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

Manolo D'Arcangelo, Fred R HirschUniversity of Colorado Denver, Department of Medical Oncology, Aurora, CO, USAAbstract: The first targeted agents approved for non-small cell lung cancer (NSCLC) treatment, the epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) gefitin...

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Autores principales:	D'Arcangelo M, Hirsch FR
Formato:	article
Lenguaje:	EN
Publicado:	Dove Medical Press 2014
Materias:	Medicine (General) R5-920
Acceso en línea:	https://doaj.org/article/460cf2b06c744ca9bf19605f969c0e31
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spelling	oai:doaj.org-article:460cf2b06c744ca9bf19605f969c0e312021-12-02T05:49:19ZClinical and comparative utility of afatinib in non-small cell lung cancer1177-5475https://doaj.org/article/460cf2b06c744ca9bf19605f969c0e312014-04-01T00:00:00Zhttp://www.dovepress.com/clinical-and-comparative-utility-of-afatinib-in-non-small-cell-lung-ca-a16542https://doaj.org/toc/1177-5475 Manolo D'Arcangelo, Fred R HirschUniversity of Colorado Denver, Department of Medical Oncology, Aurora, CO, USAAbstract: 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, afatinibD'Arcangelo MHirsch FRDove Medical PressarticleMedicine (General)R5-920ENBiologics: Targets & Therapy, Vol 2014, Iss default, Pp 183-192 (2014)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine (General) R5-920
spellingShingle	Medicine (General) R5-920 D'Arcangelo M Hirsch FR Clinical and comparative utility of afatinib in non-small cell lung cancer
description	Manolo D'Arcangelo, Fred R HirschUniversity of Colorado Denver, Department of Medical Oncology, Aurora, CO, USAAbstract: 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
format	article
author	D'Arcangelo M Hirsch FR
author_facet	D'Arcangelo M Hirsch FR
author_sort	D'Arcangelo M
title	Clinical and comparative utility of afatinib in non-small cell lung cancer
title_short	Clinical and comparative utility of afatinib in non-small cell lung cancer
title_full	Clinical and comparative utility of afatinib in non-small cell lung cancer
title_fullStr	Clinical and comparative utility of afatinib in non-small cell lung cancer
title_full_unstemmed	Clinical and comparative utility of afatinib in non-small cell lung cancer
title_sort	clinical and comparative utility of afatinib in non-small cell lung cancer
publisher	Dove Medical Press
publishDate	2014
url	https://doaj.org/article/460cf2b06c744ca9bf19605f969c0e31
work_keys_str_mv	AT d39arcangelom clinicalandcomparativeutilityofafatinibinnonsmallcelllungcancer AT hirschfr clinicalandcomparativeutilityofafatinibinnonsmallcelllungcancer
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Clinical and comparative utility of afatinib in non-small cell lung cancer

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