APG-2449 is a novel, orally active, multi-targeted tyrosine kinase inhibitor, which inhibits
FAK, ALK, and ROS1 with nanomolar potencies. In preclinical studies, APG-2449 demonstrated
potent antiproliferative activity in various cancer cell lines as a single agent. In
combination treatment, APG-2449 enhanced anti-proliferative activities of several
chemotherapeutic and targeted agents. It is indicated that APG-2449 may have a broad
therapeutic potential for the treatment of human cancer as a single agent and in combination
with other classes of anticancer drugs. APG-2449 is intended for the treatment of patients
with advanced solid tumors. Upon completion of the Phase 1 dose escalation study to establish
the maximum tolerated dose (MTD), dose-limiting toxicities (DLTs), and/or recommended phase 2
dose (RP2D), several phase Ib/II studies will be implemented accordingly.