Response and Resistance to RAS Inhibition in Cancer.

ABSTRACT: RAS inhibition has the potential to transform cancer treatment for many patients. The landscape of RAS inhibitor therapies is rapidly evolving, with two mutant-selective KRAS inhibitors now approved and multiple other mutant-selective, pan-KRAS, and pan-RAS inhibitors in development. However, monotherapy efficacy has been limited by primary and acquired resistance. In this article, we review preclinical and clinical data on RAS inhibition in cancer and describe multiple genetic and nongenetic mechanisms of resistance. Moreover, we highlight future opportunities for the design of rational combination therapy strategies, which will ultimately be needed to overcome resistance and enhance the efficacy of these promising treatments.

Significance

RAS inhibitors have shown early evidence o

SUBMITTER: Ebright RY 

PROVIDER: S-EPMC12226231 | biostudies-literature | 2025 Jul

REPOSITORIES: biostudies-literature