RAS mutations drive ∼20% of human cancers. This review summarizes clinical outcomes and resistance mechanisms of KRASG12C inhibitors and highlights emerging classes of next-generation (K)RAS inhibitors, focusing on their mechanisms of action, selectivity, early efficacy, and potential to overcome resistance in RAS-driven tumors.
RAS mutations drive ∼20% of human cancers. This review summarizes clinical outcomes and resistance mechanisms of KRASG12C inhibitors and highlights emerging classes of next-generation (K)RAS inhibitors, focusing on their mechanisms of action, selectivity, early efficacy, and potential to overcome resistance in RAS-driven tumors.