Omarigliptin (MK-3102): A Novel Long-Acting DPP-4 Inhibitor for Once-Weekly Treatment of Type 2 Diabetes

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• 作者：Tesfaye Biftu ; Ranabir Sinha-Roy ; Ping Chen ; Xiaoxia Qian ; Dennis Feng ; Jeffrey T. Kuethe ; Giovanna Scapin ; Ying Duo Gao ; Youwei Yan ; Davida Krueger ; Annette Bak ; George Eiermann ; Jiafang He ; Jason Cox ; Jacqueline Hicks ; Kathy Lyons ; Huaibing He ; Gino Salituro ; Sharon Tong ; Sangita Patel ; George Doss ; Aleksandr Petrov ; Joseph Wu ; Shiyao Sherrie Xu ; Charles Sewall ; Xiaoping Zhang ; Bei Zhang ; Nancy A. Thornberry ; Ann E. Weber
• 刊名：Journal of Medicinal Chemistry
• 出版年：2014
• 出版时间：April 24, 2014
• 年：2014
• 卷：57
• 期：8
• 页码：3205-3212
• 全文大小：343K
• 年卷期：v.57,no.8(April 24, 2014)
• ISSN：1520-4804

文摘

In our effort to discover DPP-4 inhibitors with added benefits over currently commercially available DPP-4 inhibitors, MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate. This manuscript summarizes the mechanism of action, scientific rationale, medicinal chemistry, pharmacokinetic properties, and human efficacy data for omarigliptin, which is currently in phase 3 clinical development.