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Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer

BACKGRUOND: Since their first description, activating epidermal growth factor receptor (EGFR) mutations identify a distinct clinical entity of patients with non-small-cell lung cancer (NSCLC). FINDINGS: New targeted therapies for molecularly selected NSCLC are changing the natural history of the dis...

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Detalles Bibliográficos
Autores principales: Stasi, Irene, Cappuzzo, Federico
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Springer Berlin Heidelberg 2014
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4215821/
https://www.ncbi.nlm.nih.gov/pubmed/25505694
http://dx.doi.org/10.1186/2213-0802-2-2
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author Stasi, Irene
Cappuzzo, Federico
author_facet Stasi, Irene
Cappuzzo, Federico
author_sort Stasi, Irene
collection PubMed
description BACKGRUOND: Since their first description, activating epidermal growth factor receptor (EGFR) mutations identify a distinct clinical entity of patients with non-small-cell lung cancer (NSCLC). FINDINGS: New targeted therapies for molecularly selected NSCLC are changing the natural history of the disease, with results superior to standard chemotherapy as demonstrated in large phase III studies with first generation EGFR tyrosine kinase inhibitors (TKIs) erlotinib and gefitinib. However, after an initial response, all patients inevitably progress and several mechanisms including a secondary mutation in exon 20 of the EGFR gene (T790M) or MET or HER2 amplifications are responsible for acquired resistance (AR). In clinical practice few options are available for patients with AR, and several new agents or strategies are currently under investigation, including second generation TKIs. CONCLUSIONS: Aim of the present review is to present available data on new EGFR-TKIs and to discuss how these agents could overcome AR to erlotinib or gefitinib.
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spelling pubmed-42158212014-12-10 Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer Stasi, Irene Cappuzzo, Federico Transl Respir Med Short Report BACKGRUOND: Since their first description, activating epidermal growth factor receptor (EGFR) mutations identify a distinct clinical entity of patients with non-small-cell lung cancer (NSCLC). FINDINGS: New targeted therapies for molecularly selected NSCLC are changing the natural history of the disease, with results superior to standard chemotherapy as demonstrated in large phase III studies with first generation EGFR tyrosine kinase inhibitors (TKIs) erlotinib and gefitinib. However, after an initial response, all patients inevitably progress and several mechanisms including a secondary mutation in exon 20 of the EGFR gene (T790M) or MET or HER2 amplifications are responsible for acquired resistance (AR). In clinical practice few options are available for patients with AR, and several new agents or strategies are currently under investigation, including second generation TKIs. CONCLUSIONS: Aim of the present review is to present available data on new EGFR-TKIs and to discuss how these agents could overcome AR to erlotinib or gefitinib. Springer Berlin Heidelberg 2014-01-06 /pmc/articles/PMC4215821/ /pubmed/25505694 http://dx.doi.org/10.1186/2213-0802-2-2 Text en © Stasi and Cappuzzo; licensee Springer. 2014 This article is published under license to BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Report
Stasi, Irene
Cappuzzo, Federico
Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
title Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
title_full Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
title_fullStr Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
title_full_unstemmed Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
title_short Second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
title_sort second generation tyrosine kinase inhibitors for the treatment of metastatic non-small-cell lung cancer
topic Short Report
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4215821/
https://www.ncbi.nlm.nih.gov/pubmed/25505694
http://dx.doi.org/10.1186/2213-0802-2-2
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