Seven steps of sitagliptin – therapeutic guide for practicing physician Review article
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Published:
Mar 31, 2025
Keywords:
dipeptidyl peptidase 4 inhibitors, sitagliptin, type 2 diabetes mellitus
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Abstract
Sitagliptin is the most commonly used representative of dipeptidyl peptidase 4 (DPP-4) inhibitors, known as gliptins. According to current guidelines of the Diabetes Poland, DPP-4 inhibitors are component of type 2 diabetes mellitus therapy at the stage of initiating monotherapy, in the case of metformin intolerance, or at the stage of therapy intensification to achieve glycemic goals, while simultaneously providing patient education and behavioural management. Thanks to good tolerability, lack of significant side effects, and a safe cardiovascular profile, sitagliptin can be combined with other antihyperglycemic drug groups, including insulin, also in patients with chronic kidney disease. Therapeutic guide highlights potential applications of sitagliptin in the clinical practice.
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Łebkowska, A. (2025). Seven steps of sitagliptin – therapeutic guide for practicing physician. Medycyna Faktow (J EBM), 18(1(66), 85-90. https://doi.org/10.24292/01.MF.0125.13
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References
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2. Defronzo RA. Banting Lecture. From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus. Diabetes. 2009; 58(4): 773-95.
3. Green JB, Bethel MA, Armstrong PW et al.; TECOS Study Group. Effect of Sitagliptin on Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. 2015; 373(3): 232-42.
4. Scott LJ. Sitagliptin: A Review in Type 2 Diabetes. Drugs. 2017; 77(2): 209-24.
5. Enzan N, Matsushima S, Kaku H et al. Beneficial Effects of Dipeptidyl Peptidase-4 Inhibitors on Heart Failure With Preserved Ejection Fraction and Diabetes. JACC Asia. 2023; 3(1): 93-104.
6. Yanagimachi T, Fujita Y, Takeda Y et al. Dipeptidyl peptidase-4 inhibitor treatment induces a greater increase in plasma levels of bioactive GIP than GLP-1 in non-diabetic subjects. Mol Metab. 2016; 6(2): 226-31.
7. Zaccardi F, Jacquot E, Cortese V et al. Comparative effectiveness of gliclazide modified release versus sitagliptin as second-line treatment after metformin monotherapy in patients with uncontrolled type 2 diabetes. Diabetes Obes Metab. 2020; 22(12): 2417-26.
8. Zhang Y, Hong J, Chi J et al. Head-to-head comparison of dipeptidyl peptidase-IV inhibitors and sulfonylureas - a meta-analysis from randomized clinical trials. Diabetes Metab Res Rev. 2014; 30(3): 241-56.
9. Sakura H, Hashimoto N, Sasamoto K et al. Effect of sitagliptin on blood glucose control in patients with type 2 diabetes mellitus who are treatment naive or poorly responsive to existing antidiabetic drugs: the JAMP study. BMC Endocr Disord. 2016; 16(1): 70.
10. Chen R, Li J, Chen D et al. Efficacy and Safety of DPP-4 Inhibitors and Metformin Combinations in Type 2 Diabetes: A Systematic Literature Review and Network Meta-Analysis. Diabetes Metab Syndr Obes. 2024; 17: 2471-93.
11. Frias JP, Zimmer Z, Lam RLH et al. Double-blind, randomized clinical trial assessing the efficacy and safety of early initiation of sitagliptin during metformin uptitration in the treatment of patients with type 2 diabetes: The CompoSIT-M study. Diabetes Obes Metab. 2019; 21(5): 1128-35.
12. Roussel M, Mathieu J, Dalle S. Molecular mechanisms redirecting the GLP-1 receptor signalling profile in pancreatic β-cells during type 2 diabetes. Horm Mol Biol Clin Investig. 2016; 26(2): 87-95.
13. Derosa G, Carbone A, Franzetti I et al. Effects of a combination of sitagliptin plus metformin vs metformin monotherapy on glycemic control, β-cell function and insulin resistance in type 2 diabetic patients. Diabetes Res Clin Pract. 2012; 98(1): 51-60.
14. Matthews DR, Paldánius PM, Proot P et al. Glycaemic durability of an early combination therapy with vildagliptin and metformin versus sequential metformin monotherapy in newly diagnosed type 2 diabetes (VERIFY): a 5-year, multicentre, randomised, double-blind trial. Lancet. 2019; 394(10208): 1519-29.
15. Tsapas A, Karagiannis T, Kakotrichi P et al. Comparative efficacy of glucose-lowering medications on body weight and blood pressure in patients with type 2 diabetes: A systematic review and network meta-analysis. Diabetes Obes Metab. 2021; 23(9): 2116-24.
16. Zhang Y, Hong J, Chi J et al. Head-to-head comparison of dipeptidyl peptidase-IV inhibitors and sulfonylureas – a meta-analysis from randomized clinical trials. Diabetes Metab Res Rev. 2014; 30(3): 241-56.
17. Tanase DM, Gosav EM, Costea CF et al. The Intricate Relationship between Type 2 Diabetes Mellitus (T2DM), Insulin Resistance (IR), and Nonalcoholic Fatty Liver Disease (NAFLD). J Diabetes Res. 2020; 2020: 3920196.
18. Jang H, Kim Y, Lee DH et al. Outcomes of Various Classes of Oral Antidiabetic Drugs on Nonalcoholic Fatty Liver Disease. JAMA Intern Med. 2024; 184(4): 375-83.
19. Charakterystyka produktu leczniczego Jazeta.
20. Li M, Wang S, Wang X. Efficacy and Safety of Triple Therapy with SGLT-2 Inhibitor, DPP-4 Inhibitor, and Metformin in Type 2 Diabetes: A Meta-Analysis. Altern Ther Health Med. 2023; 29(5): 320-6.
21. Shankar RR, Bao Y, Han P et al. Sitagliptin added to stable insulin therapy with or without metformin in Chinese patients with type 2 diabetes. J Diabetes Investig. 2017; 8(3): 321-9.
22. de Boer IH, Khunti K, Sadusky T et al. Diabetes Management in Chronic Kidney Disease: A Consensus Report by the American Diabetes Association (ADA) and Kidney Disease: Improving Global Outcomes (KDIGO). Diabetes Care. 2022; 45(12): 3075-90.
23. Kawanami D, Takashi Y, Takahashi H et al. Renoprotective Effects of DPP-4 Inhibitors. Antioxidants (Basel). 2021; 10(2): 246.