Structure Report for: 4PNZ

Biftu, T., Sinha-Roy, R., Chen, P., Qian, X., Feng, D., Kuethe, J.T., Scapin, G., Gao, Y.D., Yan, Y., Krueger, D., Bak, A., Eiermann, G., He, J., Cox, J., Hicks, J., Lyons, K.A., He, H., Salituro, G., Tong, S., Patel, S., Doss, G., Petrov, A., Wu, J., Xu, S.S., Sewall, C., Zhang, X., Zhang, B., Thornberry, N.A., Weber, A.E

Title: Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes
Biftu T, Sinha-Roy R, Chen P, Qian X, Feng D, Kuethe JT, Scapin G, Gao YD, Yan Y and Weber AE <19 more 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 (- 19)
Ref: Journal of Medicinal Chemistry, 57:3205, 2014 : PubMed
Abstract


ESTHER: Biftu_2014_J.Med.Chem_57_3205
PubMedSearch: Biftu 2014 J.Med.Chem 57 3205
PubMedID: 24660890
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: Omarigliptin

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.