Sotorasib (AMG510) racemate s a potent, selective, covalent KRAS G12C inhibitor with p-ERK IC50 of 68 nM. AMG510 showed great promise in the treatment of KRAS p.G12C-mutant tumors both pre-clinically and clinically. Treatment with AMG 510 led to the regression of KRASG12C tumours and improved the anti-tumour efficacy of chemotherapy and targeted agents. In immune-competent mice, treatment with AMG 510 resulted in a pro-inflammatory tumour microenvironment and produced durable cures alone as well as in combination with immune-checkpoint inhibitors.
