Adagrasib (KRAS G12C)

Overview

Adagrasib is an orally available small molecule inhibitor of KRAS G12C with broad development in both monotherapy and combination therapies. Discovered by Mirati Therapeutics, Adagrasib has been investigated in the Phase 1/2 Krystal-1 study in patients with KRAS G12C-mutant Non-Small Cell Lung Cancer (NSCLC), Colorectal Cancer (CRC) and other solid tumors. In December 2022, the FDA granted accelerated approval for KRAZATI™ (adagrasib), a targeted treatment option for adult patients with KRAS G12C-mutated locally advanced or metastatic NSCLC, as determined by an FDA-approved test, who have received at least one prior systemic therapy.

Zai Lab obtained exclusive rights to develop and commercialize Adagrasib in Greater China from Mirati Therapeutics on June 1, 2021.

Mechanism of Action

Adagrasib elicits antitumor activity through selective and high affinity for, covalent binding to, and inhibition of the KRAS G12C mutant variant. KRAS G12C is an oncogenic mutation prevalent in lung, colorectal and other cancers and is implicated in tumor pathogenesis.