EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer

T790M mutation is the most common mechanism for resistance to first- and second-generation tyrosine kinase inhibitors (TKI) for epidermal growth factor receptor (EGFR). Several third-generation EGFR mutant selective TKIs are being explored to conquer this resistance. AZD9291 (osimertinib, tagrisso)...

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Autores principales: Wang, Shuhang, Tsui, Stella T., Liu, Christina, Song, Yongping, Liu, Delong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: BioMed Central 2016
Materias:
Review
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4957905/
https://www.ncbi.nlm.nih.gov/pubmed/27448564
http://dx.doi.org/10.1186/s13045-016-0290-1
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author Wang, Shuhang
Tsui, Stella T.
Liu, Christina
Song, Yongping
Liu, Delong
author_facet Wang, Shuhang
Tsui, Stella T.
Liu, Christina
Song, Yongping
Liu, Delong
author_sort Wang, Shuhang
collection PubMed
description T790M mutation is the most common mechanism for resistance to first- and second-generation tyrosine kinase inhibitors (TKI) for epidermal growth factor receptor (EGFR). Several third-generation EGFR mutant selective TKIs are being explored to conquer this resistance. AZD9291 (osimertinib, tagrisso) has been approved for treatment of the metastatic EGFR T790M mutation-positive non-small cell lung cancer. Resistance to AZD9291 has been described. C797S mutation was reported to be a major mechanism for resistance to T790M-targeting EGFR inhibitors. This review summarizes the latest development in identifying the C797S mutation and EAI045, the novel selective inhibitor overcoming the C797S mutant.
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spelling pubmed-49579052016-07-23 EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer Wang, Shuhang Tsui, Stella T. Liu, Christina Song, Yongping Liu, Delong J Hematol Oncol Review T790M mutation is the most common mechanism for resistance to first- and second-generation tyrosine kinase inhibitors (TKI) for epidermal growth factor receptor (EGFR). Several third-generation EGFR mutant selective TKIs are being explored to conquer this resistance. AZD9291 (osimertinib, tagrisso) has been approved for treatment of the metastatic EGFR T790M mutation-positive non-small cell lung cancer. Resistance to AZD9291 has been described. C797S mutation was reported to be a major mechanism for resistance to T790M-targeting EGFR inhibitors. This review summarizes the latest development in identifying the C797S mutation and EAI045, the novel selective inhibitor overcoming the C797S mutant. BioMed Central 2016-07-22 /pmc/articles/PMC4957905/ /pubmed/27448564 http://dx.doi.org/10.1186/s13045-016-0290-1 Text en © The Author(s). 2016 Open AccessThis article is distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution, and reproduction in any medium, provided you give appropriate credit to the original author(s) and the source, provide a link to the Creative Commons license, and indicate if changes were made. The Creative Commons Public Domain Dedication waiver (http://creativecommons.org/publicdomain/zero/1.0/) applies to the data made available in this article, unless otherwise stated.
spellingShingle Review
Wang, Shuhang
Tsui, Stella T.
Liu, Christina
Song, Yongping
Liu, Delong
EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
title EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
title_full EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
title_fullStr EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
title_full_unstemmed EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
title_short EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
title_sort egfr c797s mutation mediates resistance to third-generation inhibitors in t790m-positive non-small cell lung cancer
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4957905/
https://www.ncbi.nlm.nih.gov/pubmed/27448564
http://dx.doi.org/10.1186/s13045-016-0290-1
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