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Exelixis Presents Encouraging Phase 1 Data For XL019, A Novel Selective Inhibitor of JAK2
Date:12/10/2007

oietin and thrombopoietin. Mutational activation of JAK2 is observed in the majority of patients with polycythemia vera, essential thrombocythemia and myelofibrosis, and is thought to drive the inappropriate expansion of blood cells observed in these conditions. Other members of the JAK family play critical roles in regulating immune responses, including the anti-viral and anti-parasitic responses.

XL019 is a potent JAK2 inhibitor (IC50 = 2 nM) with excellent selectivity versus the other members of the JAK kinase family (JAK1 IC50 = 130 nM, JAK3 IC50 = 250 nM, TYK2 IC50 = 340 nM). It is active against both wild type and mutationally activated forms of JAK2, and in preclinical studies showed good oral bioavailability and pharmacodynamic properties. Preclinical safety studies showed that XL019 was well tolerated.

About Exelixis

Exelixis, Inc. 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. The company 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. Exelixis has established strategic corporate alliances with major pharmaceutical and biotechnology companies, including GlaxoSmithKline, Bristol-Myers Squibb Company, Genentech, Wyeth Pharmaceuticals and Daiichi-Sankyo. For more information, please visit the company's web site at http://www.exelixis.com.

Forward-Looking Statements

This press release contains forward-looking statements, including, without limitation, statements related to the future development and potential efficacy of XL019 and the timing of the initiation of pivotal trials for XL019. Words such
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SOURCE Exelixis, Inc.
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