First Approval of Adagrasib for the Treatment of Non-Small CellLung Cancer Harboring a KRASG12C Mutation
Surya K. De
Abstract
Adagrasib is an orally bioavailable, highly selective, small-molecule, irreversible covalent inhibitor of KRAS</i><sup>G12C</sup>. It was approved by the US FDA on December 12, 2022, for patients with tumors harboring the KRAS</i><sup>G12C</sup> 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.
Topics & Concepts
KRASPharmacokineticsBioavailabilityPharmacodynamicsPharmacologyMedicineCancerLung cancerMutationCancer researchSmall moleculeMechanism of actionAdverse effectChemistryInternal medicineBiochemistryColorectal cancerIn vitroGeneLung Cancer Treatments and MutationsCancer-related Molecular PathwaysColorectal Cancer Treatments and Studies