Ahren_2006_Expert.Opin.Investig.Drugs_15_431

Vildagliptin is a competitive and reversible inhibitor of dipeptidyl peptidase-4. Dipeptidyl peptidase-4 inhibitors act mainly by preventing the rapid degradation of glucagon-like peptide-1. In clinical trials, vildagliptin improves glycaemic control both as monotherapy and in combination with metformin for periods of < or = 52 weeks in subjects with Type 2 diabetes. This is evident by reduced fasting and prandial glucose levels, and reduced glycosylated haemoglobin levels. Vildagliptin acts by increasing active glucagon-like peptide-1, improving beta-cell function and inhibiting glucagon secretion. Furthermore, vildagliptin has proven to be safe and tolerable, with a low occurrence of hypoglycaemia. Further studies are now required to evaluate its long-term durability, effects, safety and tolerability in comparison with other antidiabetic agents and in different patient subgroups.