Biftu_2014_J.Med.Chem_57_3205

Reference

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

Related information

Inhibitor Omarigliptin
Gene_locus human-DPP4
Structure 4PNZ

Citations formats

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