The antidiabetic effect of the dipeptidyl peptidase 4 (DPP-4) inhibitors depends on the prolongation of action of the 2 incretin hormones: glucagon like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) by preventing their rapid degradation by the enzyme DPP-4. The use of the DPP-4 inhibitor vildagliptin is associated with mean reduction in glycosylated hemoglobin (HbA1c) levels ranging from 0.5% to 1.0% compared with baseline or placebo. Head-to-head trials show that vildagliptin is less effective than metformin and rosiglitazone, and equally effective to submaximal doses of pioglitazone and glimepiride. The main advantages of vildagliptin are the decreased risk of hypoglycemia, the neutral effect on body weight, the simplicity of use, and reassuring safety profile for up to 2 years. However, its moderate efficacy, the lack of long-term safety and efficacy data, the need for evaluation in patients with renal insufficiency, and relative high cost represent its major limitations. Overall, vildagliptin may be a useful second agent for patients with type 2 diabetes who are not optimally controlled on metformin. This drug can also be used as monotherapy in patients with mild hyperglycemia who cannot tolerate metformin or a sulfonylurea (SU).
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