First-in-Human Phase I Trial of Two Schedules of OSI-930 a Novel Multikinase Inhibitor Incorporating Translational Proof-of-Mechanism Studies

摘要

PurposeOSI-930 is a novel, potent, oral small-molecule receptor tyrosine kinase inhibitor, predominantly against VEGF receptors (VEGFR), c-Kit, and platelet-derived growth factor receptors. A phase I trial was undertaken to determine safety, maximum-tolerated dose (MTD), pharmacokinetics, pharmacodynamics, and antitumor activity of OSI-930 in patients with advanced solid tumors.