diaendoСахарный диабетDiabetes mellitus2072-03512072-0378Endocrinology research centre10.14341/2072-0351-5499diaendo-5499Research ArticleСтатьиArticlesВилдаглиптин: первый инновационный ингибитор ДПП-4Vildagliptin: the first innovative DDP-4 inhibitorВиллхауэрЭдвинVillkhauerEdvin-Novartis Pharmaceuticals, East HanoverNovartis Pharmaceuticals, East Hanover201015092010133№3 (2010)118120Copyright © Виллхауэр Э., 20102010Виллхауэр Э.Villkhauer E.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.dia-endojournals.ru/jour/article/view/5499

В статье представлен обзор этапов научного поиска новой молекулы для лечения сахарного диабета 2 типа - ингибитора дипептидил-пептидазы 4 типа (ДПП-4) вилдаглиптина - компанией новартис?. Представлены данные о специфичности и селективности действияданной молекулы, а также данные сравнительного анализа с другими препаратами этой группы (ситаглиптином).

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).

ингибиторы дипептидилпептидазы 4 типаДПП-4вилдаглиптинНовартисdipeptidyl peptidase-4 inhibitorDPP-4vildagliptinNovartisReferencesDrucker D.J. Enhancing incretin action for the treatment of type 2 diabetes // Diabetes Care. - 2003. - 26. - Р. 2929-2940.Drucker D.J. Enhancing incretin action for the treatment of type 2 diabetes // Diabetes Care. - 2003. - 26. - Р. 2929-2940.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.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.

The authors declare that there are no conflicts of interest present.