Metabolic and neuroendocrine
Dual GIP and GLP-1 receptor signalling
Simultaneous agonism of glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1 receptors affects glucose-dependent insulin secretion, appetite regulation, gastric function and energy balance.
Biological pathway
GIP receptor and GLP-1 receptor agonism → Gs protein signalling → increased cyclic AMP in responsive tissues → coordinated metabolic and appetite-related effects.
Evidence summary
Tirzepatide has established dual-receptor pharmacology and randomized clinical evidence for glycaemic control and chronic weight management.
Limitations
The relative contribution of GIP receptor activation versus GLP-1 receptor activation to individual clinical outcomes remains incompletely resolved.