Mini-review: Pharmacokinetics of omarigliptin, a once-weekly dipeptidyl peptidase-4 inhibitor

Document Type

Article

Publication Date

1-1-2016

Abstract

The dipeptidyl peptidase-4 (DPP-4) inhibitors are novel oral hypoglycemic drugs which have been in clinical use for the past 10 years. The drugs are safe, weight neutral and widely prescribed. There are currently many gliptins approved by FDA, namely sitagliptin, vildagliptin, saxagliptin, linagliptin, alogliptin with several more in advanced stages of development. The gliptins may possess cardiovascular protective effects and their administration may promote ß-cell survival; claims currently being evaluated in clinical and preclinical studies. The gliptins are an optional second-line therapy after metformin; they are generally well tolerated with low risk of hypoglycemia. The various compounds differ with respect to their pharmacokinetic properties; however, their clinical efficacy appears to be similar. The clinical differences between the various compounds stem from effects other than hypoglycemic effects, their safety and side effects profile. The currently registered compounds appear to have maximized the clinical potential of DPP-4 inhibition, and the new compounds in the companies' pipelines seem to be as effective as the ones presently in use. In our effort to review and evaluate DPP-4 inhibitors with added benefits over currently commercially available DPP-4 inhibitors, omarigliptin was selected for this review article as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing. Omarigliptin is a potent, oral, long-acting (DPP)-4 inhibitor approved in Japan and in global development as a once-weekly treatment for type 2 diabetes mellitus. The aim of this review was to investigate the different pharmacokinetic studies of omarigliptin in a concise way in the form of tables.

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