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

Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation [2].

Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice [2]. Vildagliptin (10 μmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats [1]. Animal Model: Male db/db mice (BKS) and wildtype mice [2] Dosage: 35 mg/kg Administration: Oral gavage; once daily; for 6 weeks Result: Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44). Animal Model: Obese male Zucker rats [1] Dosage: 10 μmol/kg (Pharmacokinetic Analysis) Administration: Orally Result: Significantly decreased glucose excursions and stimulate insulin secretion.