Covalent inhibitor targets KRas^G12C: A new paradigm for drugging the undruggable and challenges ahead.

ABSTRACT: KRAS is one of the most commonly mutated oncogenes in cancers and therapeutics directly targeting the KRas have been challenging. Among the different known mutants, KRas^G12C has been proved to be successfully targeted recently. Several covalent inhibitors selectively targeting KRas^G12C have shown promising efficacy against cancers harboring KRAS^G12C mutation in clinical trials and AMG510 (sotorasib) has been approved for the treatment of KRAS^G12C-mutated locally advanced or metastatic non-small cell lung cancer. However, the overall responsive rate of KRas^G12C inhibitors was around 50% in patients with non-small cell lung cancer and the efficacy in patients with colorectal cancer or appendiceal cancer

SUBMITTER: Li HY 

PROVIDER: S-EPMC10201555 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature