Tirzepatide is a synthetic peptide that functions as a dual agonist, simultaneously activating both the glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptors. This dual mechanism distinguishes it from single-receptor agonists, as it engages two complementary incretin pathways involved in glucose homeostasis, insulin secretion, and energy metabolism. The GIP receptor activation contributes to enhanced insulin sensitivity and lipid metabolism, while GLP-1 receptor engagement promotes insulin secretion, suppresses glucagon release, and modulates gastric emptying. Research has demonstrated that the combined activation of both pathways produces synergistic metabolic effects that exceed those achievable through single-receptor targeting alone.

Tirzepatide is widely used in preclinical and in vitro research investigating incretin-based metabolic pathways, dual receptor agonism, pancreatic beta-cell function, and insulin sensitivity mechanisms. It serves as a critical reference compound for comparative studies against mono-agonist GLP-1 and GIP receptor ligands. Researchers also employ Tirzepatide in studies examining appetite regulation, energy expenditure, hepatic lipid metabolism, and cardiovascular biomarker modulation. Its well-characterized pharmacological profile makes it an essential tool for metabolic disease research and drug development programs targeting type 2 diabetes and obesity pathways.