Tirzepatide

Class: Dual GIP and GLP-1 receptor agonist (“ twincretin ”) Amino Acids: 3 9 FDA Approvals: May 2022 – Type 2 diabetes November 2023 – Obesity management Formulation: Subcutaneous injection, onceweekly dosin g Half-Life: ~ 5 days (via C20 fatty diacid albumin binding) Mechanism of Actio n Tir z epatide is a dual incretin receptor agonist designed to optimi z e metabolic outcomes through: GIP receptor (GIPR) activatio n Enhances glucose-dependent insulin secretion via cAMP/P K A pathways Stimulates β -cell proliferation and reduces apoptosis Contributes to appetite suppression without signi fi cant nausea GLP-1 receptor (GLP-1R) activatio n Stimulates insulin release and suppresses glucagon secretio n Delays gastric emptyin g Provides central appetite regulatio n E x hibits biased signaling favoring cAMP over β -arrestin recruitment → sustained receptor e x pression and enhanced insulin secretory capacit y Synergistic Effects Enhanced insulin secretio n Comprehensive appetite suppression through multiple brain pathways Improved insulin sensitivit y Favorable body composition changes