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-First Combination Study of a MET and EGFR Inhibitor-
SOUTH SAN FRANCISCO, Calif., Jan. 7 /PRNewswire-FirstCall/ -- Exelixis, Inc. (Nasdaq: EXEL) today announced that it has initiated a phase 1/2 trial of XL184 in patients with non-small cell lung cancer (NSCLC) who have had progressive disease while on a regimen containing erlotinib.
XL184 is a small molecule that simultaneously inhibits the MET, RET and VEGFR receptor tyrosine kinases. In the initial phase 1 part of the study, safety and pharmacokinetics of combining XL184 with erlotinib will be evaluated. The primary endpoint of the phase 2 part of the study is overall response rate. Secondary endpoints include progression-free survival, overall survival and pharmacodynamics.
"XL184 is a potent inhibitor of MET, and MET amplification has been shown to play an important role in the development of resistance to EGFR inhibitors in NSCLC," said Michael Morrissey, Ph.D., president of research and development of Exelixis. "Our preclinical data suggest that XL184 effectively inhibits growth of cancer cells that have become resistant to EGFR inhibitors through activation of the MET signaling pathway. XL184 also potently inhibits VEGFR, which is a validated target in the treatment of NSCLC. The compound has shown encouraging anti-tumor activity in an initial phase 1 trial and we are executing a phase 2 clinical development program, and are planning on initiation of a pivotal trial for XL184 in medullary thyroid cancer in 2008."
The phase 1/2 study of XL184 is expected to enroll up to 86 NSCLC
patients who have had disease progression while on erlotinib. The phase 1
portion of the study will evaluate dose escalation of XL184 in combination
with erlotinib, both
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| SOURCE Exelixis, Inc. Copyright©2008 PR Newswire. All rights reserved |