Tirzepatide

Czech version

Authors: Jan Brož ¹; Marika Koželuhová ¹; Juraj Michalec ¹; Ondřej Lukáč ²
Authors‘ workplace: Interní klinika FN Motol a Homolka, Praha ¹; Klinika hemato-onkologie a buněčné terapie, Univerzitní nemocnice Magdeburg, Německo ²
Published in: Čes. slov. Farm., 2026; 75, 112-116
Category: MEDICAMENT NOVA
doi: https://doi.org/10.36290/csf.2026.020

Overview

Tirzepatide represents a significant breakthrough in the treatment of type 2 diabetes mellitus and/or obesity as the first dual agonist of glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Current analysis of available clinical data demonstrates the exceptional efficacy of tirzepatide in glycemic control, with a dose -⁠ and duration-dependent reduction in HbA1c of 20.4–28.2 mmol/mol. Weight reduction reaches 5–20.9 % with 72 weeks of therapy, with the effect being dose-dependent. The mechanism of action includes improved insulin sensitivity, delayed gastric emptying, and modulation of central regulatory centers for food intake. The safety profile is characterized primarily by gastrointestinal side effects with a treatment discontinuation rate of 4–10 %. Tirzepatide also has beneficial effects on cardiovascular risk factors, including lipid profile and anti-inflammatory biomarkers. A key strategy for optimizing therapeutic outcomes is gradual dose escalation and individualization of treatment according to the patient's clinical condition.

Keywords:

obesity – type 2 diabetes – treatment – tirzepatide

Sources

1. Nadváha a obezita. SZÚ [Internet]. 2023; [cited 2026 Jan 28]. Available from: https://szu.gov.cz/temata-zdravi-a-bezpecnosti/podpora-zdravi/nadvaha-a-obezita/.

2. Diabetes. SZÚ [Internet]. 2023; [cited 2026 Jan 28]. Available from: https://szu.gov.cz/.temata-zdravi-a-bezpecnosti/nemoci-a-jejich-prevence/neinfekcni-nemoci/diabetes/.

3. Bawady N, Aldafrawy O, ElZobair ME, et al. Prevalence of overweight and obesity in type 2 diabetic patients visiting PHC in the Dubai Health Authority. Dubai Diabetes Endocrinol J. 2021;28 : 20-4.

4. Guh DP, Zhang W, Bansback N, et al. The incidence of co-morbidities related to obesity and overweight: a systematic review and meta-analysis. BMC Public Health 2009;9 : 88.

5. Powell J, Taylor J. Use of Dulaglutide, Semaglutide, and Tirzepatide in Diabetes and Weight Management. Clin Ther. 2024 Mar;46(3):289-292.

6. Brož J. Léčba diabetes mellitus 2. typu –⁠ aktuální pohled na jednotlivé lékové třídy a strategii jejich použití. Vnitr Lek. 2025;71 : 144-51.

7. Piťhová P. Tirzepatid –⁠ slibný lék pro kardiovaskulární protekci a léčbu diabetu a obezity. Vnitr Lek. 2025;71 : 51-7.

8. Bonga KN, Padhan M. Incretin Analogues for Weight Reduction in Non-Diabetic Obese: A Review of Liraglutide, Semaglutide, and Tirzepatide Beyond Glycemic Control. Rambam Maimonides Med J. 2026;17:e0006.

9. Sokary S, Bawadi H. The promise of tirzepatide: A narrative review of metabolic benefits. Primary Care Diabetes. 2025;19 : 229-37.

10. Kamrul-Hasan ABM, Chatterjee S, Nagendra L, et al. Efficacy of tirzepatide in glycemic control and weight management in adults with type 2 diabetes: a systematic review and meta-analysis of real-world studies. Postgrad Med J. 2026:qgaf238.

11. Wang L. Designing a Dual GLP-1R/GIPR Agonist from Tirzepatide: Comparing Residues Between Tirzepatide, GLP-1, and GIP. Drug Des Devel Ther. 2022;16 : 1547-59.

12. Coskun T, Sloop KW, Loghin C, et al. LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept. Mol Metab. 2018;18 : 3-14.

13. Baggio LL, Drucker DJ. Biology of incretins: GLP-1 and GIP. Gastroenterology. 2007;132 : 2131-57.

14. Seufert J, Gallwitz B. The extra-pancreatic effects of GLP-1 receptor agonists: a focus on the cardiovascular, gastrointestinal and central nervous systems. Diabetes Obes Metab. 2014;16 : 673-88.

15. Willard FS, Douros JD, Gabe MB, et al. Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist. JCI Insight 2020;5:e140532.

16. Inagaki N, Takeuchi M, Oura T, et al. Efficacy and safety of tirzepatide monotherapy compared with dulaglutide in Japanese patients with type 2 diabetes (SURPASS J-mono): a double-blind, multicentre, randomised, phase 3 trial. Lancet Diabetes Endocrinol. 2022 Sep;10(9):623-633.

17. Aronne LJ, Bade D, le Roux CW, et al. Tirzepatide as compared with semaglutide for the treatment of obesity. N Engl J Med. 2025;393 : 26-36.

18. Wilson JM, Lin Y, Luo MJ, et al. The dual glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 receptor agonist tirzepatide improves cardiovascular risk biomarkers in patients with type 2 diabetes: A post hoc analysis. Diabetes Obes Metab. 2022;24 : 148-53.

19. Taktaz F, Scisciola L, Fontanella RA, et al. Evidence that tirzepatide protects against diabetes-related cardiac damages. Cardiovasc Diabetol. 2024;23 : 112.

20. Goldenberg RM. An indirect treatment comparison of tirzepatide 10 and 15 mg versus high-dose semaglutide 7.2 mg in people with obesity and type 2 diabetes. Diabetes Obes Metab. 2026;28 : 793-5.

21. Wharton S, Freitas P, Hjelmesæth J, et al. Once-weekly semaglutide 7·2 mg in adults with obesity (STEP UP): a randomised, controlled, phase 3b trial. Lancet Diabetes Endocrinol. 2025;13 : 949-63.

22. Lingvay I, Bergenheim SJ, Buse JB, et al.. Once-weekly semaglutide 7·2 mg in adults with obesity and type 2 diabetes (STEP UP T2D): a randomised, controlled, phase 3b trial. Lancet Diabetes Endocrinol. 2025;13 : 935-48.

23. Macabeo B, Quenéchdu A, Aballéa S, et al. Methods for Indirect Treatment Comparison: Results from a Systematic Literature Review. J Mark Access Health Policy. 2024;12 : 58-80.

24. Yao H, Zhang A, Li D, et al. Comparative effectiveness of GLP-1 receptor agonists on glycaemic control, body weight, and lipid profile for type 2 diabetes: systematic review and network meta-analysis. BMJ. 2024;384:e076410.

25. Hagerich K, Durkee M, Goldstein MG. Tirzepatide Once Weekly for the Treatment of Obesity. N Engl J Med. 2022;387 : 1433.

26. Furihata K, Mimura H, Urva S, et al. A phase 1 multiple-ascending dose study of tirzepatide in Japanese participants with type 2 diabetes. Diabetes Obes Metab. 2022;24 : 239-46.

27. Frias JP, Nauck MA, Van J, Benson C, et al. Efficacy and tolerability of tirzepatide, a dual glucose-dependent insulinotropic peptide and glucagon-like peptide-1 receptor agonist in patients with type 2 diabetes: A 12-week, randomized, double-blind, placebo-controlled study to evaluate different dose-escalation regimens. Diabetes Obes Metab. 2020;22 : 938-46.

28. Eli Lilly and Company. Highlights of prescribing information [Internet]. 2023 [cited 2024 Feb 24]. Available from: https://uspl.lilly.com/mounjaro/mounjaro.html#s15.

29. Le TTB, Minh LHN, Devi P, et al. A Case Report of Systemic Allergic Reaction to the Dual Glucose-Dependent Insulinotropic Polypeptide/Glucagon-Like Peptide-1 Receptor Agonist Tirzepatide. Cureus. 2024;16:e51460.

30. Chavda VP, Ajabiya J, Teli D, et al. Tirzepatide, a New Era of Dual-Targeted Treatment for Diabetes and Obesity: A Mini-Review. Molecules. 2022;27 : 4315.

31. Tirzepatide. In LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012.

32. European commission. Souhrn údajů o přípravku. [Internet]. 2025; [cited 2026 Jan 28]. Available from: https://ec.europa.eu/health/documents/community-register/2024/20240419162204/anx_162204_cs.pdf.