Dacomitinib, also known as PF-299 and PF-00299804 ; or PF299804, is an orally bioavailable, highly selective, second-generation small-molecule inhibitor of the pan-epidermal growth factor receptor (EGFR) family of tyrosine kinases (ErbB family) with potential antineoplastic activity. Dacomitinib specifically and irreversibly binds to and inhibits human EGFR subtypes, resulting in inhibition of proliferation and induction of apoptosis in EGFR-expressing tumor cells. EGFRs play major roles in tumor cell proliferation and tumor vascularization, and are often overexpressed or mutated in various tumor cell types.
Yu, Shu; Dirat, Olivier. Early and late stage process development for the manufacture of dacomitinib. ACS Symposium Series. Volume 1239. Issue Comprehensive Accounts of Pharmaceutical Research and Development: From Discovery to Late-Stage Process Development, Volume 1. Pages 235-252. Journal; Online Computer File. (2016).
Smaill, Jeff B.; Gonzales, Andrea J.; Spicer, Julie A.; Lee, Helen; Reed, Jessica E.; Sexton, Karen; Althaus, Irene W.; Zhu, Tong; Black, Shannon L.; Blaser, Adrian; Denny, William A.; Ellis, Paul A.; Fakhoury, Stephen; Harvey, Patricia J.; Hook, Ken; McCarthy, Florence O. J.; Palmer, Brian D.; Rivault, Freddy; Schlosser, Kevin; Ellis, Teresa; Thompson, Andrew M.; Trachet, Erin; Winters, R. Thomas; Tecle, Haile; Bridges, Alexander. Tyrosine Kinase Inhibitors. 20. Optimization of Substituted Quinazoline and Pyrido[3,4-d]pyrimidine Derivatives as Orally Active, Irreversible Inhibitors of the Epidermal Growth Factor Receptor Family. Journal of Medicinal Chemistry. Volume 59. Issue 17. Pages 8103-8124. Journal; Online Computer File. (2016).
Lin, Kaichao; Mo, Guoning. A process for preparing dacomitinib. Assignee Hunan Ouya Biological Co., Ltd., Peop. Rep. China. CN 103304492. (2013).
Xu, Xuenong. Process for preparation of Dacomitinib. Assignee Suzhou Miracpharma Technology Co., Ltd., Peop. Rep. China. CN 103288759. (2013).
Cheng, Haibo; Xu, Bin; Zhang, Huibin; Zhou, Jinpei. Synthetic process of antitumor drug dacomitinib. Zhongguo Yaoke Daxue Xuebao. Volume 45. Issue 2. Pages 165-169. Journal. (2014).