s First Approval of Adagrasib for the Treatment of Non-Small Cell Lung Cancer Harboring a KRAS^G12C Mutation

Adagrasib is an orally bioavailable, highly selective, small-molecule, irreversible covalent inhibitor of KRAS^G12C&. It was approved by the US FDA on December 12, 2022, for patients with tumors harboring the KRAS^G12C& mutation in locally advanced or metastatic non-small cell lung cancer (NSCLC). Herein, synthesis, dosage and administration, mechanism of action, pharmacokinetics, pharmacodynamics, and adverse events of adagrasib are described.