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.

doi:10.1158/1078-0432.CCR-17-1192

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Article

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.

Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Nov 2017

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

Abstract excerpt

Purpose:MET exon 14 deletion (METex14 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 METex14 del-positive nonclinical models and NSCLC patients and assessed its ability to overcome resistance to type I MET inhibitors.Experimental Design: As most MET inhibitors in...

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PMID: 28765324
DOI: 10.1158/1078-0432.CCR-17-1192

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