John T Johnson, Kish L Golden, and Rogelio Braceras

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Objective: To review the clinical efficacy and tolerability of vildagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, for the treatment of type 2 diabetes, based on recent Phase 3 trials.

Data Sources: Primary literature and review articles were obtained via a MEDLINE search (2005–November 2007) using the search terms diabetes, vildagliptin, and LAF-237. Additional data from abstracts presented at clinical meetings were included when appropriate.

Study Selection: Nine double-blind, randomized, multicenter, parallel-group trials and vildagliptin studies were identified and reviewed.

Data Synthesis: Vildagliptin, a selective DPP-4 inhibitor, has been shown to produce clinically significant reductions in hemoglobin A1c (A1C) levels when used as monotherapy (0.6–1%) or in combination with other glucose-lowering agents (mean decrease 0.7%). Phase 3 trials indicated a 24- to 52-week sustained effect on reduction of blood glucose in patients with type 2 diabetes. The primary endpoint for all trials was change from baseline A1C. In the intent-to-treat population, baseline A1C was compared with end-of-study A1C. More than 2,500 patients with type 2 diabetes enrolled in monotherapy trials; an additional 2,119 participated in combination therapy trials. Males outnumbered females, and all groups included obese patients. The most common adverse effects reported were nasopharyngitis, headache, and dizziness. Vildagliptin was weight-neutral and produced a rate of hypoglycemia similar to that of placebo.

CONCLUSIONS: Vildagliptin appears to be a promising agent for the management of type 2 diabetes.

J Pharm Technol 2009;25:235-43.