Exelixis (EXEL) is a development-stage biotechnology company dedicated to the discovery and development of novel small molecule therapeutics for the treatment of cancer and other serious diseases.

It is leveraging its fully integrated drug discovery platform to fuel the growth of its development pipeline, which is primarily focused on cancer.

Currently, Exelixis' broad product pipeline includes investigational compounds in Phase 2 and Phase 1 clinical development for cancer and renal disease.

Alliances: GlaxoSmithKline, Bristol-Myers Squibb Company, Genentech, Wyeth Pharmaceuticals and Sankyo.

For more information, please visit the company's web site at http://www.exelixis.com.

NEWS

5/24/07

Treatment For cancers and polycythemia vera

    The excitement about the emergence of biotechnology is about the hope they offer through new capabilities in bringing far-reaching treatments. Excelixis, in our view, is one of the biotech firms that can realize the dream of many debilitated patients and frustrated physicians. Integrating its productivity of its discovery strength as a genomics firm with drug development enabled it to have 14 compounds in its pipeline and to file four investigational new drug applications (IND) this year alone.

    In the news, Exelixis submitted an investigational new drug (IND) application to the FDA for a new compound it called XL019. In preclinical studies, the compound has demonstrated to be a potent, selective and orally available small molecule inhibitor of the cytoplasmic tyrosine kinase JAK2. This mode of action  makes the drug a candidate for the treatment of myeloproliferative disorders such as myelofibrosis, polycythemia vera and essential thrombocythemia, in addition to lymphomas and solid tumors.  (Activating mutations in JAK2 are frequently observed in patients with these diseses.)  

XL019 is a selective inhibitor of the cytoplasmic tyrosine kinase JAK2. JAK2 is activated by cytokine and growth factor receptors and phosphorylates members of the STAT family of inducible transcription factors. Activation of the JAK/STAT pathway promotes cell growth and survival, and is a common feature of human tumors. JAK2 is activated by mutation in the majority of patients with polycythemia vera, essential thrombocythemia and myelofibrosis and appears to drive the inappropriate expansion of blood cells observed in these conditions. JAK2 also plays a role in immune cell function and inhibitors may therefore have utility in a broad spectrum of inflammatory diseases. XL019 is a potent and selective JAK2 inhibitor with favorable pharmacodynamic properties and preclinical safety profile. 

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