divarasib

Divarasib is an orally available, small molecule inhibitor that selectively targets the oncogenic KRAS G12C substitution mutation. By covalently binding to and inhibiting the KRAS G12C mutant protein, divarasib blocks mutant-dependent signaling pathways involved in tumor cell growth, proliferation, and survival. It has demonstrated high potency and selectivity in preclinical studies—being 5 to 20 times as potent and up to 50 times as selective as other KRAS G12C inhibitors such as sotorasib and adagrasib. Divarasib is being developed primarily for advanced or metastatic cancers harboring the KRAS G12C mutation, including non-small cell lung cancer (NSCLC) and colorectal cancer (CRC). The drug is currently under investigation in phase I/II clinical trials with promising early efficacy results[1][2][3][5][6][8].

Other names

divarasib [INN]