| Literature DB >> 24660890 |
Tesfaye Biftu1, 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.
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.Entities:
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Year: 2014 PMID： 24660890 DOI： 10.1021/jm401992e
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446