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.