The Sound of Evolution
Tirzepatide
Mechanism of action:
Tirzepatide is a dual incretin receptor agonist that acts on both the glucagon-like peptide-1 receptor and the glucose-dependent insulinotropic polypeptide receptor. Tirzepatide activates the GLP-1 receptor, promoting insulin secretion from pancreatic beta cells and suppressing glucagon secretion from pancreatic alpha cells. At the GIP receptor, it further enhances the insulin-secreting capacity of pancreatic beta cells.
Reference(s):
1. Coskun T et al. (2018). 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.
2. Frias JP et al. (2020). Tirzepatide: a glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) dual agonist in development for the treatment of type 2 diabetes. Expert Rev Endocrinol Metab.
3. Min T et al. (2021). The Role of Tirzepatide, Dual GIP and GLP-1 Receptor Agonist, in the Management of Type 2 Diabetes: The SURPASS Clinical Trials. Diabetes Ther.