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Plexxikon and Roche Enter Partnership to Develop Targeted Cancer Therapeutic Medicine PLX4032



    Plexxikon Inc. and Roche today announced they have entered into an
    agreement to develop and commercialize PLX4032, Plexxikon's
    investigational targeted cancer therapy which selectively inhibits
    B-Raf(V600E), a mutated form of the BRAF kinase gene. The BRAF(V600E)
    gene has been associated with increased tumor aggressiveness and
    decreased survival in many types of cancers and is a common
    cancer-causing kinase gene. The BRAF(V600E) gene is found in
    approximately 70% of malignant melanomas and a large number of
    colorectal and thyroid tumors. PLX4032 may offer a new treatment
    modality for the estimated 100,000 cancer patients in the United
    States who carry the BRAF(V600E) gene. Plexxikon recently filed an
    Investigational New Drug (IND) application for PLX4032 and plans to
    initiate a Phase 1 clinical trial by the end of this year.

    Separately, Roche Molecular Diagnostics, a business unit of Roche
    Diagnostics, and Plexxikon announced they will collaborate on
    development of an in vitro assay to screen for the presence of the
    BRAF(V600E) mutation in biological samples taken from patient tumors.
    An assay that correlates the presence of this mutation with clinical
    outcome may aid clinical development of PLX4032.

    "As one of the leading pharmaceutical companies in oncology,
    together with their commitment to personalized medicine, Roche makes
    an ideal partner for the development of this unique compound," said K.
    Peter Hirth, Ph.D., chief executive officer of Plexxikon Inc. "We
    believe PLX4032 could be a first-in-class oral cancer therapeutic
    which selectively targets an oncogenic protein found only in diseased
    tissue. Along with our Phase 2 diabetes product and preclinical stage
    portfolio in multiple therapeutic areas, PLX4032's entry into
    development further validates Plexxikon's discovery platform for novel
    drug candidates."

    "There is a growing body of evidence demonstrating that agents
    such as PLX4032, which selectively inhibit activated kinases, are
    increasingly useful in treating cancer and improving patient
    outcomes," said Peter Hug, Roche's Global Head of Pharma Partnering.
    "We are very excited to partner with Plexxikon for the development of
    PLX4032 and other B-Raf(V600E) targeted compounds. This could be a
    further example of the potential of personalized medicine. With our
    combined expertise in diagnostic and therapeutic development as well
    as commercialization, we are confident in our capability to develop
    this potential drug to make a difference to patients' lives."

    Plexxikon Roche Collaboration

    Under the terms of the agreement, Roche will pay Plexxikon $40
    million as an upfront payment and a further $6 million in guaranteed
    research funding over the next two years. In addition, Plexxikon could
    potentially receive up to approximately $660 million over the term of
    the collaboration based on the successful completion of a series of
    development and commercial milestones for multiple indications and/or
    multiple compounds, as well as royalties on potential product sales.

    Also under the collaboration, Roche and Plexxikon will jointly
    develop PLX4032 and follow on compounds targeting other BRAF kinase
    mutations. Plexxikon has filed an IND application for PLX4032, and
    will conduct a Phase 1 dose escalation study in patients with cancer,
    including melanomas. Roche will have a worldwide, exclusive license to
    develop and commercialize PLX4032, in addition to other anticancer
    compounds resulting from the partnership. Plexxikon retains the right
    to co-promote any product in the collaboration in the United States.

    About PLX4032

    PLX4032 is a selective inhibitor of the B-Raf(V600E) kinase found
    in approximately 70% of malignant melanomas, a large percentage of
    colorectal and thyroid cancers and many other tumor types. In
    preclinical studies in both melanoma and colorectal cancer models,
    PLX4032 reduces tumor size and slows the progression of the tumors
    even after the completion of treatment, without evidence of side
    effects. Highly selective against B-Raf(V600E) compared to a panel of
    over 70 other kinases, PLX4032 is designed to work specifically on
    cancer cells, leaving healthy cells untouched in contrast to
    chemotherapeutic agents.

    About Roche

    Headquartered in Basel, Switzerland, Roche is one of the world's
    leading research-focused healthcare groups in the fields of
    pharmaceuticals and diagnostics. As a supplier of innovative products
    and services for the early detection, prevention, diagnosis and
    treatment of disease, the Group contributes on a broad range of fronts
    to improving people's health and quality of life. Roche is a world
    leader in diagnostics, a leading supplier of medicines for cancer and
    transplantation and a market leader in virology. In 2005 sales by the
    Pharmaceuticals Division totaled 27.3 billion Swiss francs, and the
    Diagnostics Division posted sales of 8.2 billion Swiss francs. Roche
    employs roughly 70,000 people in 150 countries and has R&D agreements
    and strategic alliances with numerous partners, including majority
    ownership interests in Genentech and Chugai. Additional information
    about the Roche Group is available on the Internet (www.roche.com).

    Plexxikon Profile

    Plexxikon is a leader in the discovery and development of novel
    small molecule pharmaceuticals to treat human disease. Plexxikon's
    proprietary Scaffold-Based Drug Discovery(TM) platform is being
    applied to build therapeutic franchises in metabolic and
    cardiovascular disease, inflammation and oncology. This discovery
    process integrates a number of state-of-the-art technologies,
    including structural screening as one key component that provides a
    significant competitive advantage over other drug discovery
    approaches. To date, the company has discovered a portfolio of
    clinical and preclinical stage compounds in each of these franchises.

    Currently, the company's most advanced program is a PPAR
    pan-agonist for the treatment of diabetes and related cardiovascular
    complications, with the lead candidate now in Phase 2 clinical testing
    in collaboration with Wyeth Pharmaceuticals. Other discovery programs
    include a dual kinase inhibitor for the treatment of rheumatoid
    arthritis and other inflammatory diseases and a renin inhibitor for
    hypertension in collaboration with Servier. Plexxikon is seeking
    pharmaceutical and biotechnology partners for select collaboration
    opportunities. For more information, please visit www.plexxikon.com.

    Forward-Looking Statements

    This press release contains forward-looking statements. Such
    forward-looking statements, include, among others, those relating to
    the successful development, approval and launch of a product from
    PLX4032; the potential receipt by Plexxikon of substantial payments by
    successfully fulfilling certain development and commercial milestones
    for multiple indications and/or multiple compounds and successful
    launch of a product in the U.S. and other countries; that PLX4032 will
    be successfully developed and approved as a product which may be sold
    to the public; that Plexxikon will receive royalties from sales of
    this product, if successfully launched and that this product, if
    developed, could represent a significant step forward in treating
    patients. These statements are based on current expectations of future
    events. Forward-looking statements are not guarantees of performance.
    If underlying assumptions prove inaccurate or unknown risks or
    uncertainties materialize, actual results could vary materially from
    expectations and projections.

    These forward looking statements are subject to numerous risks and
    uncertainties. These risks and uncertainties include but are not
    limited to, general industry conditions and competition; obtaining
    U.S. and other countries regulatory approvals; health care changes in
    the U.S. and other countries; unexpected outcomes; product efficacy or
    safety concerns; product manufacturing issues; successful marketing of
    the product if developed; superior products being brought to market;
    loss of key employees; government reimbursement issues; economic
    conditions; technological advances and patents attained by
    competitors; manufacturing and supply disruptions; challenges inherent
    in new product development, including obtaining regulatory approvals;
    challenges to patents by competitors or allegations that the product
    infringes the patents of third parties; U.S. and other countries
    health care reforms; governmental laws and regulations; product
    liability claims or litigation risks; governmental investigations; and
    trends toward health care cost containment. These risks and
    uncertainties also include the risks that clinical trials may not
    proceed as planned due to technical, scientific, or patient enrollment
    issues, or disagreements with regulatory authorities over trial design
    or other matters; that the scale and scope of future clinical and
    nonclinical studies may change and will be determined in significant
    part by data collected in ongoing and future trials; that further
    clinical studies may not reflect the results obtained in early
    clinical and nonclinical studies; that ongoing nonclinical studies,
    including toxicology studies, will yield currently unanticipated
    negative outcomes that could adversely affect planned clinical trials;
    that results from the clinical trials will be insufficient to support
    additional phase programs without additional trials and consequent
    delay in the timetable for potential approval; and that any potential
    product may not achieve sales sufficient to earn the royalties
    referenced above. The foregoing list sets forth many, but not all, of
    the factors that could impact upon the ability to achieve results
    described in any forward-looking statements. It is not possible to
    predict or identify all such factors and should not consider this list
    to be a complete statement of all potential risks and uncertainties.
    Neither company assumes any obligation to update any forward-looking
    statements as a result of new information or future events or
    developments.