Possibilities of vildagliptin in optimal control of type 2 diabetes mellitus


  • V.I. Pankiv MD, PhD, Professor, Ukrainian Research and Practical Centre of Endocrine Surgery, Transplantation of Endocrine Organs and Tissues of the Ministry of Health of Ukraine, Kyiv, Ukraine; e-mail: endocr@i.ua; Web of Science Researcher ID O-6794-2018 http://orcid.org/0000-0002-9205-9530




type 2 diabetes mellitus, glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide, insulin resistance, vildagliptin, efficiency, review


Incretin hormones are important for the normal functioning of pancreatic islet cells and glucose homeostasis. In type 2 diabetes mellitus, there is a violation of the sensiti­vity of pancreatic α- and β-cells, which leads to progressive insufficient insulin secretion, insulin resistance due to excessive production of glucagon during periods of postprandial hyperglycemia. In addition, type 2 diabetes mellitus is associated with an increase in lipotoxicity directly related to insulin resistance. The literature review provides data on the safety and efficacy of vildagliptin in patients with type 2 diabetes mellitus, as well as on the pancreatic effects of incretin-targeted therapy. It is clinically confirmed that vildagliptin effectively reduces the level of glycated hemoglobin, has a minimal risk of hypoglycemia and is able to maintain a normal body weight. In addition, vildagliptin inhibits postprandial triglyceride production and decreases fas­ting lipolysis, possibly affecting the inhibition of lipid absorption and triglyceride stores in non-adipose tissue cells.


Download data is not yet available.


Ahrén B, Schweizer A, Dejager S, Villhauer EB, Dunning BE, Foley JE. Mechanisms of action of the dipeptidyl peptidase-4 inhibitor vildagliptin in humans. Diabetes Obes Metab. 2011 Sep;13(9):775-83. doi: 10.1111/j.1463-1326.2011.01414.x.

Schweizer A, Foley JE, Kothny W, Ahrén 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.

Ahren B, Carr RD, Deacon CF. Incretin hormone secretion over the day. Vitam Horm. 2010;84:203-20. doi: 10.1016/B978-0-12-381517-0.00007-2.

Nauck M, Stockmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia. 1986 Jan;29(1):46-52. doi: 10.1007/bf02427280.

Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet. 2006 Nov 11;368(9548):1696-705. doi: 10.1016/S0140-6736(06)69705-5.

He YL. Clinical pharmacokinetics and pharmacodynamics of vildagliptin. Clin Pharmacokinet. 2012 Mar 1;51(3):147-62. doi: 10.2165/11598080-000000000-00000.

Xiaoyan C, Jing W, Xiaochun H, Yuyu T, Shunyou D, Yingyu F. Effects of vildagliptin versus saxagliptin on daily acute glucose fluctuations in Chinese patients with T2DM inadequately controlled with a combination of metformin and sulfonylurea. Curr Med Res Opin. 2016 Jun;32(6):1131-6. doi: 10.1185/03007995.2016.1162773.

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 Oct;35(10):2076-82. doi: 10.2337/dc12-0199.

He YL, Yamaguchi M, Ito H, Terao S, Sekiguchi K. Pharmacokinetics and pharmacodynamics of vildagliptin in Japanese patients with type 2 diabetes. Int J Clin Pharmacol Ther. 2010 Sep;48(9):582-95. doi: 10.5414/cpp48582.

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 Nov;92(11):4165-71. doi: 10.1210/jc.2006-1932.

Pittas AG, Joseph NA, Greenberg AS. Adipocytokines and insulin resistance. J Clin Endocrinol Metab. 2004 Feb;89(2):447-52. doi: 10.1210/jc.2003-031005.

Abbott WG, Howard BV, Ruotolo G, Ravussin E. Energy expenditure in humans: effects of dietary fat and carbohydrate. Am J Physiol. 1990 Feb;258(2 Pt 1):E347-51. doi: 10.1152/ajpendo.1990.258.2.E347.

Macauley M, Hollingsworth KG, Smith FE, et al. Effect of vildagliptin on hepatic steatosis. J Clin Endocrinol Metab. 2015 Apr;100(4):1578-85. doi: 10.1210/jc.2014-3794.

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 Sep;12(9):780-9. doi: 10.1111/j.1463-1326.2010.01233.x.

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 Sep;49(9):2049-57. doi: 10.1007/s00125-006-0340-2.

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 Mar;94(3):846-52. doi: 10.1210/jc.2008-1400.

Ou SM, Chen HT, Kuo SC, Chen TJ, Shih CJ, Chen YT. Dipeptidyl peptidase-4 inhibitors and cardiovascular risks in patients with pre-existing heart failure. Heart. 2017 Mar;103(6):414-420. doi: 10.1136/heartjnl-2016-309687.

Kim YG, Yoon D, Park S, et al. Dipeptidyl Peptidase-4 Inhibitors and Risk of Heart Failure in Patients With Type 2 Diabetes Mellitus: A Population-Based Cohort Study. Circ Heart Fail. 2017 Sep;10(9). pii: e003957. doi: 10.1161/CIRCHEARTFAILURE.117.003957.

Zhang J, Chen Q, Zhong J, Liu C, Zheng B, Gong Q. DPP-4 Inhibitors as Potential Candidates for Antihypertensive Therapy: Improving Vascular Inflammation and Assisting the Action of Traditional Antihypertensive Drugs. Front Immunol. 2019 May 9;10:1050. doi: 10.3389/fimmu.2019.01050.

Olivares M, Neyrinck AM, Pötgens SA, et al. The DPP-4 inhibitor vildagliptin impacts the gut microbiota and prevents disruption of intestinal homeostasis induced by a Western diet in mice. Diabetologia. 2018 Aug;61(8):1838-1848. doi: 10.1007/s00125-018-4647-6.

Liao X, Song L, Zeng B, et al. Alteration of gut microbiota induced by DPP-4i treatment improves glucose homeostasis. EBioMedicine. 2019 Jun;44:665-674. doi: 10.1016/j.ebiom.2019.03.057.

Bayrasheva VK, Babenko AY, Bayramov AA, et al. Prospects of nephroprotection against type 2 diabetes using the DPP-4 inhibitor vildagliptin. Medical Council. 2017;(3):8-16. doi: 10.21518/2079-701X-2017-3-8-16. (in Russian).

Tsygankova OV, Veretyuk VV, Ametov AS. Incretins today: multiple effects and therapeutic potential. Diabetes mellitus. 2019;22(1):70-78. doi: 10.14341/DM9841. (in Russian).



How to Cite

Pankiv, V. (2021). Possibilities of vildagliptin in optimal control of type 2 diabetes mellitus. INTERNATIONAL JOURNAL OF ENDOCRINOLOGY (Ukraine), 15(6), 482–487. https://doi.org/10.22141/2224-0721.15.6.2019.185411



Literature Review

Most read articles by the same author(s)

1 2 3 4 5 6 7 8 9 10 > >>