BPI-421286

BPI-421286 is a small molecule, orally bioavailable, potent and highly selective covalent irreversible inhibitor of the KRAS G12C mutant protein. It was developed as an antineoplastic agent targeting cancers harboring the KRAS G12C mutation. The drug was being developed by Betta Pharmaceuticals for the treatment of advanced solid tumors, particularly those with metastatic or late-stage disease. Its mechanism involves direct inhibition of the oncogenic KRAS G12C protein, thereby blocking downstream signaling pathways that drive tumor growth and survival[1][3][4]. Clinical development reached Phase 1 trials in China but has since been discontinued for solid tumors[1].