Vildagliptin: the first innovative DDP-4 inhibitor
https://doi.org/10.14341/2072-0351-5499
Abstract
A review of the main stages of investigation undertaken by Novartis Pharmaceuticals in search of a new molecule for the treatment of type 2 diabetesmellitus, dipeptidyl peptidase-4 (DPP-4) inhibitor (Vildaglyptin). The data on specificity and selectivity of the action of this molecule are presentedalong with the results of its comparison with another agent of this group (sitagliptin).
References
1. Drucker D.J. Enhancing incretin action for the treatment of type 2 diabetes // Diabetes Care. - 2003. - 26. - Р. 2929-2940.
2. Wang Q., Li L., Wong V., Rhodes C., Brubaker P.L. Glucagon-like peptide- 1 regulates proliferation and apoptosis via activation of protein kinase B in pancreatic INS-1 beta cells // Diabetologia. - 2004. - 47(3). - Р. 478-487.
3. Hansen L., Deacon C., Orskov C., et al. Glucagon-like peptide-1- (7-36)amide is transformed to glucagon-like peptide-1-(9-36)amide by dipeptidyl peptidase IV in the capillaries supplying the L cells of the porcine intestine // Endocrinology. - 1999. - 140. - Р. 5356-5363.
4. Rothenberg P., Kalbag J.,Smith H., Gigerich R., et al. Treatment with a DPP-IV inhibitor, NVP - Dpp 728, increases prandial intact GLP-1 levels and reduces glucose exposure in humans // Diabetes. - 2000. - 49 (Suppe1). - A 39.
5. Ahren B., Simonsson E., Larsson H., Landin-Olsson M., et al. Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in type 2 diabetes // Diabetes Care. - 2002 - 25. - P. 869- 875.
6. Villhauer E., Brinkman J., Naderi G., Burkey B. et al. 1-[[(3-hydroxy-1- adamantyl) amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglicemic properties // J.Med.Chem. - 2003. - 46. - P. 2774-2789.
7. Burkey BF., Russell M., Wang K. et al. Vildagliptin displays 'slow tightbinding to DPP-4, but not DPP-8, or DPP-9 // Diabetologia.- 2006.- 49(suppe1): P. 485-486.
8. Ahren B., Landen-Olsson M., Jansson P.A. et al. Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels, and reduces glucagon levels in type 2 diabetes // J. Clin. Endocrinol. Metab. - 2004. - 89. - Р. 2078-2084.
9. Marfella R., Barbieri M., Grella R., et al. Effects of vildagliptin twice daily vs sitagliptin once daily.// Diabetes Complications. - 2010.- 24(2). - P. 79-83.
Review
For citations:
Villkhauer E. Vildagliptin: the first innovative DDP-4 inhibitor. Diabetes mellitus. 2010;13(3):118-120. (In Russ.) https://doi.org/10.14341/2072-0351-5499
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