Tirzepatide

Tirzepatide is a novel, synthetic 39-amino acid linear peptide that functions as a dual agonist for both the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. Structurally, it is based on the native GIP sequence, modified with a C20 fatty diacid moiety attached via a hydrophilic linker to the lysine residue at position 20, which facilitates albumin binding and extends its half-life. In research settings, Tirzepatide exhibits biased signaling at the GLP-1 receptor and full agonism at the GIP receptor, a mechanism termed “twincretin” agonism, which has been shown to synergistically improve glycemic control and reduce adiposity in preclinical models.