Tirzepatide
A dual GIP/GLP-1 receptor agonist approved by the FDA for type 2 diabetes and chronic weight management. Included here as a reference profile only.
| Total citations | 4 |
|---|---|
| Human clinical studies | 3 |
| Animal models | 0 |
| In vitro studies | 1 |
| Reviews / meta-analyses | 0 |
Mechanism of action
Tirzepatide is based on the GIP sequence and agonises both the GIP and GLP-1 receptors. Willard and colleagues showed it is an imbalanced and biased dual agonist — full potency at GIPR but weaker GLP-1R affinity, with signalling bias toward cAMP generation over beta-arrestin recruitment and reduced GLP-1R internalisation.
The combined incretin action enhances glucose-dependent insulin secretion and produces greater reductions in food intake and body weight than GLP-1 receptor agonism alone.
Peer-reviewed literature
Study type is tagged on every entry so animal and in-vitro findings are never mistaken for human clinical evidence.
Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes
SURPASS-2 head-to-head phase 3 trial against semaglutide.
Tirzepatide Once Weekly for the Treatment of Obesity
SURMOUNT-1 phase 3 trial in obesity.
Tirzepatide is an imbalanced and biased dual GIP and GLP-1 receptor agonist
Receptor pharmacology establishing the biased dual-agonist mechanism.
LY3298176, a novel dual GIP and GLP-1 receptor agonist for the treatment of type 2 diabetes mellitus: From discovery to clinical proof of concept
Discovery paper through to phase 1 human proof of concept.
Limitations & open questions
Tirzepatide is an FDA-approved prescription medicine (Mounjaro, Zepbound) and is under patent. It is a regulated drug product, not a research chemical.