MET inhibitors for targeted therapy of EGFR TKI-resistant lung cancer

Treatment of non-small cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) activating mutation with EGFR-TKIs has achieved great success, yet faces the development of acquired resistance as the major obstacle to long-term disease remission in the clinic. MET (or c-MET ) gene a...

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Vydané v:	Journal of hematology and oncology Ročník 12; číslo 1; s. 63 - 11
Hlavní autori:	Wang, Qiming, Yang, Sen, Wang, Kai, Sun, Shi-Yong
Médium:	Journal Article
Jazyk:	English
Vydavateľské údaje:	London BioMed Central 21.06.2019 BioMed Central Ltd Springer Nature B.V BMC
Predmet:	Acrylamides - pharmacology Acrylamides - therapeutic use Aniline Compounds - pharmacology Aniline Compounds - therapeutic use Animals Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Cancer Research Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - genetics Development and progression Drug Resistance, Neoplasm Drug therapy Emerging agents and regimens for cancer therapy Epidermal growth factor Epidermal growth factor receptors ErbB Receptors - antagonists & inhibitors ErbB Receptors - genetics Gene amplification Gene expression Genetic aspects Hematology Humans Immunotherapy Kinases Ligands Lung cancer Lung cancer, Non-small cell Lung Neoplasms - drug therapy Lung Neoplasms - genetics Medicine Medicine & Public Health MEK inhibitors Molecular Targeted Therapy Mutation Non-small cell lung carcinoma Oncology Phosphorylation Physiological aspects Protein Kinase Inhibitors - pharmacology Protein Kinase Inhibitors - therapeutic use Proteins Proto-Oncogene Proteins c-met - antagonists & inhibitors Proto-Oncogene Proteins c-met - genetics Remission Review Targeted cancer therapy China
ISSN:	1756-8722, 1756-8722
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Popis
Shrnutí:	Treatment of non-small cell lung cancer (NSCLC) harboring epidermal growth factor receptor (EGFR) activating mutation with EGFR-TKIs has achieved great success, yet faces the development of acquired resistance as the major obstacle to long-term disease remission in the clinic. MET (or c-MET ) gene amplification has long been known as an important resistance mechanism to first- or second-generation EGFR-TKIs in addition to the appearance of T790 M mutation. Recent preclinical and clinical studies have suggested that MET amplification and/or protein hyperactivation is likely to be a key mechanism underlying acquired resistance to third-generation EGFR-TKIs such as osimertinib as well, particularly when used as a first-line therapy. EGFR-mutant NSCLCs that have relapsed from first-generation EGFR-TKI treatment and have MET amplification and/or protein hyperactivation should be insensitive to osimertinib monotherapy. Therefore, combinatorial therapy with osimertinib and a MET or even a MEK inhibitor should be considered for these patients with resistant NSCLC carrying MET amplification and/or protein hyperactivation.
Bibliografia:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 14 ObjectType-Review-3 content type line 23
ISSN:	1756-8722 1756-8722
DOI:	10.1186/s13045-019-0759-9