AZD4625 is a Potent and Selective Inhibitor of KRAS(G12C)

AZD4625 is a potent, selective, and orally bioavailable inhibitor of oncogenic KRAS(G12C) as demonstrated in cellular assays and in vivo in preclinical cell line–derived and patient-derived xenograft models. In vitro and cellular assays have shown selective binding and inhibition of the KRAS(G12C) mutant isoform, which carries a glycine to cysteine mutation at residue 12, with no binding and inhibition of wild-type RAS or isoforms carrying non-KRAS(G12C) mutations. The pharmacology of AZD4625 shows that it has the potential to provide therapeutic benefit to patients with KRAS(G12C) mutant cancer as either a monotherapy treatment or in combination with other targeted drug agents.