Sitagliptin in real clinical practice today

• Anna L. Terekhova

Abstract

Type 2 diabetes mellitus (T2DM) is characterized by relative insulin deficiency caused by pancreatic β-cell dysfunction and insulin resistance in target organs. The International Diabetes Federation (IDF) publishes data on the prevalence of diabetes mellitus on a regular basis. The continuing progressive growth of the disease is associated with the high prevalence of overweight, obesity and metabolic syndrome. Dipeptidyl peptidase‑4 inhibitors (DPP‑4i) are widely used for more than 15 years in clinical practice. This class of drugs has proven to be effective and safe not only according to data from phase III clinical trials, but also in a number of observational programs. Sitagliptin is a highly selective DPP‑4i and first in class approved for clinical use in patients with T2DM. Early combination therapy of sitagliptin + metformin is pathogenetically substantiated, affecting several links in the pathogenesis of T2DM – ​β-cell dysfunction, hyperglucagonemia, insulin resistance. In addition, sitagliptin-based therapy, can have a long-term (for 10 years) renoprotective and β-cell protective effects. DPP‑4i is not only a beneficial partner for metformin, but also for sodium-glucose transport protein 2 inhibitors, improving overall survival and decreasing adverse events on the sodium-glucose transport protein 2 inhibitors therapy.

Keywords:diabetes mellitus; β-cells; glucagon; α-cells; insulinresistance; DPP 4i; combination therapy

References

1. Diabetes Atlas. 10th ed. International Diabetes Federation, 2021. Online version of IDF Diabetes Atlas. URL: www.diabetesatlas.org

2. Chatterjee S., Khunti K., Davies M.J. Type 2 diabetes. Lancet. 2017; 389 (10 085): 2239–51.

3. Cahn A., Cernea S., Raz I. An update on DPP-4 inhibitors in the management of type 2 diabetes. Expert Opin Emerg Drugs. 2016; 21 (4): 409–19.

4. Goldstein B.J., Feinglos M.N., Lunceford J.K., Johnson J., Williams-Herman D.E. Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes. Diabetes Care. 2007; 30 (8): 1979–87.

5. Scott L.J. Sitagliptin: a review in type 2 diabetes. Drugs. 2017; 77: 209–24.

6. Dedov I.I., Shestakova M.V. Algorithms of specialized medical care for patients with diabetes mellitus. 11th issue. Moscow, 2023. (in Russian)

7. Williams-Herman D., Johnson J., Teng R., et al. Efficacy and safety of sitagliptin and metformin as initial combination therapy and as monotherapy over 2 years in patients with type 2 diabetes. Diabetes Obes Metab. 2010; 12 (5): 442–51.

8. Shestakova M.V. Experience with sitagliptin (the first DPP-4 inhibitor) application to the treatment of type 2 diabetes mellitus in the Russian Federation: results of the DIA-DA observation program. Sakharniy diabet [Diabetes Mellitus]. 2010; (3): 57–60. (in Russian)

9. Hattori S. Ten-year follow-up of sitagliptin treatment in patients with type 2 diabetes mellitus. Diabetol Metab Syndr. 2021; 13: 1–7.

10. Süto G., Molnár G.A., Rokszin G., et al. Risk of morbidity and mortality in patients with type 2 diabetes treated with sodium-glucose cotransporter-2 inhibitor and/or dipeptidyl peptidase-4 inhibitor: a nationwide study. BMJ Open Diabetes Res. Care. 2021; 9 (1): e001765.

11. Instructions for the medical use of the drug Sitadiab^®. LP-No. (000724)-(RG-RU)-220422. (in Russian)

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