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Exelixis Reports Top-Line Results of the Phase 2 Trial of XL784 in Patients With Proteinuria Associated With Diabetic Nephropathy
Date:10/16/2007

multi-site phase 2 trial of XL784 was designed to enroll approximately 130 diabetic patients who have clinically significant proteinuria. Participants were randomly assigned to receive 200mg of XL784 or placebo daily for three months. The primary endpoint of the trial was a significant reduction in proteinuria compared with placebo. Secondary endpoints included changes in renal function and cardiovascular events.

About XL784

XL784 was the first small molecule compound developed by Exelixis, using its proprietary drug discovery engine. The compound is a potent inhibitor of the ADAM-10 and MMP-2 metalloprotease enzymes, targets of significant interest because of their important role in renal fibrosis and impairment. XL784 was specifically optimized to be matrix metalloprotease-1 (MMP-1) sparing, thus potentially significantly enhancing its safety profile and enabling higher dosing compared with other previously studied metalloprotease inhibitors. Results of single and repeat dose phase 1 clinical trials of XL784 administered orally to 70 healthy volunteers demonstrated that XL784 has attractive safety and pharmacokinetic profiles.

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 GSK, Bristol-Myers Squibb, Genentech, Wyeth Pharmaceuticals and Daiichi-Sankyo. For more information, please visit the company's web site at

SOURCE Exelixis, Inc.
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