Omarigliptin (MK-3102): A Novel Long-Acting DPP-4 Inhibitor for Once-Weekly Treatment of Type 2 Diabetes
Journal of Medicinal Chemistry2014Vol. 57(8), pp. 3205–3212
Citations Over TimeTop 1% of 2014 papers
Tesfaye Biftu, Ranabir SinhaRoy, Ping Chen, Xiaoxia Qian, Dennis Feng, Jeffrey T. Kuethe, Giovanna Scapin, Ying Gao, Youwei Yan, Davida Krueger, Annette Bak, George J. Eiermann, Jiafang He, Jason M. Cox, Jacqueline D. Hicks, Kathy Lyons, Huaibing He, Gino Salituro, Sharon Tong, Sangita B. Patel, George A. Doss, Aleksandr Petrov, Joseph K. Wu, Shiyao Xu, Charles H. Sewall, Xiaoping Zhang, Bei Zhang, Nancy A. Thornberry, Ann E. Weber
Abstract
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.
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