OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical efficacy and safety studies, adverse effects, drug interactions, dosage, and administration of vildagliptin (LAF 237), a dipeptidyl peptidase IV (DPP-4) inhibitor in Phase III development for the treatment of type 2 diabetes mellitus.

DATA SOURCES: Information was obtained from MEDLINE searches of the English-language literature (1990–September 2005). Search terms included vildagliptin, LAF 237, DPP-IV inhibitor, DPP-4 inhibitor, and GLP-1 agonist.

STUDY SELECTION AND DATA EXTRACTION: Available literature reviewed included abstracts, clinical trials with human and animal data, and review articles.

DATA SYNTHESIS: Vildagliptin is a potent and highly selective DPP-4 inhibitor. This novel treatment modality enhances the activity of incretin hormones through inhibition of the enzyme responsible for their degradation.

CONCLUSIONS: Vildagliptin demonstrates good tolerability with minimal adverse effects and can effectively improve metabolic control of glucose through an array of mechanisms.


J Pharm Technol 2006; 22: 105-9.

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