GIP Receptor Agonist
A compound that activates the glucose-dependent insulinotropic polypeptide (GIP) receptor. GIP receptor agonism is a component of tirzepatide, the first approved dual GLP-1/GIP receptor agonist, which demonstrated superior weight loss and glycaemic control compared to selective GLP-1 receptor agonists in clinical trials.
Technical Context
GIP (glucose-dependent insulinotropic polypeptide) acts through the GIPR, a GPCR expressed on pancreatic beta cells, adipocytes, osteoblasts, and brain neurons. Tirzepatide activates both GLP-1R and GIPR — its GIP component may contribute to superior weight loss through central appetite mechanisms and peripheral metabolic effects. Interestingly, both GIP receptor agonism and antagonism have shown metabolic benefits in preclinical models, creating debate about the optimal approach. Several investigational compounds targeting GIP receptors (alone or in combination with GLP-1R and glucagon receptors) are in clinical development, representing a highly active area of metabolic drug research.