AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

doi:10.1158/2159-8290.CD-14-0337

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AZD9291, an irreversible EGFR TKI, overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer.

Cancer discovery - 1 Sept 2014

Cross Darren A E, Ashton Susan E, Ghiorghiu Serban, Eberlein Cath, Nebhan Caroline A, Spitzler Paula J, Orme Jonathon P, Finlay M Raymond V, Ward Richard A, Mellor Martine J, Hughes Gareth, Rahi Amar, Jacobs Vivien N, Red Brewer Monica, Ichihara Eiki, Sun Jing, Jin Hailing, Ballard Peter, Al-Kadhimi Katherine, Rowlinson Rachel, Klinowska Teresa, Richmond Graham H P, Cantarini Mireille, Kim Dong-Wan, Ranson Malcolm R, Pao William

Abstract excerpt

UNLABELLED: First-generation EGFR tyrosine kinase inhibitors (EGFR TKI) provide significant clinical benefit in patients with advanced EGFR-mutant (EGFRm(+)) non-small cell lung cancer (NSCLC). Patients ultimately develop disease progression, often driven by acquisition of a second T790M EGFR TKI resistance mutation. AZD9291 is a novel oral, potent, and selective third-generation irreversible inhibitor of both...

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Identifiers

PMID: 24893891
DOI: 10.1158/2159-8290.CD-14-0337
PMCID: PMC4315625

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EGFR

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