T. Doi, T. Yoshino, N. Fuse
May 20, 2012
Citations
0
Influential Citations
5
Citations
Quality indicators
Journal
Journal of Clinical Oncology
Abstract
3079 Background: Golvatinib is a highly potent, small molecule ATP-competitive inhibitor of the c-Met receptor tyrosine kinase and multiple members of the Eph receptor family as well as c-Kit and Ron, based on isolated kinase assays. Golvatinib showed antiproliferative activity in human cancer xenograft models, warranting further investigation in the clinical setting. Methods: Japanese patients (pts) with advanced solid tumors that had progressed after approved therapy received oral golvatinib at escalating doses of 50 to 100, 200 and 300 mg administered twice daily (BID) in conventional 3 pt cohorts. The primary objective was to determine the MTD of golvatinib when administered continually BID. The secondary objectives were to evaluate the safety, PK, PD biomarkers, and efficacy. Results: 16pts were enrolled (8 M, 8 F; med age 59 years; ECOG 0-1). Tumor types were colorectal (5), gastric (4) and others (7). One DLT (Gr 3 ALT increase) and 1 equivalent DLT (Gr 2 vomiting, nausea and anorexia) appeared in ...