The adverse event profile in phase 2 was consistent with phase 1: the most common adverse events were Grade 1 and 2 diarrhea, rash, fatigue, and nausea. Clinically asymptomatic QTc prolongation was also observed.
About the Phase 2 Trial of XL647 as First-Line Therapy
This open-label phase 2 trial is ongoing in previously untreated patients with stage IIIB or IV NSCLC who have adenocarcinoma histology and meet one of the following three criteria: Asian descent, female gender, or no or minimal smoking history. XL647 is administered orally at a dose of 350 mg on Days 1-5 of repeated 14-day cycles. The trial is designed to enrich for patients with activating mutations in the EGF receptor (EGFR) which have been associated with improved sensitivity to other EGFR inhibitors. Based on the selection criteria, Exelixis anticipates that approximately 30 percent of subjects in the trial will have activating EGFR mutations. This design should allow the accumulation of data for patients with and without EGFR mutations, helping to identify those patients most likely to benefit from treatment with XL647.
XL647 is a potent inhibitor of receptor tyrosine kinases (RTKs) that are implicated in driving tumor cell proliferation and tumor vascularization (blood vessel formation). XL647 inhibits EGFR, HER2 and VEGFR2. The compound has been optimized for high potency and oral bioavailability, demonstrates excellent activity in target-specific cellular functional assays, and has shown sustained inhibition of target RTKs in vivo in preclinical models following a single oral dose. Two phase 2 trials in patients with NSCLC are ongoing.
|SOURCE Exelixis, Inc.|
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