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Clinical and comparative utility of afatinib in non-small cell lung cancer

Authors D'Arcangelo M, Hirsch F

Received 31 December 2013

Accepted for publication 27 February 2014

Published 23 April 2014 Volume 2014:8 Pages 183—192


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Manolo D'Arcangelo, Fred R Hirsch

University of Colorado Denver, Department of Medical Oncology, Aurora, CO, USA

Abstract: The first targeted agents approved for non-small cell lung cancer (NSCLC) treatment, the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) gefitinib and erlotinib, have an impressive activity in the presence of activating mutations of the EGFR gene. However, all patients develop acquired resistance principally through secondary mutations (T790M), HER2 amplification, MET amplification, and other molecular aberrations. An attempt to overcome EGFR TKI resistance has been through the development of irreversible blockers. Afatinib is an irreversible inhibitor of the tyrosine kinase activity of all members of the HER family. The pharmacologic properties of afatinib (formation of covalent bonds, inhibition of other family members, and in vitro and in vivo activity on T790M mutation positive tumors) made this drug particularly appealing to study in clinic. Therefore, an intense program of clinical research (LUX-Lung program) was started and clinical results have shown very encouraging activity profiles in patients harboring EGFR activating mutations and in those with acquired resistance to reversible TKIs.

Keywords: NSCLC, EGFR, tyrosine kinase inhibitor, afatinib

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