Vildagliptin: optimal control in type 2 diabetes mellitus treatment
https://doi.org/10.14341/DM7599
Abstract
Incretin hormones are important for normal pancreatic islet function and glucose homeostasis. Sensitivity to glucose of the α- and β-cells of the pancreas is diminished in type 2 diabetes mellitus (T2DM), leading to impaired insulin secretion, insulin resistance due to elevated glucagon levels in hyperglycaemia and impaired glucagon counterregulation in hypoglycaemia. In addition, T2DM is associated with increased lipotoxicity-induced insulin resistance. This article is a comprehensive review of the safety and efficacy of vildagliptin in patients with T2DM and evaluates the extra-pancreatic effects of incretin-based therapies. Clinical evidence has proven that vildagliptin effectively decreases HbA1c with a low risk of hypoglycaemia and is weight neutral. Vildagliptin also suppresses postprandial triglyceride (TG)-rich lipoprotein levels after ingestion of fat-rich meals and reduces fasting lipolysis, suggesting inhibition of fat absorption and reduced TG stores in non-fat tissues.
About the Author
Alexander Sergeevich Ametov
Russian Medical Academy of Postgraduate Education
Russian Federation
MD, PhD, Professor
Russian Federation
MD, PhD, Professor
References
1. Ahren B, Schweizer A, Dejager S, et al. Mechanisms of action of the dipeptidyl peptidase-4 inhibitor vildagliptin in humans. Diabetes Obes Metab. 2011;13(9):775-783. doi: 10.1111/j.1463-1326.2011.01414.x
2. Schweizer A, Foley JE, Kothny W, Ahren B. Clinical evidence and mechanistic basis for vildagliptin’s effect in combination with insulin. Vasc Health Risk Manag. 2013;9:57-64. doi: 10.2147/VHRM.S40972
3. Дедов И.И., Шестакова М.В. Инкретины: новая веха в лечении сахарного диабета 2 типа. – М.: Дипак; 2010. [Dedov II, Shestakova MV. Inkretiny: novaja veha v lechenii saharnogo diabeta 2 tipa. Moscow: Dipak; 2010.]
4. Ahren B, Carr RD, Deacon CF. Incretin hormone secretion over the day. Vitam Horm. 2010;84:203-220. doi: 10.1016/B978-0-12-381517-0.00007-2
5. Nauck M, Stockmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia. 1986;29(1):46-52. doi: 10.1007/BF02427280
6. Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet. 2006;368(9548):1696-1705. doi: 10.1016/S0140-6736(06)69705-5
7. Boden G, Cheung P, Mozzoli M, Fried SK. Effect of thiazolidinediones on glucose and fatty acid metabolism in patients with type 2 diabetes. Metabolism. 2003;52(6):753-759. doi: 10.1016/S0026-0495(03)00055-6
8. Potashman MH, Duggan ME. Covalent modifiers: an orthogonal approach to drug design. J Med Chem. 2009;52(5):1231-1246. doi: 10.1021/jm8008597
9. Rizzo MR, Barbieri M, Marfella R, Paolisso G. Reduction of Oxidative Stress and Inflammation by Blunting Daily Acute Glucose Fluctuations in Patients With Type 2 Diabetes: Role of dipeptidyl peptidase-IV inhibition. Diabetes Care. 2012;35(10):2076-2082. doi: 10.2337/dc12-0199
10. He YL, Yamaguchi M, Ito H, et al. Pharmacokinetics and pharmacodynamics of vildagliptin in Japanese patients with type 2 diabetes. Int J Clin Pharmacol Ther. 2010;48(9):582-595. doi: 10.5414/CPP48582
11. El-Ouaghlidi A, Rehring E, Holst JJ, et al. The Dipeptidyl Peptidase 4 Inhibitor Vildagliptin Does Not Accentuate Glibenclamide-Induced Hypoglycemia but Reduces Glucose-Induced Glucagon-Like Peptide 1 and Gastric Inhibitory Polypeptide Secretion. J Clin Endocrinol Metab. 2007;92(11):4165-4171. doi: 10.1210/jc.2006-1932
12. Бирюкова Е.В. Вилдаглиптин в клинической практике: анализ сравнительных исследований лекарственных средств с инкретиновой активностью. // Сахарный диабет. – 2014. – Т. 17. – №1 – C.81-84.[Biryukova EV. Clinical implementetion of vildagliptin: data from recent studies comparing incretin-based medications. Diabetes mellitus. 2014;17(1):81-84] doi: 10.14341/DM2014181-84
13. Pittas AG, Joseph NA, Greenberg AS. Adipocytokines and insulin resistance. J Clin Endocrinol Metab. 2004;89(2):447-452. doi: 10.1210/jc.2003-031005
14. Abbott WG, Howard BV, Ruotolo G, Ravussin E. Energy expenditure in humans: effects of dietary fat and carbohydrate. Am J Physiol. 1990;258(2 Pt 1):E347-351.
15. Macauley M, Hollingsworth KG, Smith FE, et al. Effect of vildagliptin on hepatic steatosis. J Clin Endocrinol Metab. 2015;100(4):1578-1585. doi: 10.1210/jc.2014-3794
16. Matthews DR, Dejager S, Ahren B, et al. Vildagliptin add-on to metformin produces similar efficacy and reduced hypoglycaemic risk compared with glimepiride, with no weight gain: results from a 2-year study. Diabetes Obes Metab.2010;12(9):780-789. doi: 10.1111/j.1463-1326.2010.01233.x
17. Matikainen N, Manttari S, Schweizer A, et al. Vildagliptin therapy reduces postprandial intestinal triglyceride-rich lipoprotein particles in patients with type 2 diabetes. Diabetologia. 2006;49(9):2049-2057. doi: 10.1007/s00125-006-0340-2
18. Boschmann M, Engeli S, Dobberstein K, et al. Dipeptidyl-peptidase-IV inhibition augments postprandial lipid mobilization and oxidation in type 2 diabetic patients. J Clin Endocrinol Metab. 2009;94(3):846-852. doi: 10.1210/jc.2008-1400
Supplementary files
Review
For citations:
Ametov A.S. Vildagliptin: optimal control in type 2 diabetes mellitus treatment. Diabetes mellitus. 2015;18(4):125-129. (In Russ.) https://doi.org/10.14341/DM7599
Views:
2493
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License (CC BY-NC-ND 4.0).
Email this article 
