Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.

doi:10.1021/acs.jmedchem.5b01985

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Discovery of (R,E)-N-(7-Chloro-1-(1-[4-(dimethylamino)but-2-enoyl]azepan-3-yl)-1H-benzo[d]imidazol-2-yl)-2-methylisonicotinamide (EGF816), a Novel, Potent, and WT Sparing Covalent Inhibitor of Oncogenic (L858R, ex19del) and Resistant (T790M) EGFR Mutants for the Treatment of EGFR Mutant Non-Small-Cell Lung Cancers.

Journal of medicinal chemistry - 28 Jul 2016

Lelais Gérald, Epple Robert, Marsilje Thomas H, Long Yun O, McNeill Matthew, Chen Bei, Lu Wenshuo, Anumolu Jaganmohan, Badiger Sangamesh, Bursulaya Badry, DiDonato Michael, Fong Rina, Juarez Jose, Li Jie, Manuia Mari, Mason Daniel E, Gordon Perry, Groessl Todd, Johnson Kevin, Jia Yong, Kasibhatla Shailaja, Li Chun, Isbell John, Spraggon Glen, Bender Steven, Michellys Pierre-Yves

Abstract excerpt

Over the past decade, first and second generation EGFR inhibitors have significantly improved outcomes for lung cancer patients with activating mutations in EGFR. However, both resistance through a secondary T790M mutation at the gatekeeper residue and dose-limiting toxicities from wild-type (WT) EGFR inhibition ultimately limit the full potential of these therapies to control mutant EGFR-driven tumors and new...

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PMID: 27433829
DOI: 10.1021/acs.jmedchem.5b01985

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EGFR

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