Vildagliptin dihydrate (LAF237 dihydrate) is a potent and stable dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells, exhibiting exceptional oral bioavailability and significant antihyperglycemic activity [1].

Vildagliptin enhances beta cell longevity by preventing apoptosis (cell death) and encouraging cell proliferation [2].

Vildagliptin, administered orally at doses of 35 mg/kg once daily via gavage, effectively increases plasma active GLP-1 levels in the islets of db/db mice, as shown by elevated GLP-1 levels from 11.69±0.44 to 22.63±1.19 after 6 weeks. In a similar vein, when given orally at a dosage of 10 μmol/kg to obese male Zucker rats, vildagliptin significantly reduces glucose excursions and enhances insulin secretion. These findings demonstrate vildagliptin's potential in modulating glucose metabolism and insulin secretion in different animal models of diabetes.