What is Tirzepatide?
Tirzepatide (LY3298176) is a synthetic 39-amino acid peptide engineered as a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Its structure includes a C20 fatty diacid side chain, enhancing albumin binding and enabling once-weekly subcutaneous administration due to its extended half-life (~5 days) (Chavda et al. 2022).
This dual-receptor activity leverages the synergistic effects of GIP and GLP-1 signaling, resulting in pronounced metabolic changes. Tirzepatide demonstrates preferential affinity for GIP receptors while maintaining GLP-1 receptor activation, contributing to improvements in glycemic parameters and energy regulation in experimental models (Min & Bain 2020).
Across randomized controlled trials, Tirzepatide induced dose-dependent reductions in HbA1c and body weight, outperforming GLP-1 receptor agonists and basal insulin comparators (Karagiannis et al. 2022). Reductions in fat mass, as confirmed via body composition studies, indicate preferential loss of adiposity over lean mass (Sokary & Bawadi 2025).
References
Chavda, V. P., Ajabiya, J., Teli, D., Bojarska, J., & Apostolopoulos, V. (2022). Tirzepatide, a new era of dual-targeted treatment for diabetes and obesity: A mini-review. Molecules, 27(13), 4315. https://doi.org/10.3390/molecules27134315
Karagiannis, T., Avgerinos, I., Liakos, A., Del Prato, S., Matthews, D. R., Tsapas, A., & Bekiari, E. (2022). Management of type 2 diabetes with the dual GIP/GLP-1 receptor agonist tirzepatide: A systematic review and meta-analysis. Diabetologia, 65, 1251–1261.
https://doi.org/10.1007/s00125-022-05715-4
Min, T., & Bain, S. C. (2020). The role of tirzepatide, dual GIP and GLP-1 receptor agonist, in the management of type 2 diabetes: The SURPASS clinical trials. Diabetes Therapy, 11(9), 1941–1957. https://doi.org/10.1007/s13300-020-00981-0
Sokary, S., & Bawadi, H. (2025). The promise of tirzepatide: A narrative review of metabolic benefits. Primary Care Diabetes, 19(3), 229–237. https://doi.org/10.1016/j.pcd.2025.03.008
More Information
Tirzepatide Peptide Structure
Product Usage
