Adagrasib (Krazati)

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Mechanism of action

From the NCI Drug Dictionary: An orally available, small molecule inhibitor that targets the oncogenic KRAS substitution mutation, G12C, with potential antineoplastic activity. Upon oral administration adagrasib covalently binds to cytosine 12 within the switch II pocket of GDP-bound KRAS G12C, thereby inhibiting mutant KRAS-dependent signaling.

Diseases for which it is used

History of changes in FDA indication

  • 2022-12-12: Granted accelerated approval for adult patients with KRAS G12C­-mutated locally advanced or metastatic non-small cell lung cancer (NSCLC), as determined by an FDA-approved test, who have received at least one prior systemic therapy. (Based on KRYSTAL-1)

Also known as

  • Code name: MRTX-849
  • Brand name: Krazati