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IND Application Filed for Anticancer Agent XL647

SOUTH SAN FRANCISCO, Calif., February 19 /PRNewswire-FirstCall/ -- Exelixis, Inc. has submitted an investigational new drug (IND) application for XL647, a proprietary novel anticancer compound. XL647 demonstrates potent inhibition in vitro against multiple receptor tyrosine kinases (RTKs) that are implicated in tumor proliferation and vascularization (angiogenesis). Pending clearance by the U.S. Food & Drug Administration (FDA), the company intends to initiate a Phase 1 clinical trial in the second quarter of 2004.

XL647 is the first of several Spectrum Selective Kinase Inhibitors™ (SSKI) that Exelixis intends to advance into clinical development. Each SSKI has a different RTK inhibition spectrum, and each has the potential to achieve efficacy through simultaneous inhibition of multiple RTKs. XL647 simultaneously inhibits the EGFR, HER2, VEGFR and EphB4 RTKs with high potency and demonstrates excellent activity in target-specific cellular functional assays. XL647 has good oral bioavailability in preclinical models and shows sustained inhibition of target RTKs in vivo following a single oral dose. In preclinical models of major tumor types, including human breast, lung, colon and prostate cancer, XL647 demonstrates potent inhibition of tumor growth and has been shown to cause tumor regression. Consistent with its spectrum of activity, analysis of tumors from XL647-treated animals shows significant decreases in both tumor vascularity and tumor cell proliferation and an increase in tumor cell death.

"We believe that Exelixis is generating a therapeutically and commercially valuable anticancer pipeline," said George A. Scangos, Ph.D., president and chief executive officer. "XL647 is the first of what we believe is a very exciting portfolio of novel and highly potent anticancer compounds advancing toward clinical development whose activity is a direct result of selectively inhibiting a spectrum of target RTK proteins, not just a single target. We are equally enthusiastic about XL999, XL844 and other preclinical compounds in our growing pipeline, and we anticipate filing additional IND applications and initiating multiple clinical development programs during the course of this year and in 2005."

The Phase 1 clinical trial of XL647 will be an open-label, single and repeat dose escalation study conducted in subjects with solid tumors for whom there is no approved therapy. The study is designed to measure the safety, tolerability, pharmacokinetics and biological activity of XL647 following oral administration. The study will be conducted at two major medical centers in the U.S.

Source: Exelixis, Inc.

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