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• W2560845936 abstract "The search for potent and efficacious epidermal growth factor receptor (EGFR) inhibitors has been the focus of considerable research over the last three decades. This collective research has resulted in considerable success in the treatment of non-small cell lung cancer (NSCLC) and other cancers driven by EGFR dysregulation. The discovery and clinical development of potent EGFR kinase inhibitors has led to a number of regulatory approvals for this class of inhibitors, following the observation that NSCLC patients harboring activating mutations in EGFR are particularly responsive to therapy. This chapter describes the discovery of the irreversible small molecule EGFR inhibitor, dacomitinib. Structure-activity relationships for inhibition of erbB1, erbB2 and erbB4 were determined for a series of quinazoline- and pyrido[3,4-d]pyrimidine- based analogues. Optimum 4- and 6-substituents with known 7-substituents provided preferred compounds for in vivo testing. Pharmacodynamic screening in vivo led to identification of a quinazoline and a pyrido[3,4-d]pyrimidine as potent irreversible pan erbB inhibitors with superior efficacy to canertinib. Pharmacokinetic comparison of selected lead compounds across three species led to the selection of dacomitinib (PF-00299804) as the preferred clinical candidate. Dacomitinib is currently in phase III clinical development for the treatment of NSCLC and other cancers." @default.
• W2560845936 created "2016-12-16" @default.
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• W2560845936 date "2016-01-01" @default.
• W2560845936 modified "2023-10-01" @default.
• W2560845936 title "The Discovery of Dacomitinib, a Potent Irreversible EGFR Inhibitor" @default.
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• W2560845936 doi "https://doi.org/10.1021/bk-2016-1239.ch008" @default.
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