<PAGE>

AS FILED WITH THE SECURITIES AND EXCHANGE COMMISSION ON SEPTEMBER 22, 2000
                                                 REGISTRATION NO. 333-[______]
==============================================================================

                       SECURITIES AND EXCHANGE COMMISSION
                             WASHINGTON, D.C. 20549

                                    FORM S-3

                             REGISTRATION STATEMENT
                                      UNDER
                           THE SECURITIES ACT OF 1933

                              CV THERAPEUTICS, INC.
             (EXACT NAME OF REGISTRANT AS SPECIFIED IN ITS CHARTER)

            DELAWARE                                         45-1570294
  (STATE OR OTHER JURISDICTION                            (I.R.S. EMPLOYER
OF INCORPORATION OR ORGANIZATION)                       IDENTIFICATION NUMBER)

                                3172 PORTER DRIVE
                           PALO ALTO, CALIFORNIA 94304
                                 (650) 812-0585
        (ADDRESS, INCLUDING ZIP CODE, AND TELEPHONE NUMBER, INCLUDING
           AREA CODE, OF REGISTRANT'S PRINCIPAL EXECUTIVE OFFICES)

                           LOUIS G. LANGE, M.D., PH.D.
                             CHIEF EXECUTIVE OFFICER
                              CV THERAPEUTICS, INC.
                                3172 PORTER DRIVE
                           PALO ALTO, CALIFORNIA 94304
                                  (650) 812-0585
      (NAME, ADDRESS, INCLUDING ZIP CODE, AND TELEPHONE NUMBER, INCLUDING
                         AREA CODE, OF AGENT FOR SERVICE)

                                   COPIES TO:
                             ALAN C. MENDELSON, ESQ.
                                LATHAM & WATKINS
                             135 COMMONWEALTH DRIVE
                          MENLO PARK, CALIFORNIA 94025
                                (650) 463-4693

        APPROXIMATE DATE OF COMMENCEMENT OF PROPOSED SALE TO THE PUBLIC:
As soon as practicable after the effective date of this Registration Statement.

     If the only securities being registered on this Form are being offered
pursuant to dividend or interest reinvestment plans, please check the following
box. / /

     If any of the securities being registered on this Form are to be offered on
a delayed or continuous basis pursuant to Rule 415 under the Securities Act of
1933, other than securities offered only in connection with dividend or interest
reinvestment plans, check the following box. /X/

     If this Form is filed to register additional securities for an offering
pursuant to Rule 462(b) under the Securities Act, please check the following box
and list the Securities Act registration statement number of the earlier
effective registration statement for the same offering. / /

     If this Form is a post-effective amendment filed pursuant to Rule 462(c)
under the Securities Act, check the following box and list the Securities Act
registration statement number of the earlier effective registration statement
for the same offering. / /

     If delivery of the prospectus is expected to be made pursuant to Rule 434,
please check the following box. / /

                         CALCULATION OF REGISTRATION FEE
<TABLE>
<CAPTION>
---------------------------------------------------------------------------------
  TITLE OF SECURITIES   |       PROPOSED MAXIMUM        |      AMOUNT OF
   TO BE REGISTERED     |   AGGREGATE OFFERING PRICE    |  REGISTRATION FEE (1)
---------------------------------------------------------------------------------
<S>                     <C>                             <C>
Common Stock            |         $9,000,000            |       $2,376
------------------------------------------ --------------------------------------
</TABLE>

(1) Estimated solely for the purpose of computing the amount of the registration
    fee in accordance with Rule 457(o) under the Securities Act of 1933.

    THE REGISTRANT HEREBY AMENDS THIS REGISTRATION STATEMENT ON SUCH DATE OR
DATES AS MAY BE NECESSARY TO DELAY ITS EFFECTIVE DATE UNTIL THE REGISTRANT
SHALL FILE A FURTHER AMENDMENT THAT SPECIFICALLY STATES THAT THIS
REGISTRATION STATEMENT SHALL THEREAFTER BECOME EFFECTIVE IN ACCORDANCE WITH
SECTION 8(a) OF THE SECURITIES ACT OF 1933 OR UNTIL THE REGISTRATION
STATEMENT SHALL BECOME EFFECTIVE ON SUCH DATE AS THE COMMISSION, ACTING
PURSUANT TO SAID SECTION 8(a), MAY DETERMINE.
==============================================================================

<PAGE>


                                   PROSPECTUS

                              CV THERAPEUTICS, INC.

                  $9,000,000 AGGREGATE AMOUNT OF COMMON STOCK

                               ------------------

         This prospectus will allow us to issue common stock to Biotech
Manufacturing Ltd. ("BML") as repayment of the $9,000,000 of principal that
we owe BML under our Loan Agreement with BML dated March 7, 1997.

         CV Therapeutics' common stock is traded on the Nasdaq National
Market under the symbol "CVTX." On September 21, 2000, the last reported sale
price for our common stock on the Nasdaq National Market was $71.4375 per share.

         INVESTING IN OUR COMMON STOCK INVOLVES CERTAIN RISKS. SEE "RISK
FACTORS" BEGINNING ON PAGE 5.

         NEITHER THE SECURITIES AND EXCHANGE COMMISSION NOR ANY STATE SECURITIES
COMMISSION HAS APPROVED OR DISAPPROVED OF THE SECURITIES OR PASSED UPON THE
ACCURACY OR ADEQUACY OF THIS PROSPECTUS. ANY REPRESENTATION TO THE CONTRARY IS A
CRIMINAL OFFENSE.

                 The date of this prospectus is September 22, 2000.

<PAGE>

                                TABLE OF CONTENTS
<TABLE>
<CAPTION>
                                                                         PAGE
                                                                         ----
<S>                                                                      <C>
Prospectus Summary.........................................................3

The Company................................................................3

The Offering...............................................................4

Risk Factors...............................................................5

Forward-Looking Statements................................................16

Where You Can Find More Information.......................................17

Use of Proceeds...........................................................18

Dilution..................................................................19

Plan of Distribution......................................................20

Legal Matters.............................................................21

Experts...................................................................21

Material Changes..........................................................21

</TABLE>

                                       2
<PAGE>

                               PROSPECTUS SUMMARY

         The following summary is qualified in its entirety by reference to the
more detailed information and consolidated financial statements appearing
elsewhere or incorporated by reference in this prospectus.

                                   THE COMPANY

         CV Therapeutics was incorporated in Delaware in December 1990, and in
June 1992 we changed our name to CV Therapeutics, Inc. Our executive offices are
located at 3172 Porter Drive, Palo Alto, California 94304, and our telephone
number is (650) 812-0585.

         CV Therapeutics, Inc. and the CV Therapeutics logo are our service
marks.  All other service marks and all brand names or trademarks appearing
in this prospectus are the property of their respective holders.


                                      3

<PAGE>

                                  THE OFFERING
<TABLE>
<CAPTION>
<S>                                              <C>
Common stock offered in this
prospectus..................................     ________ shares

Common stock outstanding after
the offering................................     ________ shares (l)

Use of proceeds.............................     See "Use of Proceeds."

Nasdaq National Market symbol...............     CVTX

</TABLE>
------------------
(1)   Based on shares outstanding as of [________]. Does not include [_______]
      shares of common stock issuable upon exercise of outstanding options or
      [_______] shares of common stock issuable upon exercise of outstanding
      warrants as of [_______].



                                      4
<PAGE>


                                  RISK FACTORS

          AN INVESTMENT IN THE SECURITIES OFFERED BY THIS PROSPECTUS IS VERY
RISKY. YOU SHOULD CAREFULLY CONSIDER THE FOLLOWING RISK FACTORS IN ADDITION TO
THE INFORMATION IN THE REMAINDER OF THIS PROSPECTUS BEFORE DECIDING TO PURCHASE
THE STOCK.

          THESE RISKS AND UNCERTAINTIES ARE NOT THE ONLY ONES WE FACE. OTHERS
THAT WE DO NOT KNOW ABOUT NOW, OR THAT WE DO NOT NOW THINK ARE IMPORTANT, MAY
IMPAIR OUR BUSINESS OR THE TRADING PRICE OF OUR SECURITIES.

RISKS RELATED TO OUR BUSINESS

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.

         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 cardiac
imaging, cell cycle inhibition, cardiac conduction, cardiac metabolism and
Tangier disease drug discovery 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.


                                      5
<PAGE>

         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, clinical trials and 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 two products in clinical development:
ranolazine and CVT-510. 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.
We cannot assure you that enrollment for the second Phase III trial for
ranolazine, called Combination Assessment of Ranolazine In Stable Angina or
CARISA, will not also be delayed.

         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 trial and than we are using
in the CARISA trial. 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.

         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


                                      6
<PAGE>

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 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. 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. In particular, we or our third
party manufacturers will be required to adhere to 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


                                      7
<PAGE>

manufacturing, testing and quality control activities. Furthermore, we or our
third party manufacturers must pass a preapproval inspection of manufacturing
facilities by the FDA before obtaining marketing approval. We will also be
subject to ongoing FDA requirements for submission of safety reports and
other postmarket information.

         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 Inc., a subsidiary of
Quintiles Transnational Corp., 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, marketing or distribution capability. As
a result, we depend on collaborations with third parties, such as Innovex,
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 its contractual obligations. Its 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 Adentri-TM- 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

                                      8
<PAGE>

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 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., a subsidiary of Roche, 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.


                                      9
<PAGE>

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 June 30,
2000, we had an accumulated deficit of $107.1 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 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:

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

              -    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


                                      10
<PAGE>

              -    competing technological and market developments

              -    the cost of manufacturing or obtaining preclinical and
                   clinical material.

         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

              -    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 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


                                      11
<PAGE>

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 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 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 we 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,


                                      12
<PAGE>

licensees or other third parties for the manufacturing of clinical and
commercial scale quantities of our products.

         For example, we have entered into an agreement with a third party
manufacturer for clinical scale production of an amount of ranolazine's
active pharmaceutical ingredient that we believe will be sufficient to
support the remainder of the Phase III clinical program. We cannot be certain
that we will be able to enter into an agreement for the commercial scale
manufacture of the active ingredient in ranolazine. If we are unable to do
so, our commercial launch of ranolazine may be delayed. We have entered into
an agreement with a third party manufacturer for clinical scale production of
ranolazine tablets sufficient to support the remainder of the Phase III
clinical program and are negotiating with them for registration and
commercialization supply of ranolazine tablets. If we are unable to negotiate
an agreement to supply ranolazine tablets for registration and
commercialization, commercial launch of ranolazine may be delayed. 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 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. 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


                                      13
<PAGE>

and may materially adversely affect our business, financial condition and
results of operations.

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 $10.375
and $82.75. 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


                                      14
<PAGE>

              -    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.

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, or "poison
pill," and authorized severance agreements in the event of a change of
control for key executives. The Board of Directors amended the stockholder
rights plan in July 2000 while maintaining it in effect.

                                      15
<PAGE>

                           FORWARD-LOOKING STATEMENTS

         This prospectus contains forward-looking statements. 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.

         These statements reflect only management's current expectations. In
evaluating these statements, you should specifically consider various factors,
including the risks outlined above. These factors may cause our actual results
to differ materially from any 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.
You are advised, however, to consult any additional disclosures we make in our
Form 10-Q, 8-K and 10-K reports to the SEC. Also note that we provide a
cautionary discussion of risks and uncertainties under "Risk Factors" on page 5
of this prospectus. These are factors that we think could cause our actual
results to differ materially from expected results.


                                      16
<PAGE>

                       WHERE YOU CAN FIND MORE INFORMATION

         We file annual, quarterly and special reports, proxy statements and
other information with the SEC. You may read and copy any document we file at
the SEC's public reference room at 450 Fifth Street, N.W., Washington, D.C.,
20549. You can request copies of these documents by contacting the SEC and
paying a fee for the copying cost. Please call the SEC at 1-800-SEC-0330 for
further information on the public reference rooms. Our SEC filings are also
available to the public from the SEC's website at www.sec.gov.

         This prospectus is part of a registration statement on Form S-3,
including amendments, relating to the common stock offered by this prospectus
with the SEC. This prospectus does not contain all of the information set forth
in the registration statement, the exhibits and schedules, some portions of
which the SEC allows us to omit. Statements contained in this prospectus as to
the contents of any contract or other document referred to are not necessarily
complete and in each instance reference is made to the copy of that contract or
other document filed as an exhibit to the registration statement. For further
information about us and the common stock offered by this prospectus we refer
you to the registration statement and its exhibits and schedules which may be
obtained as described above.

         The SEC allows us to "incorporate by reference" the information
contained in documents that we file with them, which means that we can disclose
important information to you by referring you to those documents. The
information incorporated by reference is considered to be part of this
prospectus. Information in this prospectus supersedes information incorporated
by reference that we filed with the SEC before the date of this prospectus,
while information that we file later with the SEC will automatically update and
supersede prior information. We incorporate by reference the documents listed
below and any future filings we will make with the SEC under Sections 13(a),
13(c), 14 or 15(d) of the Securities Exchange Act of 1934, as amended, prior to
the termination of the offering:

         1.   our Annual Report on Form 10-K for the fiscal year ended
              December 31, 1999;

         2.   our Quarterly Reports on Form 10-Q for the fiscal quarters ended
              March 31, 2000 and June 30, 2000;

         3.   our Current Reports on Form 8-K, dated March 1, 2000 and
              August 16, 2000; and

         4.   the description of our common stock contained in our registration
              statement on Form 8-A filed on October 30, 1996.

         You may request copies of these filings, at no cost, by writing or
telephoning us at:

                             CV Therapeutics, Inc.
                         Attention: Investor Relations
                               3172 Porter Drive
                          Palo Alto, California 94304
                            Telephone (650) 812-0585



                                      17
<PAGE>

                                 USE OF PROCEEDS

         We intend to transfer the securities issued under this offering to
Biotech Manufacturing Ltd. ("BML") as repayment of the $9,000,000 of
principal that we owe BML under our Loan Agreement with BML dated March 7,
1997 (the "Loan Agreement").

         The Loan Agreement permits us to repay the $9,000,000 of principal
we currently owe BML with common stock that has been registered for resale.
We believe that it is in the best interest of our company and our shareholders
to repay BML the $9,000,000 of outstanding principal with common stock.

         We borrowed $4,500,000 of the $9,000,000 that we owe BML on August
31, 2000. We intend to use the $4,500,000 that was borrowed on August 31,
2000 to fund research, development and product manufacturing, to provide
working capital and for general corporate purposes.


                                      18
<PAGE>


                                   DILUTION

        The net tangible book value of CV Therapeutics at June 30, 2000 was
$69,324,000 or approximately $3.76 per share of common stock. Net tangible
book value per share represents the amount of our tangible assets less total
liabilities, divided by 18,448,889 shares of common stock.

        Net tangible book value dilution per share represents the difference
between the amount per share paid by purchasers of shares of common stock in
the offering made hereby and the pro forma net tangible book value per share
of common stock immediately after completion of the offering. After giving
effect to the sale of [______] shares of common stock in this offering at an
assumed offering price of $[______] per share and the application of the
estimated net proceeds therefrom (after deducting estimated offering
expenses) the pro forma net tangible book value of CV Therapeutics as of
[_____] would have been $[______] or $[______] per share, an immediate
increase in net tangible book value of $[______] per share to existing
stockholders and an immediate dilution in net tangible book value of $[______]
per share to purchasers of common stock in the offering, as illustrated in
the following table:

<TABLE>
<S>                                                                                    <C>
Assumed public offering price per share................................................$[_______]
Net tangible book value per share at [_________].......................................$[_______]
Increase per share attributable to new investors.......................................$[_______]
Pro forma net tangible book value per share after offering.............................$[_______]
Net tangible book value dilution per share to new investors............................$[_______]
</TABLE>

        To the extent that outstanding options and warrants are exercised,
there will be further dilution to new investors.


                                        19

<PAGE>


                             PLAN OF DISTRIBUTION

         We intend to transfer the common stock of this offering to Biotech
Manufacturing Ltd.

         We will bear the expenses incident to the registration of the shares.
These expenses are estimated to be $24,876.



                                      20
<PAGE>

                                  LEGAL MATTERS

         The validity of the issuance of the common stock offered in this
prospectus will be passed upon for CV Therapeutics by Latham & Watkins, Menlo
Park, California. Alan C. Mendelson, our Secretary and a partner of Latham &
Watkins, owns 1008 shares of our common stock.

                                     EXPERTS

         Ernst & Young LLP, independent auditors, have audited our
consolidated financial statements included in our Annual Report on Form 10-K
for the year ended December 31, 1999, as set forth in their report, which is
incorporated by reference in this prospectus and elsewhere in the
registration statement. Our consolidated financial statements are
incorporated by reference in reliance on Ernst & Young LLP's report, given
upon their authority as experts in accounting and auditing.

                                MATERIAL CHANGES

         On July 11, 2000, we entered into a Collaboration and License
Agreement with Fujisawa Healthcare, Inc. to collaborate in the development
and marketing of second generation pharmacologic cardiac stress agents. Under
this agreement, Fujisawa receives exclusive North American rights to
CVT-3146, a short acting selective A2A adenosine receptor agonist, and a
backup compound. We will retain the responsibility for managing the CVT-3146
development program. Fujisawa will be responsible for selling and marketing
CVT-3146 in North America. Under the agreement, we have received $10 million
from Fujisawa, in part for the purchase of our common stock, and may receive
up to an additional $24 million based on our reaching development and
regulatory milestones. Fujisawa will reimburse us for 75% of the development
costs and, if approved by the FDA, we will receive a royalty based on product
sales of CVT-3146 and we may receive a royalty on other products.

                                      21
<PAGE>

                                     PART II

                     INFORMATION NOT REQUIRED IN PROSPECTUS

ITEM 14.  OTHER EXPENSES OF ISSUANCE AND DISTRIBUTION

         The following table sets forth all expenses payable by CV Therapeutics
in connection with the sale of the $9,000,000 aggregate amount of common stock
being registered. All the amounts shown are estimates except for the
registration fee.

<TABLE>
<CAPTION>
<S>                                                        <C>
         SEC registration fee............................. $  2,376.00
         Legal fees and expenses.......................... $ 10,000.00
         Accounting fees and expenses..................... $  7,500.00
         Miscellaneous.................................... $  5,000.00
                 Total.................................... $ 24,876.00
</TABLE>

ITEM 15.  INDEMNIFICATION OF OFFICERS AND DIRECTORS

         The Registrant's Restated Certificate of Incorporation provides that
directors of the Registrant shall not be personally liable to the Registrant or
its stockholders for monetary damages for breach of fiduciary duty as a
director, to the fullest extent permitted by the General Corporation Law of the
State of Delaware. The Registrant's Restated Bylaws provide for indemnification
of officers and directors to the full extent and in the manner permitted by
Delaware law. Section 145 of the Delaware General Corporation Law makes
provision for such indemnification in terms sufficiently broad to cover officers
and directors under certain circumstances for liabilities arising under the
Securities Act of 1933, as amended (the "Securities Act").

         The Registrant has entered into indemnification agreements with
substantially all of its officers and directors which provide indemnification
under certain circumstances for acts and omissions which may not be covered by
any directors' and officers' liability insurance.

ITEM 16.  EXHIBITS

<TABLE>
<CAPTION>
       EXHIBIT
       NUMBER                    DESCRIPTION OF DOCUMENT
       -------                   -----------------------
<S>             <C>
         4.1    Amended and Restated Certificate of Incorporation. (l)
         4.2    Restated By-laws. (l)
         5.1    Opinion of Latham & Watkins.
         23.1   Consent of Ernst & Young LLP, Independent Auditors.
         23.2   Consent of Latham & Watkins.  Reference is made to Exhibit 5.1.
         24.1   Power of Attorney.  Reference is made to page II-3.
</TABLE>
-------------
(1)    Filed as an exhibit to the Registration Statement on Form S-1 (No.
       333-12675) or amendments thereto and incorporated herein by reference.


                                      II-1
<PAGE>

ITEM 17.  UNDERTAKINGS

         Insofar as indemnification for liabilities arising under the
Securities Act may be permitted to directors, officers, and controlling
persons of the Registrant pursuant to the provisions described in Item 15 or
otherwise, the Registrant has been advised that in the opinion of the
Securities and Exchange Commission, such indemnification is against public
policy as expressed in the Securities Act and is, therefore, unenforceable.
In the event that a claim for indemnification against such liabilities (other
than the payment by the Registrant of expenses incurred or paid by a
director, officer, or controlling person of the Registrant in the successful
defense of any action suit, or proceeding) is asserted by such director,
officer, or controlling person in connection with the securities being
registered, the Registrant will, unless in the opinion of its counsel the
matter has been settled by controlling precedent, submit to a court of
appropriate jurisdiction the question whether such indemnification by it is
against public policy as expressed in the Securities Act and will be governed
by the final adjudication of such issue.

         The undersigned Registrant hereby undertakes:

         (1)     To file, during any period in which offers or sales are being
made pursuant to this registration statement, a post-effective amendment to this
registration statement to include any material information with respect to the
plan of distribution not previously disclosed in the registration statement or
any material change to such information in the registration statement;

         (2)     That, for the purpose of determining any liability under the
Securities Act, each such post-effective amendment shall be deemed to be
a new registration statement relating to the securities offered therein, and the
offering of such securities at that time shall be deemed to be the initial bona
fide offering thereof; and

         (3)     To remove from registration by means of a post-effective
amendment any of the securities being registered which remain unsold at the
termination of the offering.

         The undersigned Registrant hereby undertakes that, for the purposes of
determining any liability under the Securities Act, each filing of the
Registrant's annual report pursuant to Section 13(a) or Section 15(d) of the
Securities Exchange Act of 1934 that is incorporated by reference in the
registration statement shall be deemed to be a new registration statement
relating to the securities offered therein, and the offering of such securities
at that time shall be deemed to be the initial bona fide offering thereof.

         The undersigned Registrant undertakes that: (1) for purpose of
determining any liability under the Securities Act, the information
omitted from the form of prospectus filed as part of the registration statement
in reliance upon Rule 430A and contained in the form of prospectus filed by the
Registrant pursuant to Rule 424(b) (1) or (4) or 497(h) under the Securities Act
shall be deemed to be part of the registration statement as of the time it was
declared effective; and (2) for the purpose of determining any liability under
the Securities Act, each post-effective amendment that contains a form
of prospectus shall be deemed to be a new registration statement relating to the
securities offered therein, and the offering of such securities at that time
shall be deemed to be the initial bona fide offering thereof.


                                      II-2
<PAGE>

                                   SIGNATURES

         Pursuant to the requirements of the Securities Act, the registrant
certifies that it has reasonable grounds to believe that it meets all of the
requirements for filing on Form S-3 and has duly caused this Registration
Statement to be signed on its behalf by the undersigned thereunto duly
authorized, in the city of Palo Alto, County of Santa Clara, State of
California, on the 22nd day of September, 2000.

                                CV THERAPEUTICS, INC.

                                By:       /s/ DANIEL K. SPIEGELMAN
                                      --------------------------------
                                              Daniel K. Spiegelman
                                             SENIOR VICE PRESIDENT
                                          AND CHIEF FINANCIAL OFFICER
                                  (Principal financial and accounting officer)


                                POWER OF ATTORNEY

         KNOW ALL PERSONS BY THESE PRESENTS, that each person whose signature
appears below constitutes and appoints LOUIS G. LANGE and DANIEL K. SPIEGELMAN,
and each of them, as his or her true and lawful attorneys-in-fact and agents,
with full power of substitution and resubstitution, for the undersigned and in
his or her name, place and stead, in any and all capacities, to sign any or all
amendments (including post-effective amendments) to the Registration Statement
and to file the same, with all exhibits thereto, and all documents in connection
therewith, with the Securities and Exchange Commission, granting unto said
attorneys-in-fact and agents, and each of them, full power of authority to do
and perform each and every act and thing requisite and necessary to be done in
connection therewith, as fully to all intents and purposes as he or she might or
could do in person, hereby ratifying and confirming all that said
attorneys-in-fact and agents, each acting alone, or his or her substitute or
substitutes, may lawfully do or cause to be done by virtue hereof.

         Pursuant to the requirements of the Securities Act, this
Registration Statement has been signed below by the following persons in the
capacities indicated and on the dates indicated.

<TABLE>
<CAPTION>
             SIGNATURES                                TITLE                     DATE
             ----------                                -----                     ----
<S>                                       <C>                              <C>
             /s/ LOUIS G. LANGE              Chairman of the Board and     September 22, 2000
       ------------------------------         Chief Executive Officer
         Louis G. Lange, M.D., Ph.D.       (Principal executive officer)


          /s/ DANIEL K. SPIEGELMAN            Chief Financial Officer      September 22, 2000
       ------------------------------        (Principal financial and
            Daniel K. Spiegelman                accounting officer)


           /s/ THOMAS L. GUTSHALL                     Director             September 22, 2000
       ------------------------------
             Thomas L. Gutshall

</TABLE>

                                      II-3
<PAGE>
<TABLE>
<CAPTION>
<S>                                       <C>                              <C>

         /s/ COSTA G. SEVASTOPOULOS                   Director             September 22, 2000
       ------------------------------
       Costa G. Sevastopoulos, Ph.D.

           /s/ PETER BARTON HUTT                      Director             September 22, 2000
       ------------------------------
             Peter Barton Hutt

           /s/ BARBARA J. MCNIEL                      Director             September 22, 2000
       ------------------------------
       Barbara J. McNiel, M.D., Ph.D.

            /s/ J. LEIGHTON READ                      Director             September 22, 2000
       ------------------------------
           J. Leighton Read, M.D.

             /s/ R. SCOTT GREER                       Director             September 22, 2000
       ------------------------------
               R. Scott Greer
</TABLE>



                                      II-4
<PAGE>

                                  EXHIBIT INDEX
<TABLE>
<CAPTION>
EXHIBIT NO.                              DESCRIPTION
<S>           <C>
4.1           Amended and Restated Certificate of Incorporation.(1)
4.2           Restated By-laws. (1)
5.1           Opinion of Latham & Watkins.
23.1          Consent of Ernst & Young LLP, Independent Auditors.
23.2          Consent of Latham & Watkins.  Reference is made to Exhibit 5.1.
24.1          Power of Attorney.  Reference is made to page II-3.
</TABLE>
---------------

(1)    Filed as an exhibit to the Registration Statement on Form S-1
       (No. 333-12675) or amendments thereto and incorporated herein by
       reference.