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A lipidated GIPR (glucose-dependent insulinotropic polypeptide receptor) agonist is a class of therapeutic peptides engineered to activate the GIP receptor while possessing a lipid (fatty acid) side chain to extend its circulating half-life. By mimicking the endogenous incretin hormone GIP, these agonists stimulate glucose-dependent insulin secretion from pancreatic beta cells, enhance lipid buffering in adipose tissue, and act on the central nervous system to regulate appetite and energy expenditure. Lipidation allows the peptide to bind reversibly to serum albumin, protecting it from rapid enzymatic degradation (such as by dipeptidyl peptidase-4) and renal clearance, thereby enabling less frequent dosing. Lipidated GIPR agonists are primarily investigated or utilized in the treatment of metabolic disorders, including type 2 diabetes and obesity, often in combination with GLP-1 receptor agonists.
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