Title : Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes - Biftu_2014_J.Med.Chem_57_3205 |
Author(s) : Biftu T , Sinha-Roy R , Chen P , Qian X , Feng D , Kuethe JT , Scapin G , Gao YD , Yan Y , Krueger D , Bak A , Eiermann G , He J , Cox J , Hicks J , Lyons K , He H , Salituro G , Tong S , Patel S , Doss G , Petrov A , Wu J , Xu SS , Sewall C , Zhang X , Zhang B , Thornberry NA , Weber AE |
Ref : Journal of Medicinal Chemistry , 57 :3205 , 2014 |
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. |
PubMedSearch : Biftu_2014_J.Med.Chem_57_3205 |
PubMedID: 24660890 |
Gene_locus related to this paper: human-DPP4 |
Inhibitor | Omarigliptin |
Gene_locus | human-DPP4 |
Structure | 4PNZ |
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE (2014)
Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes
Journal of Medicinal Chemistry
57 :3205
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y, Krueger D, Bak A, Eiermann G, He J, Cox J, Hicks J, Lyons K, He H, Salituro G, Tong S, Patel S, Doss G, Petrov A, Wu J, Xu SS, Sewall C, Zhang X, Zhang B, Thornberry NA, Weber AE (2014)
Journal of Medicinal Chemistry
57 :3205