Retatrutide vs Tirzepatide — Canada Research Comparison
Retatrutide is an investigational GLP-1 / GIP / glucagon triple agonist in Phase 3, while tirzepatide is a Health Canada approved GLP-1 / GIP dual co-agonist marketed as Mounjaro and Zepbound.
At a glance
Retatrutide and tirzepatide are both engineered incretin-class peptides from Eli Lilly. They share a GLP-1 / GIP backbone but diverge on a single critical point: retatrutide adds glucagon receptor agonism, producing a balanced triple agonist, while tirzepatide stops at the dual receptor profile. That one change shifts retatrutide from an appetite-and-insulin compound to an appetite-and-energy-expenditure compound.
Key facts
| Feature | Retatrutide (LY3437943) | Tirzepatide (LY3298176) |
|---|---|---|
| Class | GLP-1 / GIP / glucagon triple agonist | GLP-1 / GIP dual co-agonist |
| Receptors activated | GLP-1R, GIPR, GCGR | GLP-1R, GIPR |
| Developer | Eli Lilly | Eli Lilly |
| Approval (Canada) | None — Phase 3 | Mounjaro (T2D), Zepbound (obesity) |
| Key trial | Phase 2, Jastreboff NEJM 2023 | SURMOUNT-1, Jastreboff NEJM 2022 |
| Reported weight loss | ~24.2% at 48w (12 mg) | ~20.9% at 72w (15 mg) |
| Dosing | Once weekly SC | Once weekly SC |
| Current programme | TRIUMPH Phase 3 | SURPASS / SURMOUNT completed |
Mechanism contrast
Tirzepatide is built from a GIP backbone with modifications that produce balanced GLP-1R / GIPR co-agonism. The GLP-1 arm drives glucose-dependent insulin secretion, glucagon suppression, delayed gastric emptying, and central appetite reduction. The GIP arm potentiates insulin release and modulates adipose fatty-acid handling.
Retatrutide preserves both of those arms and adds glucagon receptor activation. In preclinical and early human data, glucagon agonism is associated with increased hepatic fatty-acid oxidation and elevated resting energy expenditure — effects that oppose the weight-sparing side of pure glucagon, which normally raises blood glucose. Combining glucagon with GLP-1 appears to neutralise the hyperglycaemic risk while retaining the thermogenic and hepatic-lipid benefits.
Evidence quality
Tirzepatide has a complete Phase 3 dataset (SURPASS for type 2 diabetes, SURMOUNT for obesity) and Health Canada marketing authorisation. Retatrutide is supported by a single published Phase 2 trial in obesity (Jastreboff et al., NEJM 2023) plus interim Phase 2 data in type 2 diabetes and MASLD. The Phase 3 TRIUMPH programme is ongoing — readouts expected from 2025 onward. No cardiovascular outcomes trial has reported for retatrutide.
Regulatory status
Only tirzepatide is a Health Canada approved prescription drug. Research- grade retatrutide and tirzepatide sold as laboratory chemicals are separate, unapproved forms for non-clinical research use only.
Related briefs
Frequently asked questions
What is the core mechanistic difference between retatrutide and tirzepatide?
Is retatrutide approved in Canada?
How do reported weight reductions compare?
Can Canadian researchers purchase either compound?
References
- [1]Jastreboff AM, Kaplan LM, Frías JP, et al.. Triple–Hormone-Receptor Agonist Retatrutide for Obesity — A Phase 2 Trial. New England Journal of Medicine, 2023. DOI: 10.1056/NEJMoa2301972
- [2]Jastreboff AM, Aronne LJ, Ahmad NN, et al.. Tirzepatide Once Weekly for the Treatment of Obesity (SURMOUNT-1). New England Journal of Medicine, 2022. DOI: 10.1056/NEJMoa2206038
- [3]Frías JP, Davies MJ, Rosenstock J, et al.. Tirzepatide versus Semaglutide Once Weekly in Patients with Type 2 Diabetes (SURPASS-2). New England Journal of Medicine, 2021. DOI: 10.1056/NEJMoa2107519
- [4]National Center for Biotechnology Information. PubChem CID 156588324 — Tirzepatide, 2024
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