EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer
Abstract 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, t...
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doaj-b3937d45fda240d68c72d0cfbb74565d2020-11-24T22:51:11ZengBMCJournal of Hematology & Oncology1756-87222016-07-01911510.1186/s13045-016-0290-1EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancerShuhang Wang0Stella T. Tsui1Christina Liu2Yongping Song3Delong Liu4The Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education), Peking University Cancer HospitalSUNY Stony Brook UniversityWeinberg College of Arts and Sciences, Northwestern UniversityHenan Cancer Hospital and the affiliated Cancer Hospital of Zhengzhou UniversityHenan Cancer Hospital and the affiliated Cancer Hospital of Zhengzhou UniversityAbstract 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.http://link.springer.com/article/10.1186/s13045-016-0290-1 |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Shuhang Wang Stella T. Tsui Christina Liu Yongping Song Delong Liu |
spellingShingle |
Shuhang Wang Stella T. Tsui Christina Liu Yongping Song Delong Liu EGFR C797S mutation mediates resistance to third-generation inhibitors in T790M-positive non-small cell lung cancer Journal of Hematology & Oncology |
author_facet |
Shuhang Wang Stella T. Tsui Christina Liu Yongping Song Delong Liu |
author_sort |
Shuhang Wang |
title |
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_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_sort |
egfr c797s mutation mediates resistance to third-generation inhibitors in t790m-positive non-small cell lung cancer |
publisher |
BMC |
series |
Journal of Hematology & Oncology |
issn |
1756-8722 |
publishDate |
2016-07-01 |
description |
Abstract 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. |
url |
http://link.springer.com/article/10.1186/s13045-016-0290-1 |
work_keys_str_mv |
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