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Omarigliptin (MK-3102): a novel long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes.

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

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,

doi

10.1021/jm401992e

subject

Has Abstract

pub_date

2014-04-24 00:00:00

pages

3205-12

issue

8

eissn

0022-2623

issn

1520-4804

journal_volume

57

pub_type

杂志文章

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