Overview
Tirzepatide is a first-in-class dual glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1) receptor agonist. FDA-approved as Mounjaro for type 2 diabetes and Zepbound for obesity, tirzepatide demonstrated up to 22.5% weight reduction in the SURMOUNT-1 trial. Its dual mechanism provides complementary metabolic benefits that surpass GLP-1 agonism alone.
Mechanism of action
Tirzepatide simultaneously activates GIP receptors — enhancing glucose-dependent insulin secretion and suppressing glucagon — and GLP-1 receptors, which slow gastric emptying and reduce appetite via hypothalamic signaling. GIP receptor activation also promotes adipocyte lipid utilization and reduces visceral fat accumulation, producing synergistic metabolic effects beyond GLP-1 monotherapy.
Selected literature
- [01]
Tirzepatide once weekly for the treatment of obesity (SURMOUNT-1)
Jastreboff A.M. et al. · New England Journal of Medicine · 2022
Tirzepatide produced a mean weight reduction of up to 22.5% over 72 weeks in adults with obesity, significantly exceeding placebo.
- [02]
Dual GIP and GLP-1 receptor agonist tirzepatide improves glycemic control
Frias J.P. et al. · Lancet · 2021
Tirzepatide demonstrated superior HbA1c reduction and weight loss compared to semaglutide in a head-to-head Phase 3 trial.
- [03]
GIP receptor agonism attenuates GLP-1 receptor agonist-induced nausea
Samms R.J. et al. · Diabetes · 2020
Co-activation of GIP receptors reduced the nausea side-effect profile of GLP-1 agonism while preserving or enhancing metabolic benefits.
The information on this page is summarized from the published research literature and is provided for reference and educational purposes only. It is not medical advice and should not be used to guide treatment decisions. Our peptides are sold for in-vitro research and laboratory use only.