Alogliptin (benzoate salt)

Alogliptin is an orally bioavailable dipeptidyl peptidase 4 (DPP-4) inhibitor (IC₅₀ = 6.9 nM) that is selective for DPP-4 over DPP-2, DPP-8, DPP-9, prolyl endopeptidase, fibroblast activation protein (FAP), and tryptase (IC₅₀s = >100,000 nM).¹ It does not inhibit cytochrome P450 enzymes and does not block the human ether-a-go-go-related gene (hERG) channel when used at concentrations up to 30 μM.² Alogliptin inhibits DPP-4 activity in vivo in rats, dogs, and cynomolgus monkeys (EC₅₀s = 3.4, 4.9, and 5.6 ng/ml, respectively, in plasma).¹ It increases plasma glucagon-like peptide-1 (GLP-1; Item No. 24460) and insulin levels and decreases blood glucose levels during an oral glucose challenge in Zucker fa/fa rats when administered at a dose of 10 mg/kg. Alogliptin (2.8 mg/kg per day) decreases plasma DPP-4 activity and increases GLP-1 levels in diabetic ob/ob mice when administered for 29 days.³ Formulations containing alogliptin have been used as an adjunct treatment for type 2 diabetes mellitus.

WARNING This product is not for human or veterinary use.

1. Lee, B., Shi, L., Kassel, D.B., et al. Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. Eur. J. Pharmacol. 589(1-3), 306-314 (2008).

2. Feng, J., Zhang, Z., Wallace, M.B., et al. Discovery of alogliptin: A potent, selective, bioavailable, and efficacious inhibitor of dipeptidyl peptidase IV. J. Med. Chem. 50(10), 2297-2300 (2007).

3. Moritoh, Y., Takeuchi, K., Asakawa, T., et al. Chronic administration of alogliptin, a novel, potent, and highly selective dipeptidyl peptidase-4 inhibitor, improves glycemic control and beta-cell function in obese diabetic ob/ob mice. Eur. J. Pharmacol. 588(2-3), 325-332 (2008).