How it works
Tirzepatide is a 39-amino acid linear peptide that acts as a dual agonist at both GIP and GLP-1 receptors. Its GIP receptor activity (approximately 5x native GIP potency) enhances fat metabolism in adipose tissue, improves insulin sensitivity in peripheral tissues, and may have direct effects on central appetite regulation through hypothalamic GIP receptors. Its GLP-1 receptor activity (comparable to native GLP-1) slows gastric emptying, promotes satiety through hypothalamic POMC neuron activation, and enhances glucose-dependent insulin secretion. The C20 fatty diacid moiety enables albumin binding, extending the half-life to approximately 5 days for once-weekly dosing. The dual mechanism produces additive effects on weight loss and glycemic control that exceed either pathway alone.

