APG-2449 in Patients With Advanced Solid Tumors

Summary

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.

Timeline

Start

2019-05-27

Primary completion

2027-12

Completion

2028-01

Publications

• Ma Y, Song Z, Chen J, Zhao Y, Fang W, Guo Y, Dong Y, Yang Y, Wu G, Fang J, Lin X, Li J, Huang Y, Zhao Y, Hong S, Xue J, Zhang Y, Liu Q, Yang C, Xu L, Yang Y, Xiong D, Yang D, Zhai Y, Zhang L, Zhao H. Safety, pharmacokinetic, pharmacodynamic, and efficacy properties of orally administered APG-2449 in patients with advanced ALK + and ROS1 + non-small-cell lung cancer: a multicentre, open-label, single-arm phase 1 trial. EClinicalMedicine. 2025 Oct 16;89:103556. doi: 10.1016/j.eclinm.2025.103556. eCollection 2025 Nov.
• Fang DD, Tao R, Wang G, Li Y, Zhang K, Xu C, Zhai G, Wang Q, Wang J, Tang C, Min P, Xiong D, Chen J, Wang S, Yang D, Zhai Y. Discovery of a novel ALK/ROS1/FAK inhibitor, APG-2449, in preclinical non-small cell lung cancer and ovarian cancer models. BMC Cancer. 2022 Jul 11;22(1):752. doi: 10.1186/s12885-022-09799-4.

Drugs

Indications