AN9025 is a pan-KRAS inhibitor in development to address a broad range of KRAS mutations across multiple tumor types. It is currently in lead optimization phase.

KRAS is the most frequently mutated oncogene and has attracted substantial attention. KRAS is a challenging therapeutic target, and efforts to directly inhibit its function have been continuing for decades. The most successful of these has been the development of covalent allele-specific inhibitors that trap KRAS G12C in its inactive conformation and suppress tumor growth in patients. Therefore, AN9025, has the potential to address an urgent unmet medical need in KRAS G12C -driven cancers.

In our in vitro studies, we demonstrated that AN9025 efficiently inhibited cancer types with KRAS mutations including pancreas adenocarcinoma, lung adenocarcinoma, and colorectal adenocarcinoma with sub-nanomolar IC50 values.

In addition, we also demonstrated that AN9025 showed deep, sustained and durable anti-tumor efficacy in KRAS-driven xenograft mice models.