GFH276

GFH276 is a small molecule, orally bioavailable pan-RAS inhibitor developed by GenFleet Therapeutics. It demonstrates anti-proliferative activity in cell lines harboring various mutations in the RAS proto-oncogene family, including KRAS. Unlike covalent KRAS G12C inhibitors, the activity of GFH276 is not affected by upstream receptor tyrosine kinase activation that can confer resistance to other agents. Preclinical studies indicate that GFH276 has comparable inhibitory activity to RMC-6236 (a Phase III clinical-stage pan-RAS inhibitor), but with better bioavailability, lower efficacious dose requirements, and less distribution in normal tissues. These features suggest potential for improved tolerability and efficacy across a broad patient population with RAS-driven solid tumors[1][2][6].