Tirzepatide is a once-weekly dual agonist of the glucose-dependent insu‘linotropic polypeptide (GIP, aka: gastric inhibitory polypeptide) receptor and glucagon-like peptide-1 (GLP-1) receptor. Both GIP and GLP-1 are hormones secreted by the gut that promote insu’lin secretion. Tirzepatide integrates two insu‘linotropic actions into a single molecule and represents a new class of drugs for the treatment of type 2 diabetes.
Tirzepatide is a dual glucose-dependent insu’linotropic polypeptide-GLP-1 receptor agonist. Its structure is primarily based on the glucose-dependent insu‘linotropic polypeptide amino acid sequence and includes a C20 fatty diacid moiety. Its half-life of approximately 5 days allows once-weekly subcutaneous administration. A phase 2b trial involving patients with type 2 diabetes showed that those who received tirzepatide had dose-dependent reductions in the glycated hemoglobin level and weight at 26 weeks.