BPI-9016M, a novel c-Met inhibitor, in pretreated advanced solid tumor: Results from a first-in-human, phase I, dose-escalation study.

e21108Background: BPI-9016M (Betta Pharmaceuticals Co, Ltd, Hangzhou, China) is a potent targeted therapy that inhibits MET and Axl. This first-in-human study is to assess the safety, tolerability, and PK of BPI-9016M in patients with advanced solid tumor malignancy, and to determine the MTD and RP2D for the phase Ib/II study. Methods: Eligible patients were enrolled into sequential dose-escalating cohorts from 100 mg to 1000 mg given orally once per day continually following the conventional 3+3 design. The primary endpoint was safety and tolerability. MTD was defined as the highest dose level resulting in u003c 1 of 3 DLTs. Blood levels of BPI-9016M were evaluated after single and multiple administration. This study was registered on ClinicalTrials.gov as NCT02478866. Results: Twenty patients were enrolled and treated in 6 of 7 predefined dose cohorts (100 mg n = 4, 200 mg n = 3, 300 mg n = 3, 450 mg n = 4, 600 mg n = 3, 800 mg n = 3), all had stage IV non-small cell lung cancer (NSCLC) progressed on previo...