Mechanism of action of inhibitors of dipeptidyl-peptidase-4 (DPP-4)

作者：Thornberry Nancy A; Gallwitz Baptist^*

来源：Best Practice & Research Clinical Endocrinology & Metabolism, 2009, 23(4): 479-486.

DOI：10.1016/j.beem.2009.03.004

• Type 2 diabetes
• oral antidiabetic agents
• DPP-4 inhibitors
• insulinotropic agents
• incretin-based therapies

Dipeptidyl-peptidase IV (DPP-4) inhibitors inhibit the degradation of the incretins, glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP). The first available DPP-4 inhibitors are sitagliptin and vildagliptin. These compounds are orally active and have been shown to be efficacious and well tolerated. Two additional DPP-4 inhibitors are under review, and there are several others in clinical development. This article gives an overview on the mechanism of action of DPP-4 inhibitors and focuses on their development and their important physiological actions with regard to the treatment of type 2 diabetes.

• 出版日期2009-8