire investment; and (vi) the Company has not paid any dividends on its Common Stock since inception and does not
anticipate the payment of dividends in the foreseeable future. Such risks are more fully set forth in the SEC Documents; 
 (b) The
Purchaser is able to bear the economic risk of holding the Securities for an indefinite period, and has knowledge and experience in financial and business matters such that it is capable of evaluating the risks of the investment in the Securities;
and 
 (c) The Purchaser has, in connection with the Purchaser’s decision to purchase Securities, not relied upon any
representations or other information (whether oral or written) other than as set forth in the representations and warranties of the Company contained herein and the information disclosed in the SEC Documents, and the Purchaser has, with respect to
all matters relating to this Agreement and the offer and sale of the Securities, relied solely upon the advice of such Purchaser’s own counsel and has not relied upon or consulted any counsel to the Placement Agent or counsel to the Company.

 3.4 Governmental Review. The Purchaser understands that no United States federal or state agency or any other government or
governmental agency has passed upon or made any recommendation or endorsement of the Securities or an investment therein. 
 3.5
Transfer or Resale. The Purchaser understands that: 
 (a) the Securities have not been and are not being registered under the
Securities Act (other than as contemplated in Article 6) or any applicable state securities laws and, consequently, the Purchaser may have to bear the risk of owning the Securities for an indefinite period of time because the Securities may not be
transferred unless (i) the resale of the Securities is registered pursuant to an effective registration statement under the Securities Act, as contemplated in Article 6; (ii) the Purchaser has delivered to the Company an opinion of counsel
(in form, substance and scope customary for opinions of counsel in comparable transactions) to the effect that the Securities to be sold or transferred may be sold or transferred pursuant to an exemption from such registration; or (iii) the
Securities are sold or transferred pursuant to Rule 144; 
 (b) any sale of the Securities made in reliance on Rule 144 may be made
only in accordance with the terms of Rule 144 and, if Rule 144 is not applicable, any resale of the Securities under circumstances in which the seller (or the Person through whom the sale is made) may be deemed to be an underwriter (as that term is
defined in the Securities Act) may require compliance with some other exemption under the Securities Act or the rules and regulations of the SEC thereunder; and 

(c) except as set forth in Article 6, neither the Company nor any other Person is under any obligation to register the resale of the
Securities under the Securities Act or any state securities laws or to comply with the terms and conditions of any exemption thereunder. 

3.6 Legends. 

(a) The Purchaser understands the certificates or book entries representing the Securities will bear a restrictive legend in
substantially the following form, in addition to any other legend required by applicable state securities laws or as may be appropriate to legend any restrictions on transfer set forth in this Agreement (and a stop-transfer order may be placed
against transfer of the certificates or book entries for such Securities): 
 THE SECURITIES REPRESENTED HEREBY HAVE NOT BEEN REGISTERED
UNDER THE SECURITIES ACT OF 1933, AS AMENDED, OR THE SECURITIES LAWS OF ANY STATE OF THE UNITED STATES. THE SECURITIES MAY NOT BE SOLD, OFFERED FOR SALE, PLEDGED, HYPOTHECATED, TRANSFERRED OR ASSIGNED IN THE ABSENCE OF AN EFFECTIVE

  
 9 

 
REGISTRATION STATEMENT FOR THE SECURITIES UNDER APPLICABLE SECURITIES LAWS, OR UNLESS OFFERED, SOLD, PLEDGED, HYPOTHECATED OR TRANSFERRED PURSUANT TO AN AVAILABLE EXEMPTION FROM THE REGISTRATION
REQUIREMENTS OF THOSE LAWS. THE COMPANY SHALL BE ENTITLED TO REQUIRE AN OPINION OF COUNSEL SATISFACTORY TO THE COMPANY THAT SUCH REGISTRATION IS NOT REQUIRED TO THE EXTENT THAT SUCH OPINION IS REQUIRED PURSUANT TO THAT CERTAIN SECURITIES PURCHASE
AGREEMENT UNDER WHICH THE SECURITIES WERE ISSUED. 
 (b) To the extent the resale of any issued Shares or Warrant Shares is
registered under the Securities Act pursuant to an effective Registration Statement, the Company agrees to promptly (i) authorize the removal of the legend set forth in Section 3.6(a) and any other legend not required by applicable law
from such Shares or Warrant Shares and (ii) cause its transfer agent to issue such Shares or Warrant Shares without such legends to the holders thereof by electronic delivery at the applicable balance account at the Depository Trust Company
upon surrender of any stock certificates evidencing such Shares or Warrant Shares. With respect to any Shares or Warrant Shares for which restrictive legends are removed pursuant to this Section 3.6(b), the holder thereof agrees to only sell
such Shares or Warrant Shares when and as permitted by the effective Registration Statement covering such resale and in accordance with applicable securities laws and regulations, or in accordance with Rule 144. 

(c) The Purchaser may request that the Company remove, and the Company agrees to authorize the removal of any legend from any Shares
or Warrant Shares issued to such Purchaser (i) following any sale of such Shares or Warrant Shares pursuant to Rule 144, or (ii) if such Shares or Warrant Shares are eligible for sale under Rule 144 following the expiration of the one-year holding requirement under subparagraphs (b)(1)(i) and (d) thereof and the Purchaser is not an affiliate of the Company, in each case following receipt from the Purchaser of an appropriate certification
to such effect. Following the time a legend is no longer required for the Shares or Warrant Shares under this Section 3.6(c), the Company will, no later than two Trading Days following the delivery by a Purchaser to the Company or the
Company’s transfer agent of a legended certificate representing such securities (if any) and appropriate certifications that the applicable requirements have been satisfied (the “Securities Delivery
Date”), deliver or cause to be delivered to such Purchaser a certificate or evidence of book entry representing such securities that is free from all restrictive and other legends or, in the case of Common Shares,
if requested by Purchaser, by crediting such Common Shares to the account of the Purchaser or its designee with The Depository Trust Company through its Deposit or Withdrawal at Custodian system
(“DWAC”) if the Company is then a participant in such system (“DWAC Delivery”); if the Company fails for any reason
to deliver Common Shares via DWAC Delivery (if the Company is then a participant in DWAC) to a Purchaser as required by this Section 3.6(c) (other than a failure caused by incorrect or incomplete information provided by Purchaser to the
Company), and if after such Securities Delivery Date such Purchaser is required to or otherwise purchases (in an open market transaction or otherwise), shares of Common Stock to deliver in satisfaction of a sale by such Purchaser of the Common
Shares which such Purchaser was entitled to receive relating to such Securities Delivery Date (a
“Buy-In”), then the Company shall pay in cash to such Purchaser (in addition to
any other remedies available to or elected by such Purchaser) the amount by which (x) such Purchaser’s total purchase price (including any brokerage commissions) for the shares of Common Stock so purchased exceeds (y) the product of
(1) the lesser of the (a) the number of shares of Common Stock so purchased and (b) the aggregate number of Common Shares that such Purchaser was entitled to receive for the Securities Delivery Date multiplied by (2) the actual
sale price at which the sell order giving rise to such purchase obligation was executed (including any brokerage commissions). For example, if a Purchaser purchases shares of Common Stock having a total purchase price of $11,000 to cover a Buy-In with respect to Common Shares that were not delivered via DWAC Delivery by the Securities Delivery Date with respect to which the actual sale price (including any brokerage commissions) giving rise to such
purchase obligation was a total of $10,000, the Company shall be required to pay such Purchaser $1,000. The Purchaser shall provide the Company written notice, within three (3) Business Days after the occurrence of a Buy-In, indicating the amounts payable to such 

  
 10 

 
Purchaser in respect of such Buy-In together with applicable confirmations and other evidence reasonably requested by the Company. Nothing herein shall
limit a Purchaser’s right to pursue any other remedies available to it hereunder, at law or in equity including, without limitation, a decree of specific performance and/or injunctive relief with respect to the Company’s failure to timely
deliver the Common Shares via DWAC Delivery as required pursuant to the terms hereof. 
 3.7 Authorization; Enforcement. The
Purchaser has the requisite power and authority to enter into this Agreement and to consummate the transactions contemplated hereby. The Purchaser has taken all necessary action to authorize the execution, delivery and performance of this Agreement.
Upon the execution and delivery of this Agreement, this Agreement shall constitute a valid and binding obligation of the Purchaser enforceable in accordance with its terms, except as enforceability may be limited by applicable bankruptcy,
insolvency, reorganization, moratorium or similar laws affecting creditors’ and contracting parties’ rights generally and except as enforceability may be subject to general principles of equity and except as rights to indemnity and
contribution may be limited by state or federal securities laws or public policy underlying such laws. 
 3.8 Residency.
Unless the Purchaser has otherwise notified the Company in writing, the Purchaser is a resident of the jurisdiction set forth immediately below such Purchaser’s name on the signature pages hereto. 

3.9 Acknowledgements Regarding Placement Agent. 

(a) The Purchaser acknowledges that the Placement Agent is acting as placement agent on a “best efforts” basis for the
Securities being offered hereby and will be compensated by the Company for acting in such capacity. The Purchaser represents that (i) the Purchaser was contacted regarding the sale of the Securities by the Placement Agent or the Company (or an
authorized agent or representative thereof) with whom the Purchaser entered into a verbal or written confidentiality agreement and (ii) no Securities were offered or sold to it by means of any form of general solicitation or general advertising
as such terms are used in Regulation D of the Securities Act. 
 (b) The Purchaser represents that it is making this investment
based on the results of its own due diligence investigation of the Company, and has not relied on any information or advice furnished by or on behalf of the Placement Agent in connection with the transactions contemplated hereby. The Purchaser
acknowledges that the Placement Agent has not made, and will not make, any representations and warranties with respect to the Company or the transactions contemplated hereby, and the Purchaser will not rely on any statements made by the Placement
Agent, orally or in writing, to the contrary. 
 ARTICLE 4 

COVENANTS 
 4.1
Reporting Status. The Company’s Common Stock is registered under Section 12 of the Exchange Act. During the Registration Period, the Company will timely file all documents with the SEC, and the Company will not terminate its status
as an issuer required to file reports under the Exchange Act even if the Exchange Act or the rules and regulations thereunder would permit such termination. 

4.2 Expenses. The Company and each Purchaser shall be liable for, and will pay, its own expenses incurred in connection with the
negotiation, preparation, execution and delivery of this Agreement, including, without limitation, attorneys’ and consultants’ fees and expenses. 

  
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 4.3 Financial Information. The financial statements of the Company to be
included in any documents filed with the SEC will be prepared in accordance with accounting principles generally accepted in the United States, consistently applied (except (i) as may be otherwise indicated in such financial statements or the
notes thereto, or (ii) in the case of unaudited interim statements, to the extent they may not include footnotes, may be condensed or summary statements or may conform to the SEC’s rules and instructions for Reports on Form 10-Q), and will fairly present in all material respects the financial position of the Company and results of its operations and cash flows as of, and for the periods covered by, such financial statements (subject,
in the case of unaudited statements, to normal and recurring year-end audit adjustments). 

4.4 Securities Laws Disclosure; Publicity. On or before the fourth business day following the date hereof, the Company shall
file a Current Report on Form 8-K with the SEC describing the terms of the transactions contemplated by this Agreement and including as an exhibit to such Current Report on Form
8-K this Agreement, in the form required by the Exchange Act. From and after the filing of such Current Report on Form 8-K, the Company represents to the Purchasers that
it shall have publicly disclosed the material terms and conditions of the transactions contemplated by this Agreement. 
 4.5 Non-Public Information. Except with respect to the material terms and conditions of the transactions contemplated by this Agreement, which shall be disclosed pursuant to Section 4.4, the Company covenants
and agrees that neither it, nor any other Person acting on its behalf will provide any Purchaser or its agents or counsel with any information following the date of this Agreement that constitutes, or the Company reasonably believes constitutes,
material non-public information, unless prior thereto such Purchaser has consented to the receipt of such information and agreed with the Company to keep such information confidential. The Company understands
and confirms that each Purchaser shall be relying on the foregoing covenant in effecting transactions in securities of the Company, provided that the Purchaser shall remain subject to applicable law. 

4.6 Sales by Purchasers; Purchases Prior to the Closing. Each Purchaser will sell any Shares and, if applicable, any Conversion
Shares held by it in compliance with applicable prospectus delivery requirements, if any, or otherwise in compliance with the requirements for an exemption from registration under the Securities Act and the rules and regulations promulgated
thereunder. No Purchaser will make any sale, transfer or other disposition of the Securities or, if applicable, Conversion Shares in violation of federal or state securities laws. Between the date of this Agreement and the Closing, each Purchaser
agrees that neither it nor any of such Purchaser’s Attribution Parties will acquire any shares of Common Stock or any securities of the Company which would entitle the holder thereof to acquire at any time Common Stock, other than the
Securities. 
 4.7 Reservation of Common Stock. The Company shall reserve and keep available at all times during which the
Warrants remain exercisable and the Preferred Shares remain convertible, free of preemptive rights, a sufficient number of shares of Common Stock for the purpose of enabling the Company to issue the Conversion Shares pursuant to the Warrants and the
Class A-3 Certificate of Designation, as applicable. 
 ARTICLE 5 

CONDITIONS TO CLOSING 

5.1 Conditions to Obligations of the Company. The Company’s obligation to complete the purchase and sale of the Securities
to each Purchaser at the Closing is subject to the waiver by the Company or fulfillment as of the Closing Date of the following conditions: 

  
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 (a) Receipt of Funds. The Escrow Agent shall have received immediately
available funds in the full amount of the Common Shares Subscription Amount and the Warrant Subscription Amount (collectively, “Subscription Amounts”), and in accordance with the Escrow Agreement, for the Securities being
purchased in the Closing hereunder as set forth opposite such Purchaser’s name on Exhibit A hereto. 
 (b)
Representations and Warranties. The representations and warranties made by each Purchaser in Article 3 shall be true and correct in all material respects as of the Closing Date. 

(c) Covenants. All covenants, agreements and conditions contained in this Agreement to be performed by the Purchasers on or
prior to the Closing Date shall have been performed or complied with in all material respects. 
 (d) Blue Sky. The Company
shall have obtained all necessary blue sky law permits and qualifications, or secured exemptions therefrom, required by any state for the offer and sale of the Securities. 

(e) Nasdaq Qualification. The Shares to be issued shall be duly authorized for listing by Nasdaq, subject to official notice of
issuance, to the extent required by the rules of Nasdaq. 
 (f) Absence of Litigation. No proceeding challenging this
Agreement or the transactions contemplated hereby, or seeking to prohibit, alter, prevent or materially delay the Closing, shall have been instituted or be pending before any court, arbitrator, governmental body, agency or official. 

(g) No Governmental Prohibition. The sale of the Securities by the Company shall not be prohibited by any law or governmental
order or regulation. 
 5.2 Conditions to Purchasers’ Obligations. Each Purchaser’s obligation to complete the
purchase and sale of the Securities is subject to the waiver by such Purchaser or fulfillment as of the Closing Date of the following conditions: 

(a) Representations and Warranties. The representations and warranties made by the Company in Article 2 shall be true and
correct in all material respects as of the Closing Date. 
 (b) Covenants. All covenants, agreements and conditions contained
in this Agreement to be performed by the Company on or prior to the Closing Date shall have been performed or complied with in all material respects. 

(c) Blue Sky. The Company shall have obtained all necessary blue sky law permits and qualifications, or secured exemptions
therefrom, required by any state or foreign or other jurisdiction for the offer and sale of the Securities. 
 (d) Nasdaq
Qualification. The Shares to be issued shall be duly authorized for listing by Nasdaq, subject to official notice of issuance, to the extent required by the rules of Nasdaq. 

(e) No Governmental Prohibition. The sale of the Securities by the Company shall not be prohibited by any law or governmental
order or regulation 
 (f) Certificate of Designation. The Company shall have filed the
Class A-3 Certificate of Designation with the Secretary of State of the State of Delaware prior to the Closing. 

(g) No Material Adverse Effect. There shall not have occurred any Material Adverse Effect, or any development that could
reasonably be expected to result in a Material Adverse Effect, as of the Closing. 

  
 13 

 (h) Transfer Agent Instructions. The Company shall have delivered to its
transfer agent irrevocable instructions to issue to such Purchaser or in such nominee name(s) as designated by such Purchaser in writing such number of Shares set forth opposite such Purchaser’s name on Exhibit A hereto and the Warrants to
purchase the Warrant Shares set forth opposite such Purchaser’s name on Exhibit A hereto. 
 ARTICLE 6 

REGISTRATION RIGHTS 

6.1 As soon as reasonably practicable, but in no event later than 30 days after the Closing Date (the “Filing
Date”), the Company shall file a registration statement covering the resale of the Registrable Securities with the SEC for an offering to be made on a continuous basis pursuant to Rule 415, or if Rule 415 is not available for offers and
sales of the Registrable Securities, by such other means of distribution of Registrable Securities as the Holders of a majority of such Registrable Securities may reasonably specify (the “Initial Registration
Statement”). The Initial Registration Statement shall be on Form S-3 (except if the Company is ineligible to register for resale the Registrable Securities on Form S-3, in which case such registration shall be on Form S-1) and the Company shall effect the registration, qualifications or compliances (including, without limitation, the
execution of any required undertaking to file post-effective amendments, appropriate qualifications or exemptions under applicable blue sky or other state securities laws and appropriate compliance with applicable securities laws, requirements or
regulations) as promptly as possible after the filing thereof, but in any event prior to the date which is five days after the receipt of a notification of no-review in the event of no review by the SEC, or 90
days after the Filing Date in the event of a review by the SEC. For purposes of clarification, any failure by the Company to file the Initial Registration Statement by the Filing Date or to effect such Registration Statement within such five days
after the notification of no-review or 90 days after the Filing Date, as applicable, shall not otherwise relieve the Company of its obligations to file or effect the Initial Registration Statement as set forth
above in this Section 6.1. In the event the SEC informs the Company that all of the Registrable Securities cannot, as a result of the application of Rule 415, be registered for resale as a secondary offering on a single registration statement,
the Company agrees to promptly (i) inform each of the Holders thereof, (ii) use its best efforts to file amendments to the Initial Registration Statement as required by the SEC and/or (iii) withdraw the Initial Registration Statement
and file a new registration statement (a “New Registration Statement”), in either case covering the maximum number of Registrable Securities permitted to be registered by the SEC, on Form
S-3 or, if the Company is ineligible to register for resale the Registrable Securities on Form S-3, Form S-1; provided,
however, that prior to filing such amendment or New Registration Statement, the Company shall be obligated to use its best efforts to advocate with the SEC for the registration of all of the Registrable Securities. In the event the Company
amends the Initial Registration Statement or files a New Registration Statement, as the case may be, under clauses (ii) or (iii) above, the Company will use its best efforts to file with the SEC, within 30 days following the date allowed by the
SEC, one or more registration statements on Form S-3 or, if the Company is ineligible to register for resale the Registrable Securities on Form S-3, Form S-1, to register for resale those Registrable Securities that were not registered for resale on the Initial Registration Statement, as amended, or the New Registration Statement (the “Remainder
Registration Statements”). If the SEC limits the number of Registrable Securities permitted to be registered on a particular Registration Statement (and notwithstanding that the Company used diligent efforts to advocate with the SEC for
the registration of all or a greater number of Registrable Securities), any required cutback of Registrable Securities (such Registrable Securities so cut back, the “Cut Back Securities”) shall be applied to the
Purchasers pro rata in accordance with the number of such Registrable Securities sought to be included in such Registration Statement by reference to the amount of Registrable Securities set forth opposite such Purchaser’s name on Exhibit
A (and in the case of a subsequent transfer, the initial Purchaser’s transferee) relative to the aggregate amount of all Registrable Securities. 

  
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 6.2 All Registration Expenses incurred in connection with any registration,
qualification, exemption or compliance pursuant to Section 6.1 shall be borne by the Company. All Selling Expenses relating to the sale of securities registered by or on behalf of Holders shall be borne by such Holders pro rata on the basis of
the number of securities so registered. 
 6.3 The Company further agrees that, in the event that (i) the Initial Registration
Statement has not been filed with the SEC within 30 days after the Closing Date, (ii) the Initial Registration Statement or the New Registration Statement, as applicable, has not been declared effective by the SEC (a) within five days
after receipt of a notification of no-review (in the event of a “no-review” by the SEC), or (b) within 90 days after the Filing Date (in the event of a
review by the SEC), or (iii) after such Registration Statement is declared effective by the SEC, is suspended by the Company or ceases to remain continuously effective as to all Registrable Securities for which it is required to be effective,
other than, in each case, within the time period(s) permitted by Section 6.7(b) (each such event referred to in clauses (i), (ii) and (iii), (a “Registration Default”)), for more than 20 consecutive days or
more than 40 days in any period of 365 days during which the Registration Default remains uncured, the Company shall pay to each Purchaser 1.0% of such Purchaser’s Aggregate Purchase Price as set forth on Exhibit A hereto (the
“Aggregate Purchase Price”) of such Purchaser’s Registrable Securities for each 30-day period (a “Penalty Period”) (provided the payment amount shall
increase by 1.0% of such Purchaser’s Aggregate Purchase Price as set forth on Exhibit A hereto for each subsequent 30-day period following the initial 30-day
period), or pro rata for any portion thereof, during which the Registration Default remains uncured; provided, however, that if a Purchaser fails to provide the Company with any information that is required to be provided in such Registration
Statement with respect to such Purchaser as set forth herein, then the commencement of the Penalty Period described above shall be extended until two Business Days following the date of receipt by the Company of such required information; and
provided, further, that in no event shall the Company be required hereunder to pay to any Purchaser pursuant to this Agreement more than 3.0% of such Purchaser’s Aggregate Purchase Price of such Purchaser’s Registrable Securities in any
Penalty Period and in no event shall the Company be required hereunder to pay to any Purchaser pursuant to this Agreement an aggregate amount that exceeds 10.0% of the Aggregate Purchase Price paid by such Purchaser for such Purchaser’s
Securities. The Company shall deliver said cash payment to the Purchaser by the fifth Business Day after the end of such Penalty Period. Notwithstanding any other provision of this Section 6.3, no Registration Default as to the Cut Back
Securities shall be deemed to have occurred until the date that is 30 days following the date on which the SEC permits the Cut Back Securities to be registered, and the payment of any penalty pursuant to this Section 6.3 shall be calculated to
apply only to the percentage of Registrable Securities which are permitted by the SEC to be registered within the timeframes provided for in this Agreement. 

6.4 In the case of the registration, qualification, exemption or compliance effected by the Company pursuant to this Agreement, the
Company shall, upon reasonable request, inform each Holder as to the status of such registration, qualification, exemption and compliance. At its expense the Company shall: 

(a) except for such times as the Company is permitted hereunder to suspend the use of the prospectus forming part of a Registration
Statement, use its best efforts to keep such registration, and any qualification, exemption or compliance under state securities laws which the Company determines to obtain, continuously effective with respect to a Holder, and to keep the applicable
Registration Statement free of any material misstatements or omissions, until the earlier of the following: (i) the second anniversary of the Closing Date or (ii) the date all Common Shares and Conversion Shares held by or issuable to such
Holder may be sold under Rule 144 without being subject to any volume, manner of sale or publicly available information requirements. The period of time during which the Company is required hereunder to keep a Registration Statement effective is
referred to herein as the “Registration Period.”  
 (b) advise the Holders within two
Business Days: 

  
 15 

 (i) when a Registration Statement or any amendment thereto has been filed with the
SEC and when such Registration Statement or any post-effective amendment thereto has become effective; 
 (ii) of any request by the
SEC for amendments or supplements to any Registration Statement or the prospectus included therein or for additional information; 

(iii) of the issuance by the SEC of any stop order suspending the effectiveness of any Registration Statement or the initiation of any
proceedings for such purpose; 
 (iv) of the receipt by the Company of any notification with respect to the suspension of the
qualification of the Registrable Securities included therein for sale in any jurisdiction or the initiation or threatening of any proceeding for such purpose; and 

(v) of the occurrence of any event that requires the making of any changes in any Registration Statement or prospectus so that, as of
such date, the statements therein are not misleading and do not omit to state a material fact required to be stated therein or necessary to make the statements therein (in the case of a prospectus, in the light of the circumstances under which they
were made) not misleading; 
 (c) use its commercially reasonable efforts to obtain the withdrawal of any order suspending the
effectiveness of any Registration Statement as soon as reasonably practicable; 
 (d) if a Holder so requests in writing, promptly
furnish to each such Holder, without charge, at least one copy of each Registration Statement and each post-effective amendment thereto, including financial statements and schedules, and, if explicitly requested, all exhibits in the form filed with
the SEC; 
 (e) during the Registration Period, promptly deliver to each such Holder, without charge, as many copies of each
prospectus included in a Registration Statement and any amendment or supplement thereto as such Holder may reasonably request in writing; and the Company consents to the use, consistent with the provisions hereof, of the prospectus or any amendment
or supplement thereto by each of the selling Holders of Registrable Securities in connection with the offering and sale of the Registrable Securities covered by a prospectus or any amendment or supplement thereto; 

(f) during the Registration Period, if a Holder so requests in writing, deliver to each Holder, without charge, (i) one copy of
the following documents, other than those documents available via EDGAR: (A) its annual report to its stockholders, if any (which annual report shall contain financial statements audited in accordance with generally accepted accounting
principles in the United States by a firm of certified public accountants of recognized standing), (B) if not included in substance in its annual report to stockholders, its annual report on Form 10-K (or
similar form), (C) its definitive proxy statement with respect to its annual meeting of stockholders, (D) each of its quarterly reports to its stockholders, and, if not included in substance in its quarterly reports to stockholders, its
quarterly report on Form 10-Q (or similar form), and (E) a copy of each full Registration Statement (the foregoing, in each case, excluding exhibits); and (ii) if explicitly requested, all exhibits
excluded by the parenthetical to the immediately preceding clause (E); 
 (g) prior to any public offering of Registrable Securities
pursuant to any Registration Statement, promptly take such actions as may be necessary to register or qualify or obtain an exemption for offer and sale under the securities or blue sky laws of such United States jurisdictions as any such Holders
reasonably request in writing, provided that the Company shall not for any such purpose be required to qualify generally to transact business as a foreign corporation in any jurisdiction where it is not so qualified or to consent to general service
of process in any such jurisdiction, and do any and all other acts or things reasonably necessary or advisable to enable the offer and sale in such jurisdictions of the Registrable Securities covered by any such Registration Statement; 

  
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 (h) upon the occurrence of any event contemplated by Section 6.4(b)(v) above,
except for such times as the Company is permitted hereunder to suspend the use of a prospectus forming part of a Registration Statement, the Company shall use its best efforts to as soon as reasonably practicable prepare a post-effective amendment
to such Registration Statement or a supplement to the related prospectus, or file any other required document so that, as thereafter delivered to purchasers of the Registrable Securities included therein, such prospectus will not include any untrue
statement of a material fact or omit to state any material fact necessary to make the statements therein, in the light of the circumstances under which they were made, not misleading; 

(i) otherwise use its commercially reasonable efforts to comply in all material respects with all applicable rules and regulations of
the SEC which could affect the sale of the Registrable Securities; 
 (j) use its commercially reasonable efforts to cause all
Registrable Securities to be listed on each securities exchange or market, if any, on which equity securities issued by the Company have been listed; 

(k) use its commercially reasonable efforts to take all other steps necessary to effect the registration of the Registrable Securities
contemplated hereby and to enable the Holders to sell Registrable Securities under Rule 144; 
 (l) provide to each Purchaser and
its representatives, if requested, the opportunity to conduct a reasonable inquiry of the Company’s financial and other records during normal business hours and make available its officers, directors and employees for questions regarding
information which such Purchaser may reasonably request in order to fulfill any due diligence obligation on its part; and 
 (m)
permit a single counsel for the Purchasers to review any Registration Statement and all amendments and supplements thereto (other than supplements to a Registration Statement on Form S-1 solely for the purpose
of incorporating other filings with the SEC into such Registration Statement and other than an amendment to a Registration Statement on Form S-1 on Form S-3 for the
purpose of converting such Registration Statement into a Registration Statement on Form S-3), within two Business Days prior to the filing thereof with the SEC; 

provided that, in the case of clauses (l) and (m) above, the Company shall not be required (A) to delay the filing of any Registration
Statement or any amendment or supplement thereto as a result of any ongoing diligence inquiry by or on behalf of a Holder or to incorporate any comments to any Registration Statement or any amendment or supplement thereto by or on behalf of a Holder
if such inquiry or comments would require a delay in the filing of such Registration Statement, amendment or supplement, as the case may be, or (B) to provide, and shall not provide, any Purchaser or its representatives with material, non-public information unless such Purchaser agrees to receive such information and enters into a written confidentiality agreement with the Company in a form reasonably acceptable to the Company. 

6.5 The Holders shall have no right to take any action to restrain, enjoin or otherwise delay any registration pursuant to
Section 6.1 hereof as a result of any controversy that may arise with respect to the interpretation or implementation of this Agreement. 

6.6 (a) To the extent permitted by law, the Company shall indemnify each Holder and each Person controlling such Holder within
the meaning of Section 15 of the Securities Act, with respect to which any registration that has been effected pursuant to this Agreement, against all claims, losses, damages and liabilities (or action in respect thereof), including any of the
foregoing incurred in settlement of any litigation, commenced or threatened (subject to Section 6.6(c) below), arising out of or based on any untrue statement (or alleged untrue statement) of a material fact contained in any Registration
Statement, prospectus, any amendment or supplement thereof, or other document incident to any such registration, qualification or 

  
 17 

 
compliance or based on any omission (or alleged omission) to state therein a material fact required to be stated therein or necessary to make the statements therein not misleading, in light of
the circumstances in which they were made, or any violation by the Company of any rule or regulation promulgated by the Securities Act applicable to the Company and relating to any action or inaction required of the Company in connection with any
such registration, qualification or compliance, and will reimburse each Holder and each Person controlling such Holder, for reasonable legal and other out-of-pocket
expenses reasonably incurred in connection with investigating or defending any such claim, loss, damage, liability or action as incurred; provided that the Company will not be liable in any such case to the extent that any untrue statement or
omission or allegation thereof is made in reliance upon and in conformity with written information furnished to the Company by or on behalf of such Holder for use in preparation of any Registration Statement, prospectus, amendment or supplement;
provided further, that the Company will not be liable in any such case where the claim, loss, damage or liability arises out of or is related to the failure of such Holder to comply with the covenants and agreements contained in this Agreement
respecting sales of Registrable Securities, and except that the foregoing indemnity agreement is subject to the condition that, insofar as it relates to any such untrue statement or alleged untrue statement or omission or alleged omission made in
any preliminary prospectus but eliminated or remedied in the amended prospectus on file with the SEC at the time any Registration Statement becomes effective or in an amended prospectus filed with the SEC pursuant to Rule 424(b) which meets the
requirements of Section 10(a) of the Securities Act (each, a “Final Prospectus”), such indemnity shall not inure to the benefit of any such Holder or any such controlling Person, if a copy of a Final Prospectus furnished
by the Company to the Holder for delivery was not furnished to the Person asserting the loss, liability, claim or damage at or prior to the time such furnishing is required by the Securities Act and a Final Prospectus would have cured the defect
giving rise to such loss, liability, claim or damage. 
 (b) Each Holder will severally, and not jointly, indemnify the Company, each
of its directors and officers, and each Person who controls the Company within the meaning of Section 15 of the Securities Act, against all claims, losses, damages and liabilities (or actions in respect thereof), including any of the foregoing
incurred in settlement of any litigation, commenced or threatened (subject to Section 6.6(c) below), arising out of or based on any untrue statement (or alleged untrue statement) of a material fact contained in any Registration Statement,
prospectus, or any amendment or supplement thereof, incident to any such registration, or based on any omission (or alleged omission) to state therein a material fact required to be stated therein or necessary to make the statements therein not
misleading, in light of the circumstances in which they were made, and will reimburse the Company, such directors and officers, and each Person controlling the Company for reasonable legal and any other expenses reasonably incurred in connection
with investigating or defending any such claim, loss, damage, liability or action as incurred, in each case to the extent, but only to the extent, that such untrue statement or omission or allegation thereof is made in reliance upon and in
conformity with written information furnished to the Company by or on behalf of the Holder for use in preparation of any Registration Statement, prospectus, amendment or supplement; provided that the indemnity shall not apply to the extent that such
claim, loss, damage or liability results from the fact that a current copy of a prospectus was not made available to the Person asserting the loss, liability, claim or damage at or prior to the time such furnishing is required by the Securities Act
and a Final Prospectus would have cured the defect giving rise to such loss, claim, damage or liability. Notwithstanding the foregoing, a Holder’s aggregate liability pursuant to this subsection (b) and subsection (d) shall be limited
to the net amount actually received by the Holder from the sale of the Registrable Securities. 
 (c) Each party entitled to
indemnification under this Section 6.6 (the “Indemnified Party”) shall give notice to the party required to provide indemnification (the “Indemnifying Party”) promptly after such Indemnified Party
has actual knowledge of any claim as to which indemnity may be sought, and shall permit the Indemnifying Party (at its expense) to assume the defense of any such claim or any litigation resulting therefrom, provided that counsel for the Indemnifying
Party, who shall conduct the defense of such claim or litigation, shall be approved by the Indemnified Party (whose approval shall not unreasonably be withheld), and the Indemnified 

  
 18 

 
Party may participate in such defense at such Indemnified Party’s expense, and provided further that the failure of any Indemnified Party to give notice as provided herein shall not relieve
the Indemnifying Party of its obligations under this Agreement, unless such failure is materially prejudicial to the Indemnifying Party in defending such claim or litigation. An Indemnifying Party shall not be liable for any settlement of an action
or claim effected without its written consent (which consent will not be unreasonably withheld). No Indemnifying Party, in its defense of any such claim or litigation, shall, except with the consent of each Indemnified Party, consent to entry of any
judgment or enter into any settlement which does not include as an unconditional term thereof the giving by the claimant or plaintiff to such Indemnified Party of a release from all liability in respect to such claim or litigation. 

(d) If the indemnification provided for in this Section 6.6 is held by a court of competent jurisdiction to be unavailable to an
Indemnified Party with respect to any loss, liability, claim, damage or expense referred to therein, then the Indemnifying Party, in lieu of indemnifying such Indemnified Party thereunder, shall contribute to the amount paid or payable by such
Indemnified Party as a result of such loss, liability, claim, damage or expense in such proportion as is appropriate to reflect the relative fault of the Indemnifying Party on the one hand and of the Indemnified Party on the other in connection with
the statements or omissions which resulted in such loss, liability, claim, damage or expense as well as any other relevant equitable considerations. The relative fault of the Indemnifying Party and of the Indemnified Party shall be determined by
reference to, among other things, whether the untrue or alleged untrue statement of a material fact or the omission to state a material fact relates to information supplied by the Indemnifying Party or by the Indemnified Party and the parties’
relative intent, knowledge, access to information and opportunity to correct or prevent such statement or omission. 
 6.7 (a)
Each Holder agrees that, upon receipt of any notice from the Company of the happening of any event requiring the preparation of a supplement or amendment to a prospectus relating to Registrable Securities so that, as thereafter delivered to the
Holders, such prospectus shall not contain an untrue statement of a material fact or omit to state any material fact required to be stated therein or necessary to make the statements therein not misleading, each Holder will forthwith discontinue
disposition of Registrable Securities pursuant to a Registration Statement and prospectus contemplated by Section 6.1 until its receipt of copies of the supplemented or amended prospectus from the Company and, if so directed by the Company,
each Holder shall deliver to the Company all copies, other than permanent file copies then in such Holder’s possession, of the prospectus covering such Registrable Securities current at the time of receipt of such notice. 

(b) Each Holder shall suspend, upon request of the Company, any disposition of Registrable Securities pursuant to any Registration
Statement and prospectus contemplated by Section 6.1 during no more than two periods of no more than 30 calendar days each during any 12-month period to the extent that the Board of Directors of the
Company determines in good faith that the sale of Registrable Securities under any such Registration Statement would be reasonably likely to cause a violation of the Securities Act or Exchange Act. 

(c) As a condition to the inclusion of its Registrable Securities, each Holder shall furnish to the Company such information regarding
such Holder and the distribution proposed by such Holder as the Company may reasonably request in writing, including completing a Registration Statement Questionnaire in the form provided by the Company, or as shall be required in connection with
any registration referred to in this Article 6. 
 (d) Each Holder hereby covenants with the Company (i) not to make any sale
of the Registrable Securities without effectively causing the prospectus delivery requirements under the Securities Act to be satisfied, and (ii) if such Registrable Securities are to be sold by any method or in any transaction other than on a
national securities exchange or in the over-the-counter market, in privately negotiated transactions, or in a 

  
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combination of such methods, to notify the Company at least five Business Days prior to the date on which the Holder first offers to sell any such Registrable Securities. 

(e) At the end of the Registration Period the Holders shall discontinue sales of any Shares or Conversion Shares pursuant to any
Registration Statement upon receipt of notice from the Company of its intention to remove from registration the Shares or Conversion Shares covered by any such Registration Statement which remain unsold, and such Holders shall notify the Company of
the number of Shares or Conversion Shares registered which remain unsold immediately upon receipt of such notice from the Company. 

6.8 With a view to making available to the Holders the benefits of certain rules and regulations of the SEC which at any time permit
the sale of the Registrable Securities to the public without registration, so long as the Holders still own Registrable Securities, the Company shall use its best efforts to: 

(a) make and keep public information available, as those terms are understood and defined in Rule 144 under the Securities Act, at all
times; 
 (b) file with the SEC in a timely manner all reports and other documents required of the Company under the Exchange Act;
and 
 (c) so long as a Holder owns any Registrable Securities, furnish to such Holder, upon any reasonable request, a written
statement by the Company as to its compliance with Rule 144 under the Securities Act, and of the Exchange Act, a copy of the most recent annual or quarterly report of the Company, and such other reports and documents of the Company as such Holder
may reasonably request in availing itself of any rule or regulation of the SEC allowing a Holder to sell any such securities without registration. 

6.9 The rights to cause the Company to register Registrable Securities granted to the Holders by the Company under Section 6.1 may
be assigned by a Holder in connection with a transfer by such Holder of all or a portion of its Registrable Securities, provided, however, that such transfer must be made at least ten days prior to the Filing Date and that (i) such
transfer may otherwise be effected in accordance with applicable securities laws; (ii) such Holder gives prior written notice to the Company at least ten days prior to the Filing Date; and (iii) such transferee agrees to comply with the
terms and provisions of this Agreement, and such transfer is otherwise in compliance with this Agreement. Except as specifically permitted by this Section 6.9, the rights of a Holder with respect to Registrable Securities as set out herein
shall not be transferable to any other Person, and any attempted transfer shall cause all rights of such Holder therein to be forfeited. 

6.10 Prior to the time that Registration Statement(s) covering the resale of all Registrable Securities have been declared effective by
the SEC, the Company shall not file with the SEC a registration statement under the Securities Act of any of its equity securities other than a registration statement required to be filed pursuant to this Agreement; a registration statement on Form S-8 or, in connection with an acquisition, a registration statement on Form S-4; provided, however, that the foregoing restrictions in this Section 6.10 shall
terminate upon such time as all of the Registrable Securities (i) have been publicly sold by the Holders or (ii) may be sold under Rule 144 during any 90-day period. 

6.11 The rights of any Holder under any provision of this Article 6 may be waived (either generally or in a particular instance,
either retroactively or prospectively and either for a specified period of time or indefinitely) or amended by an instrument in writing signed by such Holder. 

ARTICLE 7 
 DEFINITIONS

  
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 7.1 “Aggregate Purchase Price” has the meaning set forth in
Section 6.3. 
 7.2 “Agreement” has the meaning set forth in the preamble. 

7.3 “Affiliate” means, with respect to any Person (as defined below), any other Person controlling, controlled
by or under direct or indirect common control with such Person (for the purposes of this definition “control,” when used with respect to any specified Person,
shall mean the power to direct the management and policies of such Person, directly or indirectly, whether through ownership of voting securities, by contract or otherwise; and the terms
“controlling” and “controlled” shall have meanings correlative
to the foregoing). 
 7.4 “Attribution Parties” means, with respect to any Person, such Person’s
Affiliates and any other Person whose beneficial ownership of Common Stock would be aggregated with such Person’s for purposes of Section 13(d) or Section 16 of the Exchange Act and the applicable regulations of the SEC, including any
“group” of which such Person is a member. 
 7.5 “Beneficial Ownership Limitation” means the
percentage set forth opposite such Purchaser’s name on Exhibit A hereto under the heading “Beneficial Ownership Limitation”. 

7.6 “Business Day” means a day Monday through Friday on which banks are generally open for business in New York
City. 
 7.7 “Class A-3 Certificate of
Designation” means the Certificate of Designation of Rights, Preferences and Privileges of the Class A-3 Convertible Preferred Stock setting forth the preferences, rights and limitations of
the Preferred Shares to be filed prior to the Closing by the Company with the Secretary of State of Delaware substantially in the form attached hereto as Exhibit C. 

7.8 “Closing” has the meaning set forth in Section 1.1(a). 

7.9 “Closing Date” has the meaning set forth in Section 1.1(c). 

7.10 “Common Shares” has the meaning set forth in Recital B to this Agreement. 

7.11 “Common Stock” means the common stock, par value $0.001 per share, of the Company. 

7.12 “Common Stock Equivalents” means any options, warrants or other securities or rights convertible into or
exercisable or exchangeable for, whether directly or following conversion into or exercise or exchange for other options, warrants or other securities or rights, shares of Common Stock, or any swap, hedge or similar agreement or arrangement that
transfers in whole or in part, the economic risk of ownership of, or voting or other rights of, shares of Common Stock. 
 7.13
“Company Intellectual Property” has the meaning set forth in Section 2.13. 
 7.14
“Conversion Shares” has the meaning set forth in Section 2.3. 
 7.15 “Cut Back
Securities” has the meaning set forth in Section 6.1. 
 7.16 “Escrow Agent” means,
Signature Bank, a New York State chartered bank. 
 7.17 “Escrow Agreement” means the escrow agreement
entered into for and prior to the Closing by and among the Company, the Escrow Agent and the Placement Agent pursuant to which the Purchasers shall deposit their applicable Subscription Amounts for the Securities to be sold and purchased at the
Closing. 

  
 21 

 7.18 “Exchange Act” means the Securities Exchange Act of
1934, as amended. 
 7.19 “FDA” means the United States Food and Drug Administration. 

7.20 “Filing Date” has the meaning set forth in Section 6.1. 

7.21 “Final Prospectus” has the meaning set forth in Section 6.6(a). 

7.22 “Financial Statements” means the financial statements of the Company included in the SEC Documents. 

7.23 “Holders” means any Person holding Registrable Securities or any Person to whom the rights under Article 6
have been transferred in accordance with Section 6.9 hereof. 
 7.24 “Indemnified Party” has the meaning
set forth in Section 6.6(c). 
 7.25 “Indemnifying Party” has the meaning set forth in
Section 6.6(c). 
 7.26 “Initial Registration Statement” has the meaning set forth in Section 6.1.

 7.27 “Market Price” means (i) $0.622 for any Purchaser that is not an officer, director, employee or
consultant of the Company and (ii) $0.6301 for any Purchaser that is an officer, director, employee or consultant of the Company. 

7.28 “Material Adverse Effect” means a material adverse effect on (a) the business, operations, assets or
condition (financial or otherwise) of the Company, taken as a whole, or (b) the ability of the Company to perform its obligations pursuant to the transactions contemplated by this Agreement. 

7.29 “Nasdaq” means The Nasdaq Stock Market LLC. 

7.30 “New Registration Statement” has the meaning set forth in Section 6.1. 

7.31 “Penalty Period” has the meaning set forth in Section 6.3. 

7.32 “Person” means any person, individual, corporation, limited liability company, partnership, trust or other
nongovernmental entity or any governmental agency, court, authority or other body (whether foreign, federal, state, local or otherwise). 

7.33 “Placement Agent” means H.C. Wainwright & Co. 

7.34 “Preferred Conversion Shares” has the meaning set forth in Section 2.3. 

7.35 “Preferred Shares” has the meaning set forth in Recital B to this Agreement. 

7.36 “Preferred Stock” means the preferred stock, par value $0.001 per share, of the Company. 

7.37 “Purchasers” has the meaning set forth in the preamble. 

7.38 The terms “register,” “registered” and “registration” refer to the
registration effected by preparing and filing a registration statement in compliance with the Securities Act, and the declaration or ordering of the effectiveness of such registration statement. 

  
 22 

 7.39 “Registrable Securities” means (i) the Common
Shares and (ii) the Conversion Shares; provided, however, that Common Shares and Conversion Shares shall only be treated as Registrable Securities if and only for so long as they (A) have not been disposed of pursuant to a
registration statement declared effective by the SEC, (B) have not been sold in a transaction exempt from the registration and prospectus delivery requirements of the Securities Act so that all transfer restrictions and restrictive legends with
respect thereto are removed upon the consummation of such sale or (C) are held by a Holder or a permitted transferee pursuant to Section 6.9. 

7.40 “Registration Default” has the meaning set forth in Section 6.3. 

7.41 “Registration Expenses” means all expenses incurred by the Company in complying with Section 6.1
hereof, including, without limitation, all registration, qualification and filing fees, printing expenses, escrow fees, fees and expenses of counsel for the Company, blue sky fees and expenses and the expense of any special audits incident to or
required by any such registration (but excluding the fees of legal counsel for any Holder). 
 7.42 “Registration
Statement” means any one or more registration statements of the Company filed under the Securities Act that covers the resale of any of the Registrable Securities pursuant to the provisions of this Agreement (including without
limitation any Initial Registration Statement, any New Registration Statement and any Remainder Registration Statements) and amendments and supplements to such Registration Statements, including post-effective amendments. 

7.43 “Registration Period” has the meaning set forth in Section 6.4(a). 

7.44 “Remainder Registration Statement” has the meaning set forth in Section 6.1. 

7.45 “Rule 144” means Rule 144 promulgated under the Securities Act, or any successor rule. 

7.46 “Rule 415” means Rule 415 promulgated under the Securities Act, or any successor rule. 

7.47 “SEC” means the United States Securities and Exchange Commission. 

7.48 “SEC Documents” has the meaning set forth in Section 2.1. 

7.49 “Securities” has the meaning set forth in Section 1.1(a). 

7.50 “Securities Act” means the Securities Act of 1933, as amended, and the rules and regulations thereunder,
or any similar successor statute. 
 7.51 “Selling Expenses” means all selling commissions applicable to the
sale of Registrable Securities and all fees and expenses of legal counsel for any Holder. 
 7.52 “Shares”
has the meaning set forth in Recital B to this Agreement. 
 7.53 “Subscription Amounts” has the meaning set
forth in Section 5.1(a). 
 7.54 “Trading Day” means a day on which the principal Trading Market is open
for trading. 
 7.55 “Trading Market” means any of the following markets or exchanges on which the Common
Stock is listed or quoted for trading on the date in question: the NYSE American, Nasdaq, or the New York Stock Exchange (or any successors to any of the foregoing). 

  
 23 

 7.56 “Warrants” has the meaning set forth in Recital B to
this Agreement. 
 7.57 “Warrant Shares” has the meaning set forth in Section 2.3. 

7.58 “Warrant Subscription Amount” has the meaning set forth in Section 1.1(b). 

ARTICLE 8 
 GOVERNING
LAW; MISCELLANEOUS 
 8.1 Governing Law; Jurisdiction. This Agreement will be governed by and interpreted in accordance
with the laws of the State of New York without regard to the principles of conflict of laws (whether of the State of New York or any other jurisdiction) which would result in the application of the laws of any other jurisdiction. 

8.2 Counterparts; Signatures by Facsimile. This Agreement may be executed in counterparts, all of which are considered one and
the same agreement and will become effective when counterparts have been signed by each party and delivered to the other parties. This Agreement may also be executed and delivered by facsimile signature, PDF or any electronic signature complying
with the U.S. federal ESIGN Act of 2000 (e.g., www.docusign.com). 
 8.3 Headings. The headings of this Agreement are for
convenience of reference only, are not part of this Agreement and do not affect its interpretation. 
 8.4 Severability. If
any provision of this Agreement is invalid or unenforceable under any applicable statute or rule of law, then such provision will be deemed modified in order to conform with such statute or rule of law. Any provision hereof that may prove invalid or
unenforceable under any law will not affect the validity or enforceability of any other provision hereof. 
 8.5 Entire Agreement;
Amendments. This Agreement (including all schedules and exhibits hereto) constitutes the entire agreement among the parties hereto with respect to the subject matter hereof and thereof. There are no restrictions, promises, warranties or
undertakings, other than those set forth or referred to herein or therein. This Agreement supersedes all prior agreements and understandings among the parties hereto with respect to the subject matter hereof. No provision of this Agreement may be
waived or amended other than by an instrument in writing signed by the party to be charged with enforcement. Any amendment or waiver by a party effected in accordance with this Section 8.5 shall be binding upon such party, including with
respect to any Securities purchased under this Agreement at the time outstanding and held by such party (including securities into which such Securities are convertible and for which such Securities are exercisable) and each future holder of all
such securities. 
 8.6 Notices. All notices required or permitted hereunder shall be in writing and shall be deemed
effectively given: (a) upon personal delivery to the party to be notified, (b) when sent by confirmed email or facsimile if sent during normal business hours of the recipient, and if sent at a time other than during normal business hours
of the recipient, then on the next business day, (c) five days after having been sent by registered or certified mail, return receipt requested, postage prepaid, or (d) one business day after deposit with a nationally recognized overnight
courier, specifying next day delivery, with written verification of receipt. The addresses for such communications are: 
  

			
	 If to the Company:
	  	Regulus Therapeutics Inc.
		  	10628 Science Center Drive, Suite 225
		  	San Diego, CA 92121

  
 24 

			
		  	Attn: Cris Calsada
		  	Email: ccalsada@regulusrx.com
		
	With a copy to:	  	Cooley LLP
		  	4401 Eastgate Mall
		  	San Diego, CA 92121
		  	Attn: Thomas A. Coll
		  	Email: collta@cooley.com

 If to a Purchaser: To the address set forth immediately below such Purchaser’s name on the signature
pages hereto. Each party will provide ten days’ advance written notice to the other parties of any change in its address. 
 8.7
Successors and Assigns. This Agreement is binding upon and inures to the benefit of the parties and their successors and assigns. The Company will not assign this Agreement or any rights or obligations hereunder without the prior written
consent of the Purchasers, and no Purchaser may assign this Agreement or any rights or obligations hereunder without the prior written consent of the Company, except as permitted in accordance with Section 6.9 hereof. 

8.8 Third Party Beneficiaries. This Agreement is intended for the benefit of the parties hereto, their respective permitted
successors and assigns and the Placement Agent, and is not for the benefit of, nor may any provision hereof be enforced by, any other Person. 

8.9 Further Assurances. Each party will do and perform, or cause to be done and performed, all such further acts and things, and
will execute and deliver all other agreements, certificates, instruments and documents, as another party may reasonably request in order to carry out the intent and accomplish the purposes of this Agreement and the consummation of the transactions
contemplated hereby. 
 8.10 No Strict Construction. The language used in this Agreement is deemed to be the language chosen
by the parties to express their mutual intent, and no rules of strict construction will be applied against any party. 
 8.11
Equitable Relief. The Company recognizes that, if it fails to perform or discharge any of its obligations under this Agreement, any remedy at law may prove to be inadequate relief to the Purchasers. The Company therefore agrees that the
Purchasers are entitled to seek temporary and permanent injunctive relief in any such case. Each Purchaser also recognizes that, if it fails to perform or discharge any of its obligations under this Agreement, any remedy at law may prove to be
inadequate relief to the Company. Each Purchaser therefore agrees that the Company is entitled to seek temporary and permanent injunctive relief in any such case. 

8.12 Survival of Representations and Warranties. Notwithstanding any investigation made by any party to this Agreement, all
representations and warranties made by the Company and the Purchasers herein shall survive for a period of one year following the date hereof. 

8.13 Independent Nature of Purchasers’ Obligations and Rights. The obligations of each Purchaser under this Agreement are
several and not joint with the obligations of any other Purchaser, and no Purchaser shall be responsible in any way for the performance of the obligations of any other Purchaser under this Agreement. Nothing contained herein and no action taken by
any Purchaser pursuant thereto, shall be deemed to constitute the Purchasers as a partnership, an association, a joint venture or any other kind of entity, or create a presumption that the Purchasers are in any way acting in concert or as a group,
or are deemed affiliates with respect to such obligations or the transactions contemplated by this Agreement. Each Purchaser shall be entitled to independently protect and enforce its rights, including without limitation the rights arising

  
 25 

 
out of this Agreement, and it shall not be necessary for any other Purchaser to be joined as an additional party in any proceeding for such purpose. The Company has elected to provide all
Purchasers with the same terms of this Agreement for the convenience of the Company and not because it was required or requested to do so by any of the Purchasers. It is expressly understood and agreed that each provision contained in this Agreement
is between the Company and a Purchaser, solely, and not between the Company and the Purchasers collectively and not between and among the Purchasers. Notwithstanding anything to the contrary in the foregoing, each of the Purchasers has been advised,
and is being advised by this Agreement, to consult with an attorney before executing this Agreement, and each Purchaser has consulted (or had an opportunity to consult) with counsel of such Purchaser’s choice concerning the terms and conditions
of this Agreement for a reasonable period of time prior to the execution hereof and thereof. 
 8.14 Waiver of Conflicts. Each
Purchaser acknowledges that Cooley LLP, outside general counsel to the Company, may have in the past performed and may now or in the future represent one or more Purchasers or their affiliates in matters unrelated to the transactions contemplated by
this Agreement (the “Financing”), including representation of such Purchasers or their affiliates in matters of a similar nature to the Financing. The applicable rules of professional conduct require that Cooley LLP inform
the Purchasers hereunder of this representation and obtain their consent. Cooley LLP has served as outside general counsel to the Company and has negotiated the terms of the Financing solely on behalf of the Company. Each Purchaser hereby
(a) acknowledges that they have had an opportunity to ask for and have obtained information relevant to such representation, including disclosure of the reasonably foreseeable adverse consequences of such representation; (b) acknowledges
that with respect to the Financing, Cooley LLP has represented solely the Company, and not any Purchaser or any stockholder, director or employee of the Company or any Purchaser; and (c) gives its informed consent to Cooley LLP’s
representation of the Company in the Financing. 
 [Signature Pages Follow] 

  
 26 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 REGULUS THERAPEUTICS INC. 

			
		
	By:	 	/s/ Joseph P. Hagan
	Name:	 	Joseph P. Hagan
	Title:	 	President and Chief Executive Officer

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
  

			
	 PURCHASER: Atom Master Fund L.P. 

		
	By:	 	/s/ John Cunningham
	Name:	 	John Cunningham
	Title:	 	Authorized Person

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Asymmetry Global Healthcare Fund, L.P. 

			
		
	By:	 	/s/ Chris Zellner
	Name:	 	Chris Zellner
	Title:	 	COO

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
  

			
	PURCHASER: Portland House Partners LLC
		
	By:	 	/s/ Timothy Collins
	Name:	 	Timothy Collins
	Title:	 	President, R&D

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Prelude Opportunity Fund, L.P., Asymmetry Capital Management, LP its Sub-Advisor 

			
		
	By:	 	/s/ Chris Zellner
	Name:	 	Chris Zellner (as its Sub-advisor)
	Title:	 	COO

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Asymmetry Global Healthcare (Master) Fund, Ltd. 

			
		
	By:	 	/s/ Chris Zellner

			
	Name:	 	Chris Zellner
	Title:	 	COO

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
  

			
	PURCHASER: Biotechnology Value Fund, L.P.
		
	 By:
	 	 /s/ Mark Lampert

	 Name:
	 	 Mark Lampert

	 Title:
	 	 Chief Executive Officer BVF I GP LLC, itself General Partner of Biotechnology Value Fund, L.P.

	
	PURCHASER: Biotechnology Value Fund II, L.P.
		
	By:	 	/s/ Mark Lampert
	Name:	 	Mark Lampert
	Title:	 	Chief Executive Officer BVF II GP LLC, itself General Partner of Biotechnology Value Fund II, L.P.
	
	PURCHASER: Biotechnology Value Trading Fund OS, L.P.
		
	By:	 	/s/ Mark Lampert
	Name:	 	Mark Lampert
	Title:	 	President BVF Inc., General Partner of BVF Partners L.P., itself sole member of BVF Partners
OS Ltd., itself GP of Biotechnology Value Trading Fund OS, L.P.
	
	PURCHASER: MSI BVF SPV, L.L.C.
		
	By:	 	/s/ Mark Lampert
	Name:	 	Mark Lampert
	 Title:
	 	 President BVF Inc., General Partner of BVF Partners L.P., itself
attorney-in-fact for MSI BVF SPV, L.L.C.

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: CVI Investments, Inc. 

By: Heights Capital Management, Inc. 

			
		
	By:	 	/s/ Martin Kobinger                
	Name:	 	Martin Kobinger
	 Title:
	 	 Investment Manager

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Growth Equity Opportunities V, LLC 

			
		
	By:	 	 /s/ Louis S. Citron                

	Name:	 	Louis S. Citron
	 Title:
	 	 Chief Legal Officer

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
  

			
	PURCHASER: Point72 Associates, LLC
		
	By:	 	/s/ Vincent Tortorella
	Name:	 	Vincent Tortorella
	Title:	 	Authorized Person

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: USAA Science & Technology Fund, 

a series of USAA Mutual Funds Trust  

			
		
	By:	 	 /s/ Christopher K. Dyer 

	Name:	 	 Christopher K. Dyer 

	Title:	 	 President 

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Victory RS Science and Technology Fund, 

a series of Victory Portfolios 

			
		
	By:	 	 /s/ Christopher K. Dyer 

	Name:	 	 Christopher K. Dyer 

	Title:	 	 President 

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
  

			
	 PURCHASER: Stelios Papadopoulos 

		
	By:	 	 /s/ Stelios Papadopoulos 

	Name:	 	 Stelios Papadopoulos 

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: PENSCO Trust Company 

                    Custodian: FBO Joseph Hagan IRA

			
		
	By:	 	/s/ Sara Estes
	Name:	 	Sara Estes
	Title:	 	Authorized Signatory

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Richard E. Gormley 

			
		
	By:	 	 /s/ Richard E. Gormley 

	Name:	 	Richard E. Gormley

  
 [Signature Page to
Securities Purchase Agreement] 

 IN WITNESS WHEREOF, the undersigned has caused this Securities Purchase Agreement to
be duly executed as of the date first above written. 
 PURCHASER: Noam Rubinstein 

			
		
	By:	 	/s/ Noam Rubinstein
	Name:	 	Noam Rubinstein

  
 [Signature Page to
Securities Purchase Agreement] 

 EXHIBIT A 

SCHEDULE OF PURCHASERS 
  

																	
	 Purchaser
	  	Beneficial
Ownership
Limitation	 	 	Common Shares
Subscription Amount	 	  	Warrant
Subscription Amount	 	  	Aggregate Purchase
Price	 
	 Atom Master Fund L.P.
	  	 	9.99	% 	 	$	800,317.45	 	  	$	120,626.75	 	  	$	920,944.20	 
	 Asymmetry Global Healthcare Fund, L.P.
	  	 	9.99	% 	 	$	401,075.55	 	  	$	60,451.50	 	  	$	461,527.05	 
	 Portland House Partners
	  	 	9.99	% 	 	$	154,927.76	 	  	$	23,351.25	 	  	$	178,279.01	 
	 Prelude Opportunity Fund, LP
	  	 	9.99	% 	 	$	83,453.12	 	  	$	12,578.25	 	  	$	96,031.37	 
	 Asymmetry Global Healthcare (Master) Fund, Ltd.
	  	 	9.99	% 	 	$	60,226.39	 	  	$	9,077.50	 	  	$	69,303.89	 
	 Biotechnology Value Fund, L.P.
	  	 	9.99	% 	 	$	1,130,174.00	 	  	$	170,343.75	 	  	$	1,300,517.75	 
	 Biotechnology Value Fund II, L.P.
	  	 	9.99	% 	 	$	794,077.54	 	  	$	119,686.13	 	  	$	913,763.67	 
	 Biotechnology Value Trading Fund OS, L.P.
	  	 	9.99	% 	 	$	126,425.23	 	  	$	19,055.25	 	  	$	145,480.48	 
	 MSI BVF SPV, L.L.C.
	  	 	9.99	% 	 	$	49,323.98	 	  	$	7,434.25	 	  	$	56,758.23	 
	 CVI Investments, Inc.
	  	 	4.99	% 	 	$	1,000,001.84	 	  	$	150,723.75	 	  	$	1,150,725.59	 
	 Growth Equity Opportunities V, LLC
	  	 	9.99	% 	 	$	4,345,087.98	 	  	$	654,906.75	 	  	$	4,999,994.73	 
	 Point72 Associates, LLC
	  	 	9.99	% 	 	$	2,000,001.19	 	  	$	301,447.13	 	  	$	2,301,448.32	 
	 USAA Science & Technology Fund
	  	 	19.99	% 	 	$	3,900,001.58	 	  	$	587,821.75	 	  	$	4,487,823.33	 
	 Victory RS Science and Technology Fund
	  	 	19.99	% 	 	$	1,100,000.16	 	  	$	165,795.88	 	  	$	1,265,796.03	 
	 Stelios Papadopoulos
	  	 	19.99	% 	 	$	500,001.99	 	  	$	74,393.25	 	  	$	574,395.24	 
	 Pensco Trust Company LLC Custodian FBO Joseph Hagan IRA
	  	 	19.99	% 	 	$	25,002.37	 	  	$	3,720.00	 	  	$	28,722.37	 
	 Richard E. Gormley
	  	 	4.99	% 	 	$	25,001.91	 	  	$	3,768.38	 	  	$	28,770.29	 
	 Noam Rubinstein
	  	 	4.99	% 	 	$	350,001.89	 	  	$	52,753.50	 	  	$	402,755.39	 
	 Total:
	  				 	$	16,845,101.94	 	  	$	2,537,935.00	 	  	$	19,383,036.94	 

 EXHIBIT B 

FORM OF WARRANT 

 EXHIBIT C 

FORM OF CLASS A-3 CERTIFICATE OF DESIGNATION

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