Tirzepatide
A dual GIP and GLP-1 receptor agonist — the first of the co-agonists.
Identity
- Class
- Dual GIP/GLP-1 receptor agonist (39 aa, acylated)
- Source
- Synthetic; engineered on a GIP backbone
- Receptor
- GIP receptor + GLP-1 receptor
Key properties
Molecular weight
~4,813.5 Da
Approximate values for the native hormone. Engineered analogs are often deliberately larger and far longer-acting.
Mechanism
Tirzepatide activates both the GIP and GLP-1 receptors from a single GIP-based, acylated peptide, with a half-life of about five days. Engaging two incretin pathways at once is studied for metabolic effects beyond either alone — the rationale behind incretin co-agonism.
Reference notes
- The first approved 'twincretin' — one molecule with dual GIP/GLP-1 agonism.
- Built on a GIP backbone with fatty-acid acylation for once-weekly dosing.
- Its dual mechanism is why it is studied head-to-head against single GLP-1 agonists.
Selected literature
Curated peer-reviewed reviews, sourced from PubMed. Selected for relevance, not exhaustive — open any entry on PubMed for the full record and its primary citations.
- 1.Tirzepatide for overweight and obesity management · Expert opinion on pharmacotherapy, 2025 · PMID 39632534
- 2.Subcutaneously administered tirzepatide vs semaglutide for adults with type 2 diabetes: a systematic review and network meta-analysis of randomised controlled trials · Diabetologia, 2024 · PMID 38613667