Verastem Inc. has announced the nomination of an oral KRAS G12D inhibitor, VS-7375 (GFH-375), as the lead program from its discovery and development collaboration with Genfleet Therapeutics (Shanghai) Inc.
KRAS is a GTP-binding protein involved in cell growth control that requires post-translational farnesylation to be active. KRAS G12D mutations are mostly associated with pancreatic, colorectal and non-small-cell lung cancers and occur less commonly in other cancers. There are currently no therapies approved to specifically target this mutation.
Pyrimidopyridine derivatives acting as GTPase KRAS G12D inhibitors have been reported in a Sunshine Lake Pharma Co. Ltd. patent as potentially useful for the treatment of cancer.
Mirati Therapeutics Inc. has received FDA clearance of its IND application for MRTX-1133, a potent, oral small-molecule inhibitor of the KRAS G12D driver mutation.
