GLP-1/GIP receptor (dual)

Class

Dual GLP-1/GIP receptor agonist

The GLP-1 and GIP receptors are class B G-protein-coupled receptors expressed on pancreatic beta cells, in the central nervous system, and in peripheral tissues including adipose tissue. Both are activated physiologically by incretin hormones released from the gut after eating, and both potentiate insulin secretion in a glucose-dependent manner, meaning insulin release is amplified only when blood glucose is elevated, which limits the risk of dangerously low blood sugar. GLP-1 receptor activation additionally suppresses glucagon secretion, slows gastric emptying, and promotes satiety signals in the brain, contributing to reduced food intake. GIP receptor activation contributes to lipid handling in fat tissue and may add metabolic benefits distinct from those of GLP-1 alone. A dual agonist engages both receptors simultaneously, aiming to combine the glucose-lowering and appetite-suppressing effects of GLP-1 signaling with the additional metabolic contributions of GIP signaling, with the goal of achieving greater improvements in blood sugar control and body weight than agonism at either receptor alone. This mechanism is broadly relevant to type 2 diabetes, where glycemic control is the primary aim, and to obesity, where appetite and energy balance are the therapeutic targets.