The Sound of Evolution
Tirzepatide
替爾泊肽
Mechanism of action:
Tirzepatide 是一種雙重腸泌素受體促效劑（dual incretin receptor agonist），同時作用於胰高血糖素樣肽-1 受體（GLP-1R，glucagon-like peptide-1 receptor）與葡萄糖依賴性促胰島素多肽受體（GIPR，glucose-dependent insulinotropic polypeptide receptor）。Tirzepatide 可活化 GLP-1 受體，促進胰島 β 細胞分泌胰島素，抑制胰島 α 細胞分泌升糖素（glucagon）；對於 GIP 受體會進一步增強胰島 β 細胞分泌胰島素的能力。
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.