KRAS mutant inhibitor BBO-11818

An orally bioavailable non-covalent inhibitor of both the active, guanosine triphosphate (GTP)-bound (ON) form and the inactive, guanosine diphosphate (GDP)-bound (OFF) form of multiple oncogenic KRAS substitution mutations, including KRAS G12D, G12V and G12X, with potential antineoplastic activity. Upon oral administration, KRAS mutant inhibitor BBO-11818 selectively targets and binds to KRAS, thereby inhibiting KRAS-dependent signaling. This inhibits the growth and survival of KRAS-overexpressing and mutated tumor cells. KRAS, a member of the RAS family of oncogenes, plays an important role in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive signal transduction leading to tumor cell growth, proliferation, invasion, and metastasis.