APG-2449 — Investigational Agent
Other · Phase 1 · Ascentage Pharma
Mechanism of Action
APG-2449 is an oral third-generation multi-kinase inhibitor targeting ALK, ROS1, and focal adhesion kinase (FAK). It inhibits ALK and ROS1 fusion oncoproteins including several resistance mutations (such as ALK G1202R) that limit earlier-generation ALK TKIs, and is CNS-penetrant to address brain metastases. Concurrent FAK inhibition may counteract adaptive survival and stromal/microenvironment-mediated resistance and could enhance activity in tumors with FAK-dependent signaling. This combined profile aims to overcome acquired resistance to crizotinib and next-generation ALK inhibitors.
Investigational Indications
- ALK-rearranged NSCLC (TKI-naive and TKI-resistant)
- ROS1-rearranged NSCLC
- FAK-dependent advanced solid tumors