Authors: Kirk, Julienne K.; Oldham, Elizabeth C.

Source: Recent Patents on Endocrine, Metabolic & Immune Drug Discovery, Volume 2, Number 3, November 2008 , pp. 162-171(10)

Publisher: Bentham Science Publishers

Abstract:

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

Document Type: Research article

Publication date: 2008-11-01

More about this publication?

• Recent Patents on Endocrine, Metabolic & Immune Drug Discovery publishes review articles by experts on recent patents in the field of endocrine, metabolic and immune drug discovery e.g. on novel bioactive compounds, analogs & targets. A selection of important and recent patents in the field is also included in the journal. The journal is essential reading for all researchers involved in endocrine, metabolic and immune drug design and discovery.

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• In this Subject: Allergy & Immunology ,  Pharmacology
• By this author: Kirk, Julienne K. ;  Oldham, Elizabeth C.

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