Drug intelligence / Profile preview

retagliptin

Development stage
Phase 4
Lead developer
Hengrui Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

Retagliptin is a small molecule oral dipeptidyl peptidase 4 (DPP‑4) inhibitor developed by Jiangsu Hengrui Medicine for the treatment of type 2 diabetes mellitus. It acts as a competitive inhibitor of DPP‑4 to prevent the degradation of incretin hormones such as glucagon-like peptide‑1 (GLP‑1) and glucose-dependent insulinotropic polypeptide (GIP), thereby increasing their plasma concentrations. This leads to enhanced insulin secretion in a glucose-dependent manner and reduced glucagon release from pancreatic alpha cells. Retagliptin has demonstrated efficacy in lowering HbA1c levels both as monotherapy and in combination with metformin in clinical trials. It was approved for marketing in China under the trade name 瑞泽唐 for improving blood glucose control in adults with type 2 diabetes[1][3][5][8].

Brand names
瑞泽唐
Other names
retagliptin phosphatemethyl (R)-7-(3-amino-4-(2,4,5-trifluorophenyl)butanoyl)-3-(trifluoromethyl)-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine-1-carboxylatemethyl 7-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-(trifluoromethyl)-5H,6H,8H-imidazo[1,5-a]pyrazine-1-carboxylate
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)

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