Omarigliptin is an investigational long-acting inhibitor of dipeptidyl peptidase 4 (DPP4). The first DPP4 inhibitor to be clinically approved was sitagliptin. This has subsequently been joined by several more drugs such as vildagliptin, saxagliptin, linagliptin and alogliptin.
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.
