acylated GIP

Acylated GIP refers to a class of long-acting analogs of the glucose-dependent insulinotropic polypeptide (GIP) hormone, modified via the covalent attachment of fatty acid chains (acylation). This modification is a key pharmacological strategy to overcome the rapid degradation of native GIP by the enzyme dipeptidyl peptidase-4 (DPP-4) and its swift renal clearance. By enabling reversible binding to serum albumin, acylation significantly extends the peptide's half-life, allowing for less frequent dosing (e.g., once-weekly). These compounds function as agonists of the GIP receptor (GIPR), which is expressed in pancreatic beta cells, adipose tissue, and the central nervous system. While native GIP's role in type 2 diabetes was historically debated, acylated GIP analogs—particularly when integrated into multi-receptor agonists like the GIP/GLP-1 co-agonist tirzepatide—have demonstrated potent effects on glucose homeostasis, insulin sensitivity, and significant weight loss. Pure acylated GIP mono-agonists and various multi-agonists continue to be explored for metabolic disorders, including obesity and dyslipidemia.

Other names

acylated glucose-dependent insulinotropic polypeptidefatty acid-conjugated GIPlong-acting GIP analog