Sitagliptin and Vildagliptin: Efficacy of Therapy in Type 2 Diabetes

Author(s): Julienne K. Kirk, Elizabeth C. Oldham

Journal Name: Recent Patents on Endocrine, Metabolic & Immune Drug Discovery
Continued as New Advances on Endocrine Metabolic and Immune Diseases

Volume 2 , Issue 3 , 2008


The clinical efficacy and tolerability of dipeptidyl peptidase-4 (DPP-4) inhibitors for the treatment of type 2 diabetes is supported by published clinical trials. Primary literature and review articles were obtained via a Pubmed search (2002-2008) using the search terms diabetes, sitagliptin, vildagliptin and DPP-4 inhibitors. Eleven sitagliptin trials were identified and reviewed along with 14 vildagliptin studies. Clinical data pertinent to this review were also included. Sitagliptin and vildagliptin belong to a new class of therapeutic agents which enhance endogenous levels of active incretin hormones by inhibiting their degradation by the enzyme DPP-4. The agents have been studied as monotherapy; as add-on therapy to metformin, a sulfonylurea, a thiazolidinedione, and insulin; and as initial-combination therapy with a thiazolidinedione. In clinical trials, treatment with DPP-4 inhibitors produced clinically significant reductions in hemoglobin A1c (A1C). In clinical trials, treatment was weight-neutral and had a rate of hypoglycemia similar to that of placebo. DPP-4 inhibitors have proven efficacy in reducing A1C levels as monotherapy or in combination with other commonly prescribed glucose-lowering agents. More recent phase III trials indicate a sustained effect on reducing blood glucose in type 2 diabetes. DPP-4 inhibitor treatment is well tolerated both as monotherapy and in combination with other agents. This review article also discusses some related patents.

Keywords: A1C, diabetes, dipeptidyl peptidase-4 (DPP-4) inhibitor, efficacy, sitagliptin, vildagliptin

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Article Details

Year: 2008
Published on: 01 March, 2012
Page: [162 - 171]
Pages: 10
DOI: 10.2174/187221408786241784
Price: $65

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