Glesatinib Exhibits Antitumor Activity in Lung Cancer Models and Patients Harboring MET Exon 14 Mutations and Overcomes Mutation-mediated Resistance to Type I MET Inhibitors in Nonclinical Models

exon 14 deletion ( ex14 del) mutations represent a novel class of non-small cell lung cancer (NSCLC) driver mutations. We evaluated glesatinib, a spectrum-selective MET inhibitor exhibiting a type II binding mode, in ex14 del-positive nonclinical models and NSCLC patients and assessed its ability to...

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Veröffentlicht in:	Clinical cancer research 2017-11, Vol.23 (21), p.6661-6672
Hauptverfasser:	Engstrom, Lars D, Aranda, Ruth, Lee, Matthew, Tovar, Elizabeth A, Essenburg, Curt J, Madaj, Zachary, Chiang, Harrah, Briere, David, Hallin, Jill, Lopez-Casas, Pedro P, Baños, Natalia, Menendez, Camino, Hidalgo, Manuel, Tassell, Vanessa, Chao, Richard, Chudova, Darya I, Lanman, Richard B, Olson, Peter, Bazhenova, Lyudmilla, Patel, Sandip Pravin, Graveel, Carrie, Nishino, Mizuki, Shapiro, Geoffrey I, Peled, Nir, Awad, Mark M, Jänne, Pasi A, Christensen, James G
Format:	Artikel
Sprache:	eng
Schlagworte:	Adult Aged Animals Anticancer properties Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Antitumor activity Benzeneacetamides - pharmacology Benzeneacetamides - therapeutic use Binding Cancer Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - genetics Carcinoma, Non-Small-Cell Lung - pathology Cell Line, Tumor Clinical trials Clonal deletion Deoxyribonucleic acid DNA Drug Resistance, Neoplasm - drug effects Exons - genetics Experimental design Female Humans Inhibitors Kinetics Liver Liver Neoplasms - drug therapy Liver Neoplasms - genetics Liver Neoplasms - pathology Liver Neoplasms - secondary Lung cancer Male Medical research Metastases Mice Middle Aged Mutation Non-small cell lung carcinoma Patients Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - adverse effects Proto-Oncogene Proteins c-met - antagonists & inhibitors Proto-Oncogene Proteins c-met - genetics Pyrazoles - administration & dosage Pyridines - administration & dosage Pyridines - pharmacology Pyridines - therapeutic use Signaling Xenograft Model Antitumor Assays Xenografts
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