<PAGE>

________________________________________________________________________________
________________________________________________________________________________


                      SECURITIES AND EXCHANGE COMMISSION
                           WASHINGTON, D.C.   20549
                            ______________________

                                  FORM 10-Q

       ( X )   QUARTERLY REPORT PURSUANT TO SECTION 13 OR 15(D) OF THE
               SECURITIES EXCHANGE ACT OF 1934

                FOR THE QUARTERLY PERIOD ENDED MARCH 31, 2001.

       (    )  TRANSITION REPORT PURSUANT TO SECTION 13 OR 15(D) OF THE
               SECURITIES EXCHANGE ACT OF 1934

           FOR THE TRANSITION PERIOD FROM __________ TO __________
                       COMMISSION FILE NUMBER: 0-21643
                        ______________________________

                            CV THERAPEUTICS, INC.
            (Exact name of Registrant as specified in its charter)


                    DELAWARE                           43-1570294
            (State of Incorporation)        (I.R.S. Employer Identification No.)


               3172 PORTER DRIVE, PALO ALTO, CALIFORNIA  94304
         (Address of principal executive offices, including zip code)

      Registrant's telephone number, including area code: (650) 812-0585

    Indicate by check whether the Registrant (1) has filed all reports to be
filed by Section 13 or 15(d) of the Securities and Exchange Act of 1934
during the preceding 12 months (or for such shorter period that the
Registrant was required to file such reports), and (2) has been subject to
such filing requirements for the past 90 days.  Yes   X     No

    The number of shares of Common Stock, $0.001 par value, outstanding as
of April 30, 2001 was 19,748,008.


________________________________________________________________________________
________________________________________________________________________________

<PAGE>

                        PART I.  FINANCIAL INFORMATION
ITEM 1. FINANCIAL STATEMENTS

                                         CV THERAPEUTICS, INC.
                                      CONSOLIDATED BALANCE SHEETS
                          (in thousands, except share and per share amounts)

<TABLE>
<CAPTION>
                                                                             December 31,        March 31,
                                                                                 2000              2001
                                                                              ---------         ---------
                                                                                 (A)            (unaudited)
<S>                                                                          <C>               <C>
                                  ASSETS
Current assets:
  Cash and cash equivalents                                                   $ 54,028          $ 33,436
  Marketable securities                                                        242,165           250,014
  Other current assets                                                           5,739             5,767
                                                                              ---------         ---------
Total current assets                                                           301,932           289,217
Notes receivable from related parties                                              303               301
Property and equipment, net                                                      3,400             3,426
Other assets                                                                     5,998             5,758
                                                                              ---------         ---------
Total assets                                                                  $311,633          $298,702
                                                                              =========         =========

                   LIABILITIES AND STOCKHOLDERS' EQUITY
Current liabilities:
  Accounts payable                                                            $  5,206          $  3,408
  Accrued liabilities                                                            9,343             7,306
  Current portion of capital lease obligation                                      764               781
  Current portion of deferred revenue                                            1,029             1,029
                                                                              ---------         ---------
Total current liabilities                                                       16,342            12,524
Capital lease obligation                                                         1,565             1,363
Convertible subordinated notes                                                 196,250           196,250
Deferred revenue                                                                 5,659             4,402
Other liabilities                                                                   35                 -
                                                                              ---------         ---------
Total liabilities                                                              219,851           214,539
Commitments
Stockholders' equity:
  Preferred stock, $0.001 par value, 5,000,000 shares authorized, none
       issued and outstanding                                                        -                 -
  Common stock, $0.001 par value, 85,000,000 shares authorized, 19,523,045
       and 19,743,342 shares issued and outstanding at December 31, 2000 and
       March 31, 2001, respectively; at amounts paid in                        222,223           227,547
  Deferred compensation                                                           (589)             (310)
  Accumulated deficit                                                         (131,055)         (146,135)
  Cumulative other comprehensive income                                          1,203             3,061
                                                                              ---------         ---------
Total stockholders' equity                                                      91,782            84,163
                                                                              ---------         ---------
Total liabilities and stockholders' equity                                    $311,633          $298,702
                                                                              =========         =========

</TABLE>

(A) Derived from the audited financial statements included in our Annual
    Report on Form 10-K for 2000


                                       See accompanying notes

<PAGE>

                                          CV THERAPEUTICS, INC.
                                  CONSOLIDATED STATEMENTS OF OPERATIONS
                                (in thousands, except per share amounts)
                                              (unaudited)
<TABLE>
<CAPTION>
                                                                             Three months ended March 31,
                                                                              -------------------------
                                                                                 2000            2001
                                                                              ---------       ---------
<S>                                                                          <C>             <C>
Revenues:
  Collaborative research                                                      $      -        $  1,818
Operating expenses:
  Research and development                                                       6,694          16,858
  General and administrative                                                     1,532           2,299
                                                                              ---------       ---------
Total operating expenses                                                         8,226          19,157
                                                                              ---------       ---------
Loss from operations                                                            (8,226)        (17,339)
Interest income                                                                  2,048           4,916
Interest and other expense                                                        (905)         (2,657)
                                                                              ---------       ---------
Net loss                                                                      $ (7,083)       $(15,080)
                                                                              =========       =========
Basic and diluted net loss per share                                          $  (0.39)       $  (0.77)
                                                                              =========       =========
Shares used in computing basic and diluted
  net loss per share                                                            18,247          19,653
                                                                              =========       =========

</TABLE>
                                         See accompanying notes

<PAGE>

                                            CV THERAPEUTICS, INC.
                                    CONSOLIDATED STATEMENTS OF CASH FLOWS
                                               (in thousands)
                                                 (unaudited)
<TABLE>
<CAPTION>
                                                                       Three months ended March 31,
                                                                        -------------------------
                                                                           2000            2001
                                                                        ---------       ---------
<S>                                                                     <C>             <C>
CASH FLOWS FROM OPERATING ACTIVITIES
Net loss                                                                $ (7,083)       $(15,080)
Adjustments to reconcile net loss to net cash used in
  operating activities:
  Amortization of deferred compensation                                      207            (114)
  Depreciation and amortization                                              452             (36)
  Change in assets and liabilities:
    Other current assets                                                     (27)            (28)
    Other assets                                                          (6,293)              -
    Accounts payable                                                        (191)         (1,798)
    Accrued and other liabilities                                          1,010          (2,072)
    Deferred revenue                                                           -          (1,257)
                                                                        ---------       ---------
Net cash used in operating activities                                    (11,925)        (20,385)
CASH FLOWS FROM INVESTING ACTIVITIES
Purchases of investments                                                  (3,549)        (82,600)
Maturities of investments                                                 17,500          77,345
Capital expenditures                                                        (142)           (486)
Notes receivable from officers and employees                                  50               2
                                                                        ---------       ---------
Net cash provided by (used in) investing activities                       13,859          (5,739)
CASH FLOWS FROM FINANCING ACTIVITIES
Payments on capital lease obligations                                        (96)           (185)
Borrowings under convertible subordinated debt, net of issuance costs    196,250               -
Repayments of long-term debt                                              (3,000)              -
Net proceeds from issuance of common stock, net of repurchases               572           5,717
                                                                        ---------       ---------
Net cash provided by (used in) financing activities                      193,726           5,532
                                                                        ---------       ---------
Net increase (decrease) in cash and cash equivalents                     195,660         (20,592)
Cash and cash equivalents at beginning of period                          20,763          54,028
                                                                        ---------       ---------
Cash and cash equivalents at end of period                              $216,423        $ 33,436
                                                                        =========       =========

</TABLE>
                                            See accompanying notes

<PAGE>

                            CV THERAPEUTICS, INC.
                 NOTES TO CONSOLIDATED FINANCIAL STATEMENTS

1.  SUMMARY OF SIGNIFICANT ACCOUNTING POLICIES

    Basis of Presentation

    The accompanying consolidated financial statements of CV Therapeutics,
Inc. have been prepared in accordance with generally accepted accounting
principles, are unaudited and reflect all adjustments (consisting solely of
normal recurring adjustments) which are, in the opinion of management,
necessary to present fairly the financial position at, and the results of
operations, for the interim periods presented. The results of operations for
the three-month period ended March 31, 2001 are not necessarily indicative
of the results to be expected for the entire year ending December 31, 2001
or of future operating results for any interim period. The financial
information included herein should be read in conjunction with our Annual
Report on Form 10-K for the year ended December 31, 2000 which includes the
audited consolidated financial statements and the notes thereto.

    Revenue Recognition

    Revenue under our collaborative research arrangements is recognized
based on the performance requirements of the contract. Payments received
consist of up-front payments, milestones and reimbursements for research
activities. Up-front payments, which are still subject to future performance
requirements, are recorded as deferred revenue and are amortized over the
performance period. Payments received related to substantive, at-risk
milestones are recognized upon completion of the scientific or regulatory
event specified in the underlying agreement. Payments received for research
activities are recognized as the related research effort is incurred.

    Net Loss Per Share

    Net loss per share is computed using the weighted average number of
common shares outstanding. Common equivalent shares have been excluded from
the computation as their effect is antidilutive.

2.  COMPREHENSIVE LOSS

    The components of comprehensive loss for the three months ended March
31, 2000 and 2001 are as follows:

        <TABLE>
        <CAPTION>
                                                                2000            2001
                                                             ---------       ---------
        <S>                                                 <C>             <C>
        (in thousands)
        Net loss                                             $ (7,083)       $(15,080)
        Unrealized gains (losses) on securities                   118           1,858
                                                             ---------       ---------
        Comprehensive loss                                   $ (6,965)       $(13,222)
                                                             =========       =========

        </TABLE>

3.  SUBSEQUENT EVENT

    On April 20, 2001, we filed a Registration Statement on Form S-3, which
has not yet been declared effective, registering up to an aggregate of
$190,000,000 of our common stock, $85,000,000 of which is carried over from
a Registration Statement on Form S-3 that we filed on July 19, 2000 , and
$100,000,000 of which is carried over from a Registration Statement on Form
S-3 that we filed on January 4, 2001, pursuant to Rule 429 of the Securities
Act of 1933, as amended. As an exhibit to the Registration Statement, we
attached the Amended and Restated Common Stock Purchase Agreement, dated as
of August 7, 2000, by and between us and Acqua Wellington North American
Equities Fund, Ltd. ("Acqua Wellington"), which reduced the number of shares
of common stock that we may sell, at a discount to the market price, to Acqua
Wellington to up to $149,000,000.

<PAGE>

ITEM 2.  MANAGEMENT'S DISCUSSION AND ANALYSIS OF FINANCIAL CONDITION AND
RESULTS OF OPERATIONS

    This Management's Discussion and Analysis of Financial Condition and
Results of Operations and other parts of this Report contain forward-looking
statements that involve risks and uncertainties. These statements relate to
future events or our future clinical or product development or financial
performance. In some cases, you can identify forward-looking statements by
terminology such as "may", "will", "should", "expects", "plans",
"anticipates", "believes", "estimates", "predicts", "potential" or
"continue" or the negative of those terms and other comparable terminology.
If one or more of these risks or uncertainties materialize, or if any
underlying assumptions prove incorrect, our actual results, performance or
achievements may vary materially from any future results, performance or
achievements expressed or implied by these forward-looking statements. We
undertake no obligation to publicly update any forward-looking statements,
whether as a result of new information, future events or otherwise. Our
actual results may differ materially from the results discussed in the
forward-looking statements. Factors that might cause such a difference
include, but are not limited to, those discussed in "Risk Factors" as well
as such other risks and uncertainties detailed in our other Securities and
Exchange Commission reports and filings.

OVERVIEW

    CV Therapeutics is a biopharmaceutical company engaged in the discovery,
development and commercialization of new small molecule drugs for the
treatment of cardiovascular diseases. Since our inception in December 1990,
substantially all of our resources have been dedicated to research and
development. To date, we have not generated any product revenues and do not
expect to generate any product revenues for at least several years. As of
March 31, 2001, we had an accumulated deficit of $146.1 million. We expect
our sources of revenues, if any, for the next several years to consist of
payments under corporate partnerships and interest income. The process of
developing our products will require significant additional research and
development, preclinical testing and clinical trials, as well as regulatory
approval. These activities, together with our general and administrative
expenses, are expected to result in operating losses for the foreseeable
future. We will not receive product revenues unless we or our collaborative
partners complete clinical trials and successfully commercialize one or more
of our products.

    We are subject to risks common to biopharmaceutical companies, including
risks inherent in our research and development efforts and clinical trials,
reliance on collaborative partners, enforcement of patent and proprietary
rights, the need for future capital, potential competition and uncertainty
of regulatory approval. In order for a product to be commercialized, it will
be necessary for us and, in some cases, our collaborators, to conduct
preclinical tests and clinical trials, demonstrate efficacy and safety of
our product candidates, obtain regulatory clearances, enter into
manufacturing, distribution and marketing arrangements and obtain market
acceptance. We cannot provide assurance that we will generate revenues or
achieve and sustain profitability in the future.

RESULTS OF OPERATIONS

    Collaborative Research Revenues.  Collaborative research revenues were
$1.8 million for the quarter ended March 31, 2001 while there were none for
the quarter ended March 31, 2000. The collaborative research revenues for
the quarter ended March 31, 2001 included recognition of a $1.0 million
milestone payment from our partner, Biogen Inc., which was released in
connection with their initiation of a phase I oral development program for
Adentri. The remaining revenues relate to our collaboration with Fujisawa
Healthcare, Inc. and consist of both the amortization of up-front payments
and the reimbursement of certain development costs.

    Research and Development Expenses.  Research and development expenses
increased to $16.9 million for the quarter ended March 31, 2001, compared to
$6.7 million for the quarter ended March 31, 2000. The increase was due to
greater external costs associated with ranolazine and our other clinical
programs in addition to hiring additional employees to provide support for
an increased level of activity in our research, development and

<PAGE>

clinical programs. We expect research and development expenses to continue to
increase in the future as we further expand product development efforts and
clinical trials.

    General and Administrative Expenses.  General and administrative
expenses increased to $2.3 million for the quarter ended March 31, 2001,
compared to $1.5 million for the quarter ended March 31, 2000. The increase
was due to additional facility expenses and greater outside legal services
related to general business matters and patents. We expect general and
administrative expenses to continue to increase in the future in line with
our research and development activities.

    Interest Income.  Interest income increased to $4.9 million for the
quarter ended March 31, 2001, compared to $2.0 million for the quarter ended
March 31, 2000. The increase was due to higher average investment balances
as a result of the sale of convertible subordinated notes in March 2000. We
expect that interest income will fluctuate with average investment balances
and market interest rates.

    Interest and Other Expense.   Interest and other expense increased to
$2.7 million for the quarter ended March 31, 2001 compared to $905,000 for
the quarter ended March 31, 2000. The increase was primarily due to interest
expense, related to the convertible subordinated notes issued in March 2000,
which was $2.3 million for the quarter ended March 31, 2001 compared to
$621,000 for the quarter ended March 31, 2000. We expect that interest and
other expense will fluctuate with average loan balances.

LIQUIDITY AND CAPITAL RESOURCES

    We have financed our operations since inception primarily through
private placements and public offerings of debt and equity securities,
equipment and leasehold improvement financing, other debt financing and
payments under corporate collaborations. In May 1999, we entered into a
sales and marketing services agreement with Innovex Inc. pursuant to which
Innovex's parent, Quintiles Transnational Corp., purchased 1,043,705 shares
of our common stock for a total investment of $5.0 million. In addition, we
entered into two promissory notes with Quintiles. The first promissory note
in the amount of $10.0 million may be drawn down by us upon filing a New
Drug Application for ranolazine. The second promissory note shall be for an
amount to be determined after commercial launch of ranolazine. Both notes
are convertible into shares of common stock at the option of Quintiles upon
the occurrence of certain events. In October 1999, we completed a follow-on
public offering and raised net proceeds of approximately $64.3 million. In
March 2000, we entered into a purchase agreement pursuant to which we sold
to certain purchasers $196.3 million in aggregate principal amount of
convertible subordinated notes. The offering of the notes was made to
qualified institutional buyers under Rule 144A of the Securities Act of
1933, as amended. Interest on the notes will accrue at a rate of 4.75% per
year, subject to adjustment in certain circumstances. The notes will mature
on March 7, 2007 and are convertible into shares of our common stock at a
conversion price of $63.84 per share, subject to adjustment in certain
circumstances. We may, at our option, redeem the notes at any time after
March 7, 2003 or earlier if our stock price reachs certain defined levels.
In March 2000, we repaid the initial $3.0 million installment under a loan
facility with Biogen, bringing the outstanding balance to $4.5 million. In
July 2000 we entered into a collaboration with Fujisawa Healthcare, Inc. to
develop and market second generation pharmacologic cardiac stress agents.
Under this agreement we received $10.0 million from Fujisawa Healthcare,
Inc. consisting of an up-front payment and the purchase of our common stock.
In August 2000, we received a financing commitment from Acqua Wellington
North American Equities Fund, Ltd. to purchase up to $120 million of our
common stock through November 2002. In August 2000, we drew down an
additional $4.5 million under a general purpose loan facility with Biogen
bringing the outstanding balance to $9.0 million. In October 2000, we
exercised our right to convert $9.0 million in debt from the Biogen loan
facility into 118,932 shares of our common stock at a price of $75.67 per
share, in full repayment of the entire principal amount under this loan
facility. In December 2000, we repaid all accrued and unpaid interest on the
loan facility, in full repayment of the loan facility. In February 2001, we
amended the common stock purchase agreement with Acqua Wellington North
American Equities Fund, Ltd. to allow for the sale of up to an aggregate of
$220 million of our common stock, an increase of $100 million. As described
under "Subsequent Event" above, we amended the common stock purchase agreement
again to reduce

<PAGE>

the number of shares to an aggregate of $149 million of our common stock. As
of March 31, 2001 we have issued shares representing $35.0 million under this
commitment.

    Cash, cash equivalents and marketable securities at March 31, 2001
totaled $283.5 million compared to $296.2 million at December 31, 2000. The
decrease was due to utilizing $20.4 million to fund operations offset by
$5.7 million raised from the issuance of our common stock, including $5.0
million of common stock issued pursuant to our agreement with Acqua Wellington.

    Net cash used in operations for the three months ended March 31, 2001
was $20.4 million compared to $11.9 million for the three months ended March
31, 2000. The increase was primarily due to increased research and
development efforts.

    As of March 31, 2001, we have invested $11.1 million in property and
equipment with the rate of investment having increased in line with
increased research and development efforts. We expect to continue to make
investments in property and equipment to support our growth.

    We may require substantial additional funding in order to complete our
research and development activities and commercialize any potential
products. We currently estimate that our existing resources and projected
interest income will enable us to maintain our current and planned
operations for at least the next 24 months. However, we cannot assure you
that we will not require additional funding prior to then or that additional
financing will be available on acceptable terms or at all.

    Our future capital requirements will depend on many factors, including
scientific progress in our research and development programs, the size and
complexity of these programs, the scope and results of preclinical studies
and clinical trials, our ability to establish and maintain corporate
partnerships, the time and costs involved in obtaining regulatory approvals,
the costs involved in filing, prosecuting and enforcing patent claims,
competing technological and market developments, the cost of manufacturing
preclinical and clinical material and other factors not within our control.
We cannot guarantee that the additional financing to meet our capital
requirements will be available on acceptable terms or at all. Insufficient
funds may require us to delay, scale back or eliminate some or all of our
research or development programs, to lose rights under existing licenses or
to relinquish greater or all rights to product candidates at an earlier
stage of development or on less favorable terms than we would otherwise
choose or may adversely affect our ability to operate as a going concern. If
additional funds are raised by issuing equity securities, substantial
dilution to existing stockholders may result.

RISK FACTORS

    OUR PRODUCT CANDIDATES WILL TAKE AT LEAST SEVERAL YEARS TO DEVELOP, AND
WE CANNOT ASSURE YOU THAT WE WILL SUCCESSFULLY DEVELOP, MARKET AND
MANUFACTURE THESE PRODUCTS.

    Since our inception in 1990, we have dedicated substantially all of our
resources to research and development. We do not have any marketed products,
and we have not generated any product revenue. Because all of our potential
products are in research, preclinical or clinical development, we will not
realize product revenues for at least several years, if at all.

    We have not applied for or received regulatory approval in the United
States or any foreign jurisdiction for the commercial sale of any of our
products. All of our product candidates are either in clinical trials under
an Investigational New Drug, or IND, or applicable foreign authority
submission, or are in preclinical research and development. We have not
submitted an NDA to the FDA or equivalent application to any other foreign
regulatory authorities for any of our product candidates, and the products
have not been determined to be safe or effective in humans for their
intended uses.

<PAGE>

    Conducting clinical trials is a lengthy, time-consuming and expensive
process. Before obtaining regulatory approvals for the commercial sale of
any products, we must demonstrate through preclinical testing and clinical
trials that our product candidates are safe and effective for use in humans.
We will incur substantial expense for, and devote a significant amount of
time to, preclinical testing and clinical trials.

    Drug discovery methods based upon molecular cardiology are relatively
new. We cannot be certain that these methods will lead to commercially
viable pharmaceutical products. In addition, some of our compounds within
our adenosine receptor research, metabolism, atherosclerosis and cell cycle
inhibition programs are in the early stages of research and development, and
we have not submitted IND applications or commenced clinical trials for
these new compounds. We cannot be certain when these clinical trials will
commence, if at all. Because these compounds are in the early stages of
product development, we could abandon further development efforts before
they reach clinical trials.

    We cannot be certain that any of our product development efforts will be
successfully completed or that any of our products will be shown to be safe
and effective. Even if we believe that any product is safe and effective, we
may not obtain the required regulatory approvals. Furthermore, we may not be
able to manufacture our products in commercial quantities or market any
products successfully.

    IF WE ARE UNABLE TO SATISFY THE REGULATORY REQUIREMENTS FOR OUR CLINICAL
TRIALS, WE WILL NOT BE ABLE TO COMMERCIALIZE OUR DRUG CANDIDATES.

    All of our products may require additional development, preclinical
studies and clinical trials, and will require regulatory approval, prior to
commercialization. Any delays in our clinical trials would delay market
launch and would increase our cash requirements.

    We currently have only three products in clinical development:
ranolazine, CVT-510 and CVT-3146. Many factors could delay completion of our
clinical trials, including:

    *       slower than anticipated patient enrollment

    *       difficulty in obtaining sufficient supplies of clinical trial
            materials

    *       adverse events occurring during the clinical trials

    For example, our first Phase III clinical trial of ranolazine, called
Monotherapy Assessment of Ranolazine In Stable Angina or MARISA, had
challenging enrollment criteria. These criteria required patients who suffer
from angina to stop taking all of their other anti-anginal medications and
receive only placebo during segments of the clinical trial. This meant that
they received no medication to treat their angina when they received
placebo. Given the difficulty of identifying patients willing to completely
stop taking anti-anginal medications, enrollment for this trial was slower
than anticipated.

    In addition, data obtained from preclinical and clinical activities are
susceptible to different interpretations, which could delay, limit or
prevent regulatory approval. Delays or rejections may be based upon many
factors, including changes in regulatory policy during the period of product
development. For example, the initial clinical trials with ranolazine used a
different formulation of ranolazine than we used in the MARISA trials and we
are using in the second Phase III clinical trial of ranolazine, called
Combination Assessment of Ranolazine In
Stable Angina or CARISA. This means that the NDA will contain data from
trials using two different formulations and is subject to interpretation by
the FDA. An unfavorable interpretation could result in actions by the FDA
that would delay potential approval. We may be unable to maintain our
proposed schedules for IND applications and clinical protocol submissions to
the FDA, initiations of clinical trials and completions of clinical trials
as a result of FDA reviews or complications that may arise in any phase of
the clinical trial program.

<PAGE>

    Furthermore, even if our clinical trials occur on schedule, the results
may differ from those obtained in preclinical studies and earlier clinical
trials. Clinical trials may not demonstrate sufficient safety and efficacy
to obtain the necessary approvals. For example, in November 1995, based on
unfavorable efficacy data from a Phase II trial, we terminated a prior
development program.

    IF WE ARE UNABLE TO SATISFY GOVERNMENTAL REGULATIONS RELATING TO THE
DEVELOPMENT OF OUR DRUG CANDIDATES, WE MAY BE UNABLE TO OBTAIN OR MAINTAIN
NECESSARY REGULATORY APPROVALS TO COMMERCIALIZE OUR PRODUCTS.

    The research, testing, manufacturing and marketing of drug products are
subject to extensive regulation by numerous regulatory authorities in the
United States and other countries. Failure to comply with FDA or other
applicable regulatory requirements may subject a company to administrative
or judicially imposed sanctions. These include:

    *       warning letters

    *       civil penalties

    *       criminal penalties

    *       injunctions

    *       product seizure or detention

    *       product recalls

    *       total or partial suspension of production

    *       FDA refusal to approve pending NDAs or supplements to approved NDAs

    The process of obtaining FDA and other required regulatory approvals,
including foreign approvals, often takes many years and can vary
substantially based upon the type, complexity and novelty of the products
involved. Furthermore, this approval process is extremely expensive and
uncertain. We cannot guarantee that any of our products under development
will be approved for marketing by the FDA or corresponding foreign
regulatory authorities. Even if regulatory approval of a product is granted,
we cannot be certain that we will be able to obtain the labeling claims
necessary or desirable for the promotion of those products.

    Even if we obtain regulatory approval, we may be required to undertake
postmarketing trials. In addition, identification of side effects after a
drug is on the market or the occurrence of manufacturing problems could
cause subsequent withdrawal of approval, reformulation of the drug,
additional preclinical testing or clinical trials, changes in labeling of
the product, and additional marketing applications.

    If we receive regulatory approval, we will also be subject to ongoing
FDA obligations and continued regulatory review, such as continued safety
reporting requirements, and we may also be subject to additional FDA
post-marketing obligations. In addition, we or our third party manufacturers
will be required to adhere to federal regulations setting forth current good
manufacturing practices, known as cGMP. The regulations require that we
manufacture our products and maintain our records in a prescribed manner
with respect to manufacturing, testing and quality control activities.
Furthermore, we or our third party manufacturers must pass a preapproval
inspection of manufacturing facilities by the FDA and foreign authorities
before obtaining marketing approval, and will be subject to periodic
inspection by the FDA and corresponding foreign regulatory authorities under
reciprocal agreements with the FDA. There can be no guarantee that such
inspections will not result in compliance issues that could prevent or delay
marketing approval, or require the expenditure of money or other

<PAGE>

resources to correct. In addition, drug product manufacturing facilities in
California must be licensed by the State of California, and other states may
have comparable requirements.

    If we receive regulatory approval and if any of our products or services
become reimbursable by a government health care program, such as Medicare or
Medicaid, we may become subject to certain federal and state health care
fraud and abuse and reimbursement laws. These laws include the federal
"Anti-Kickback Statute," "False Claims Act," and "Physician Self-Referral
Law," and their state counterparts. If and when we become subject to such
laws, our arrangements with third parties, including health care providers,
physicians, vendors, and Innovex, will need to comply with these laws as
applicable. We do not know whether our existing or future arrangements will
be found to be compliant. Violations of these statutes could result in
criminal and civil penalties and exclusion from governmental health care
programs.

    OUR PRODUCTS, EVEN IF APPROVED BY THE FDA OR FOREIGN REGULATORY
AGENCIES, MAY NOT BE ACCEPTED BY PHYSICIANS, INSURERS OR PATIENTS.

    If any of our products after receiving FDA or other foreign regulatory
approval fail to achieve market acceptance, our ability to become profitable
in the future will be adversely affected. We believe that market acceptance
will depend on our ability to provide acceptable evidence of safety,
efficacy and cost effectiveness. In addition, we believe market acceptance
depends on the effectiveness of our marketing strategy and the availability
of reimbursement for our products.

    WE HAVE NO MARKETING OR SALES EXPERIENCE, AND IF WE ARE UNABLE TO ENTER
INTO OR MAINTAIN COLLABORATIONS WITH MARKETING PARTNERS OR IF WE ARE UNABLE
TO DEVELOP OUR OWN SALES AND MARKETING CAPABILITY, WE MAY NOT BE SUCCESSFUL
IN COMMERCIALIZING OUR PRODUCTS.

    We currently have no sales or distribution capability and only limited
marketing capability. As a result, we depend on collaborations with third
parties, such as Innovex, a subsidiary of Quintiles Transnational Corp.,
Biogen Inc. and Fujisawa Healthcare, Inc., which have established
distribution systems and direct sales forces. For instance, we have entered
into a sales and marketing services agreement with Innovex with respect to
ranolazine. Innovex will market and sell ranolazine in the United States
using a dedicated sales force if and when FDA approval to market ranolazine
has been granted. Commercialization of ranolazine depends on Innovex to
perform their contractual obligations. Their failure to do so would
adversely affect commercialization of ranolazine. To the extent that we
enter into co-promotion or other licensing arrangements, our revenues will
depend upon the efforts of third parties, over which we may have little
control. In addition, Biogen is responsible for establishing marketing and
sales activities for any product that results from the AdentriTM program and
Fujisawa is responsible for establishing marketing and sales activities for
CVT-3146.

    If we are unable to reach and maintain agreement with one or more
pharmaceutical companies or collaborative partners, we may be required to
market our products directly. We may elect to establish our own specialized
sales force and marketing organization to market our products to
cardiologists. In order to do this, we would have to develop a marketing and
sales force with technical expertise and with supporting distribution
capability. Developing a marketing and sales force is expensive and time
consuming and could delay any product launch. We cannot be certain that we
will be able to develop this capacity.

    OUR BUSINESS DEPENDS ON ATTRACTING AND RETAINING COLLABORATORS AND
LICENSORS.

    We may not be able to retain current or attract new corporate and
academic collaborators, licensors, licensees and others. Our business
strategy requires us to enter into various arrangements with these parties,
and we are dependent upon the success of these parties in performing their
obligations. If we fail to obtain and maintain these arrangements, the
development of our products would be delayed. We may be unable to proceed
with the development, manufacture or sale of products or we might have to
fund development of a particular product

<PAGE>

candidate internally. If we have to fund development and commercialization of
all of our products internally, our future capital requirements will increase
substantially.

    The collaborative arrangements that we may enter into in the future may
place responsibility on the collaborative partner for preclinical testing
and clinical trials, manufacturing and preparation and submission of
applications for regulatory approval of potential pharmaceutical products.
We cannot control the amount and timing of resources which our collaborative
partners devote to our programs. If a collaborative partner fails to
successfully develop or commercialize any product, product launch would be
delayed. In addition, collaborators may pursue competing technologies or
product candidates.

    Under our collaborative arrangements, we or our collaborative partners
may also have to meet performance milestones. If we fail to meet our
obligations under our collaborative arrangements, our collaborators could
terminate their arrangements or we could lose rights to the compounds under
development. For example, under our agreement with Innovex, we are required
to launch the product by a specific date. If we fail to reach this
milestone, Innovex will no longer be obligated to provide sales and
marketing services for ranolazine. Under our agreement with Biogen, in order
for us to receive development milestone payments, Biogen must meet
development milestones. Under our license agreement with Syntex U.S.A. Inc.
for ranolazine, we are required to make milestone payments to Syntex
following FDA approval of ranolazine and following regulatory approval of
ranolazine in Europe. These payments are due no later than March 31, 2005
and March 31, 2006, respectively. Under our agreement with Fujisawa, we are
responsible for development activities and must meet development milestones
in order to receive development milestone payments.

    In addition, collaborative arrangements in our industry are extremely
complex, particularly with respect to intellectual property rights. Disputes
may arise in the future with respect to the ownership of rights to any
technology developed with or by third parties. These and other possible
disagreements between us and our collaborators could lead to delays in the
collaborative research, development or commercialization of product
candidates. These disputes could also result in litigation or arbitration,
which is time consuming and expensive.

    WE EXPECT TO CONTINUE TO OPERATE AT A LOSS AND MAY NEVER ACHIEVE
PROFITABILITY.

    We cannot be certain that we will ever achieve and sustain
profitability. Since our inception, we have been engaged in research and
development activities. We have generated no product revenues. As of March
31, 2001, we had an accumulated deficit of $146.1 million. The process of
developing our products requires significant additional research and
development, preclinical testing and clinical trials, as well as regulatory
approvals. These activities, together with our general and administrative
expenses, are expected to result in operating losses for the foreseeable
future.

    WE MUST SECURE ADDITIONAL FINANCING TO MEET OUR FUTURE NEEDS.

    We may require substantial additional funding in order to complete our
research and development activities and commercialize any products. In the
past, we have financed our operations primarily through the sale of equity
and debt securities, payments from our collaborators, equipment and
leasehold improvement financing and other debt financing. We have generated
no product revenue, and none is expected for at least several years. We
anticipate that our existing resources and projected interest income will
enable us to maintain our current and planned operations for at least the
next 24 months. However, we may require additional funding prior to that
time.

    Additional financing may not be available on acceptable terms or at all.
If we are unable to raise additional funds, we may, among other things:

    *       have to delay, scale back or eliminate some or all of our
            research or development programs

<PAGE>

    *       lose rights under existing licenses

    *       have to relinquish more of, or all of, our rights to product
            candidates at an earlier stage of development or on less
            favorable terms than we would otherwise seek

    *       be unable to operate as a going concern

    Our future capital requirements will depend on many factors, including:

    *       scientific progress in our research and development programs

    *       the size and complexity of our programs

    *       the timing, scope and results of preclinical studies and
            clinical trials

    *       our ability to establish and maintain corporate partnerships

    *       the time and costs involved in obtaining regulatory approvals

    *       the costs involved in filing, prosecuting and enforcing patent
            claims

    *       competing technological and market developments

    *       the cost of manufacturing or obtaining preclinical and clinical
            material

    If additional funds are raised by issuing equity securities, substantial
dilution to existing stockholders may result. There may be additional
factors that could affect our need for additional financing. Many of these
factors are not within our control.

    INABILITY TO COMPETE SUCCESSFULLY IN OUR MARKET WILL HARM OUR BUSINESS.

    The pharmaceutical and biopharmaceutical industries, and the market for
cardiovascular drugs in particular, are intensely competitive. If regulatory
approvals are received, some of our products will compete with
well-established, proprietary and generic cardiovascular therapies that have
generated substantial sales over a number of years. Many of these therapies
are reimbursed from government health administration authorities and private
health insurers.

    In addition, we are aware of companies which are developing products
that may compete in the same markets as our products. Many of these
potential competitors have substantially greater product development
capabilities and financial, scientific, marketing and sales resources. Other
companies may succeed in developing products earlier or obtain approvals
from the FDA more rapidly than either we or our corporate partners are able
to achieve. Competitors may also develop products that are safer or more
effective than those under development or proposed to be developed by us and
our corporate partners. In addition, research and development by others
could render our technology or our products obsolete or non-competitive.

    WE MAY BE UNABLE TO EFFECTIVELY PROTECT OUR INTELLECTUAL PROPERTY.

    Our success will depend to a significant degree on our ability to:

    *       obtain patents and licenses to patent rights

    *       maintain trade secrets

<PAGE>

    *       operate without infringing on the proprietary rights of others

    We cannot be certain that patents will issue from any of our pending or
future patent applications, that any issued patent will be sufficient to
protect our technology and investments or that we will be able to obtain
extensions of patents beyond the initial term. For example, a primary patent
relating to ranolazine will expire in May 2003 unless we are granted an
extension based upon the Waxman-Hatch Act, which we anticipate would extend
the patent protection for an additional five years.

    Patent applications in the United States are maintained in secrecy until
a patent issues. As a result, we can never be certain that others have not
filed patent applications for technology covered by our pending applications
or that we were the first to invent the technology. There may be third party
patents, patent applications and other intellectual property relevant to our
products and technology which are not known to us and that block or compete
with our compounds, products or processes.

    Competitors may have filed applications for, or may have received
patents and may obtain additional patents and proprietary rights relating
to, compounds, products or processes that block or compete with ours. We may
have to participate in interference proceedings declared by the Patent and
Trademark Office. These proceedings determine the priority of invention and,
thus, the right to a patent for the technology in the United States. In
addition, litigation may be necessary to enforce any patents issued to us or
to determine the scope and validity of the proprietary rights of third
parties. Litigation and interference proceedings, even if they are
successful, are expensive to pursue, and we could use a substantial amount
of our limited financial resources in either case.

    Just as it is important to protect our proprietary rights, we also must
not infringe patents issued to competitors and not breach the licenses that
might cover technology used in our potential products. If our competitors
own or have rights to technology that we need in our product development
efforts, we will need to obtain a license to those rights. If we fail to
obtain any necessary licenses, we may be unable to complete product
development.

    We also rely on trade secrets to develop and maintain our competitive
position. Although we protect our proprietary technology in part by
confidentiality agreements with employees, consultants, collaborators,
advisors and corporate partners, these agreements may be breached. We cannot
assure you that these agreements will provide this meaningful protection or
adequate remedies in the event of unauthorized use or disclosure of this
information. We also cannot assure you that the parties to these agreements
will not breach them. In that event, we may not have adequate remedies for
any breach. As a result, third parties may gain access to our trade secrets,
and third parties may disclose our trade secrets and confidential technology
to the public. In addition, it is possible that our trade secrets will
otherwise become known or be discovered independently by our competitors.

    Patent litigation is becoming more widespread in the biopharmaceutical
industry. Although no third party has asserted a claim of infringement
against us, we cannot assure you that third parties will not assert patent
or other intellectual property infringement claims against us with respect
to our products or technology or other matters. If they do, we may not
prevail and, as a result, may be subject to significant liabilities to third
parties or may be required to license the disputed rights from the third
parties or cease using the technology. We may not be able to obtain any
necessary licenses on reasonable terms, if at all. Any such claims against
us, with or without merit, as well as claims initiated by us against third
parties, can be time-consuming and expensive to defend or prosecute.

    WE HAVE NO MANUFACTURING EXPERIENCE AND WILL DEPEND ON THIRD PARTIES TO
MANUFACTURE OUR PRODUCTS.

    We do not currently operate manufacturing facilities for clinical or
commercial production of our products under development. We have no
experience in manufacturing and currently lack the resources or capability
to manufacture any of our products on a clinical or commercial scale. As a
result, we are dependent on corporate partners, licensees or other third
parties for the manufacturing of clinical and commercial scale quantities of
our products.

<PAGE>

    For example, we have entered into agreements with third party
manufacturers for clinical scale production of ranolazine's active
pharmaceutical ingredient and for ranolazine tableting, which we believe are
sufficient to support the remainder of the Phase III program to support
filing of an NDA for ranolazine for chronic angina. In addition, we have
entered into several other manufacturing agreements relating to ranolazine,
including for commercial scale or scale-up of bulk active pharmaceutical
ingredient, tableting, and supply of a raw material component of the
product. However, commercial launch of ranolazine is dependent on these
third party arrangements, and could be affected by delays or difficulties in
performance. In addition, because we have used various manufacturers for
ranolazine in different clinical trials prior to FDA approval of ranolazine,
we will be required to demonstrate to the FDA's satisfaction the
bioequivalence of the multiple sources of ranolazine used in our clinical
trials and their bioequivalence to the product to be commercially supplied.

    FAILURE TO OBTAIN ADEQUATE REIMBURSEMENT FROM GOVERNMENT HEALTH
ADMINISTRATION AUTHORITIES, PRIVATE HEALTH INSURERS AND OTHER ORGANIZATIONS
COULD MATERIALLY ADVERSELY AFFECT OUR FUTURE BUSINESS, RESULTS OF OPERATIONS
AND FINANCIAL CONDITION.

    Our ability and the ability of our existing and future corporate
partners to market and sell our products will depend in part on the extent
to which reimbursement for the cost of our products and related treatments
will be available from government health administration authorities, private
health insurers and other organizations. Third party payors are increasingly
challenging the price of medical products and services.

    Significant uncertainty exists as to the reimbursement status of newly
approved health care products. In addition, for sales of our products in
Europe, we will be required to seek reimbursement on a country-by-country
basis. We cannot be certain that any products approved for marketing will be
considered cost effective or that reimbursement will be available or that
allowed reimbursement in foreign countries will be adequate. In addition,
payors' reimbursement policies could adversely affect our or any corporate
partner's ability to sell our products on a profitable basis.

    OUR BUSINESS DEPENDS ON CERTAIN KEY EXECUTIVES, THE LOSS OF WHOM COULD
WEAKEN OUR MANAGEMENT TEAM, AND ON ATTRACTING AND RETAINING QUALIFIED
PERSONNEL.

    The growth of our business and success depends in large part on our
ability to attract and retain key management, technical, sales and marketing
and other operating personnel. There can be no assurance that we will be
able to attract and retain the qualified personnel or develop the expertise
in these areas as needed for our business. The loss of the services of one
or more members of these groups or the inability to attract and retain
additional personnel and develop expertise as needed could limit our ability
to develop and commercialize our existing drugs and future drug candidates.
Such persons are in high demand and often receive competing employment offers.

    OUR OPERATIONS INVOLVE HAZARDOUS MATERIALS, WHICH COULD SUBJECT US TO
SIGNIFICANT LIABILITY.

    Our research and development activities involve the controlled use of
hazardous materials, including hazardous chemicals, radioactive materials
and pathogens, and the generation of waste products. Accordingly, we are
subject to federal, state and local laws governing the use, handling and
disposal of these materials. We may incur significant costs to comply with
additional environmental and health and safety regulations in the future.
Although we believe that our safety procedures for handling and disposing of
hazardous materials comply with regulatory requirements, we cannot eliminate
the risk of accidental contamination or injury from these materials. In the
event of an accident or environmental discharge, we may be held liable for
any resulting damages, which may exceed our financial resources and may
materially adversely affect our business, financial condition and results of
operations. Although we believe that we are in compliance in all material
respects with applicable environmental laws and regulations, there can be no
assurance that we will not be required to incur significant costs to comply
with environmental laws and regulations in the future. There can also be no
assurance that our

<PAGE>

operations, business or assets will not be materially adversely affected by
current or future environmental laws or regulations.

    WE MAY BE SUBJECT TO PRODUCT LIABILITY CLAIMS IF OUR PRODUCTS HARM
PEOPLE, AND WE HAVE ONLY LIMITED PRODUCT LIABILITY INSURANCE.

    The manufacture and sale of human therapeutic products involve an
inherent risk of product liability claims and associated adverse publicity.
We currently have only limited product liability insurance for clinical
trials and no commercial product liability insurance. We do not know if we
will be able to maintain existing or obtain additional product liability
insurance on acceptable terms or with adequate coverage against potential
liabilities. This type of insurance is expensive and may not be available on
acceptable terms. If we are unable to obtain or maintain sufficient
insurance coverage on reasonable terms or to otherwise protect against
potential product liability claims, we may be unable to commercialize our
products. A successful product liability claim brought against us in excess
of our insurance coverage, if any, may require us to pay substantial
amounts. This could adversely affect our results of operations and our need
for and the timing of additional financing.

    THE MARKET PRICE OF OUR STOCK MAY CONTINUE TO BE HIGHLY VOLATILE.

    Within the last 12 months, our common stock has traded between $21.08
and $93.13. The market price of the shares of common stock for our company
has been and may continue to be highly volatile. Announcements may have a
significant impact on the market price of our common stock. These
announcements may include:

    *       results of our clinical trials and preclinical studies, or those
            of our corporate partners or our competitors

    *       our operating results

    *       developments in our relationships with corporate partners

    *       developments affecting our corporate partners

    *       negative regulatory action or regulatory approval with respect
            to our announcement or our competitors' announcement of new
            products

    *       government regulations, reimbursement changes and governmental
            investigations or audits related to us or to our products

    *       developments related to our patents or other proprietary rights
            or those of our competitors

    *       changes in the position of securities analysts with respect to
            our stock

    *       operating results below the expectations of public market
            analysts and investors

    *       market conditions for biopharmaceutical or biotechnology stocks
            in general

    The stock market has from time to time experienced extreme price and
volume fluctuations, which have particularly affected the market prices for
emerging biotechnology and biopharmaceutical companies, and which have often
been unrelated to their operating performance. These broad market
fluctuations may adversely affect the market price of our common stock. In
addition, sales of substantial amounts of our common stock in the public
market could lower the market price of our common stock.

<PAGE>

    DELAWARE LAW, PROVISIONS IN OUR CHARTER AND OUR RIGHTS PLAN COULD MAKE
THE ACQUISITION OF OUR COMPANY BY ANOTHER COMPANY MORE DIFFICULT.

    Provisions of our certificate of incorporation may have the effect of
delaying or preventing changes in control or management or limit the price
that investors may be willing to pay for shares of our common stock. In
addition, we are subject to the provisions of Section 203 of the Delaware
General Corporation Law, an anti-takeover law, which could delay a merger,
tender offer or proxy contest or make a similar transaction more difficult.
In addition, our board of directors has the authority to issue up to
5,000,000 shares of preferred stock without stockholders' approval. The
rights of the holders of common stock will be subject to, and may be
affected by, the rights of the holders of any preferred stock that may be
issued in the future. The issuance of preferred stock could have the effect
of making it more difficult for a third party to acquire a majority of our
outstanding voting stock.

    Furthermore, in February 1999, the board of directors enacted
anti-takeover provisions, including a stockholder rights plan, and
authorized severance agreements in the event of a change of control for key
executives. The board of directors amended the stockholders rights plan in
July 2000 to lower the triggering ownership percentage and increase the
exercise price while maintaining the plan in effect.

ITEM 3. MARKET RISK

    Our exposure to market rate risk for changes in interest rates relates
primarily to our investment portfolio. As of March 31, 2001 no significant
changes have occurred since our Annual Report on Form 10-K for the year
ended December 31, 2000.

<PAGE>

                         PART II.  OTHER INFORMATION


ITEM 6. EXHIBITS AND REPORTS ON FORM 8-K

    (a)     Exhibits required by Item 601 of Regulation S-K

            EXHIBIT NUMBER                             DESCRIPTION

                 10.71                             Amended and Restated
                                                   Common Stock Purchase
                                                   Agreement, dated as of
                                                   August 7, 2000, between
                                                   the Registrant and Acqua
                                                   Wellington North American
                                                   Equities Fund, Ltd.  (1)

                 10.72                             Third Amendment to Lease,
                                                   dated February 16, 2001,
                                                   between the Registrant
                                                   and Jack R. Wheatley dba
                                                   Matadero Creek.

    (b)     Reports on Form 8-K

            The Registrant filed a current report on Form 8-K with the
            Commission on February 21, 2001, with respect to the amendment of
            the stock purchase agreement between the Registrant and Acqua
            Wellington.
___________________

(1) Incorporated by reference to Exhibit 4.6 to the Registration Statement
Number 333-59318 filed by the Registrant on April 20, 2001.

<PAGE>

                                  SIGNATURES

    Pursuant to the requirements of Section 13 or 15(d) of the Securities
Exchange Act of 1934, the registrant has duly caused this report to be
signed on its behalf, by the undersigned, thereunto duly authorized.

                                              CV THERAPEUTICS, INC.

Date: May 14, 2001                   By: /s/ LOUIS G. LANGE, M.D., PH.D.
                                             Louis G. Lange, M.D., Ph.D.
                                Chairman of the Board & Chief Executive Officer
                                            (Principal Executive Officer)


Date: May 14, 2001                   By: /s/ DANIEL K. SPIEGELMAN
                                             Daniel K. Spiegelman
                                            Chief Financial Officer
                                 (Principal Financial and Accounting Officer)