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Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.
Journal of medicinal chemistry - 13 Apr 2017
Planken Simon, Behenna Douglas C, Nair Sajiv K, Johnson Theodore O, Nagata Asako, Almaden Chau, Bailey Simon, Ballard T Eric, Bernier Louise, Cheng Hengmiao, Cho-Schultz Sujin, Dalvie Deepak, Deal Judith G, Dinh Dac M, Edwards Martin P, Ferre Rose Ann, Gajiwala Ketan S, Hemkens Michelle, Kania Robert S, Kath John C, Matthews Jean, Murray Brion W, Niessen Sherry, Orr Suvi T M, Pairish Mason, Sach Neal W, Shen Hong, Shi Manli, Solowiej James, Tran Khanh, Tseng Elaine, Vicini Paolo, Wang Yuli, Weinrich Scott L, Zhou Ru, Zientek Michael, Liu Longqing, Luo Yiqin, Xin Shuibo, Zhang Chengyi, Lafontaine Jennifer
Abstract excerpt
Mutant epidermal growth factor receptor (EGFR) is a major driver of non-small-cell lung cancer (NSCLC). Marketed first generation inhibitors, such as erlotinib, effect a transient beneficial response in EGFR mutant NSCLC patients before resistance mechanisms render these inhibitors ineffective. Secondary oncogenic EGFR mutations account for approximately 50% of relapses, the most common being the gatekeeper T790M...
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