Metabolic & GLP-1 Analogues
Dual GIP/GLP-1 Agonist LY3298176
Scientific Profile
Tirzepatide is a 39-amino acid synthetic peptide that acts as a dual agonist of the glucose-dependent insulinotropic polypeptide (GIP) receptor and the glucagon-like peptide-1 (GLP-1) receptor. The peptide incorporates a C-terminal fatty acid moiety via a linker, facilitating non-covalent albumin binding. In preclinical studies, tirzepatide demonstrated high affinity and potency at both GIP and GLP-1 receptors.
Animal models have shown that this dual agonism results in enhanced improvements in glucose homeostasis and body weight reduction compared to selective GLP-1 receptor agonism. The specific amino acid substitutions, including Aib at position 2, confer resistance to degradation by dipeptidyl peptidase-4 (DPP-4).