melogliptin

Melogliptin (also known as GRC-8200 and EMD-675992) is an orally active small molecule dipeptidyl peptidase-4 (DPP-4) inhibitor developed for the treatment of type 2 diabetes mellitus. By inhibiting the DPP-4 enzyme, melogliptin prevents the degradation of incretin hormones such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which in turn stimulates insulin secretion and suppresses glucagon release in a glucose-dependent manner. The compound was originally developed by Glenmark Pharmaceuticals and was licensed to Merck KGaA in 2006 for development in Europe, Japan, and North America; however, Glenmark reacquired these rights in 2008. Melogliptin reached Phase IIb clinical development, where a 12-week study in patients with type 2 diabetes demonstrated significant improvements in glycemic control and a favorable safety and tolerability profile.

Other names

4-fluoro-1-[2-[[(1R,3S)-3-(1,2,4-triazol-1-ylmethyl)cyclopentyl]amino]acetyl]pyrrolidine-2-carbonitrile