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Current Medicinal Chemistry

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ISSN (Print): 0929-8673
ISSN (Online): 1875-533X

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Perspective

First Approval of Adagrasib for the Treatment of Non-Small Cell Lung Cancer Harboring a KRASG12C Mutation

Author(s): Surya K. De*

Volume 31, Issue 3, 2024

Published on: 27 April, 2023

Page: [266 - 272] Pages: 7

DOI: 10.2174/0929867330666230330122000

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Abstract

Adagrasib is an orally bioavailable, highly selective, small-molecule, irreversible covalent inhibitor of KRASG12C. It was approved by the US FDA on December 12, 2022, for patients with tumors harboring the KRASG12C 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.

Keywords: Non-small cell lung cancer, KRAS mutation, guanosine triphosphate, guanosine diphosphate, adagrasib, sotorasib.

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