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

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...

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Bibliographic Details
Published in:Baillière's best practice & research. Clinical endocrinology & metabolism 2009-08, Vol.23 (4), p.479-486
Main Authors: Thornberry, Nancy A., PhD, Gallwitz, Baptist, MD
Format: Article
Language:English
Subjects:
DPP-4 inhibitors
Endocrinology & Metabolism
incretin-based therapies
insulinotropic agents
oral antidiabetic agents
Type 2 diabetes
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Summary: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.
ISSN:1521-690X
1878-1594
DOI:10.1016/j.beem.2009.03.004