J Med Chem. 2014 Apr 24;57(8):3205-12.

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, 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.

Department of Discovery Chemistry, ‡Department of Metabolic Disorders, §Department of Pharmacology, ∥Department of Drug Metabolism, ⊥Basic Pharmaceutical Sciences, and #Department of Safety Assessment and Animal Resources, Merck & Co., Inc. , Whitehouse Station, New Jersey 08889, United States.



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.

PMID: 24660890


TES BIFTUDr Tesfaye Biftu | Tesfaye_Biftu@Merck.com Merck Research Laboratories, K15-ME215 2000 Galloping Hill Road, Kenilworth, NJ 07033

Dr Tesfaye Biftu received his PhD from Brandeis University and an M.B.A. from Rutgers University. After a brief career in academia, he joined Merck in 1981 and later gained experience at CytoMed Inc. Tes returned to Merck in 1995, where he has served as a Distinguished Senior Investigator and Director of Discovery Chemistry, and is currently a Principal Scientist. Tes has published over 110 papers and patents in various areas of drug discovery, including inflammation, cardiovascular disease, thrombosis, obesity, metabolic disorders and infectious disease. He was the program leader and key innovator in the discovery of several drug candidates including omarigliptin. He continues to lecture on various topics in medicinal chemistry and therapeutics at Jefferson University, Philadelphia.

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