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What Is Retatrutide? The Triple Agonist Peptide Explained

Retatrutide (LY3437943) is one peptide that activates GIP, GLP-1 and glucagon receptors. Its pharmacology, half-life and trial results.

Retatrutide (LY3437943) is an investigational single peptide that activates three receptors: GIP, GLP-1 and glucagon. Online it is sometimes called “GLP-3”, a nickname rather than a scientific name. Adding glucagon receptor activity to dual incretin agonism is the defining idea behind the molecule, and it has now been tested through phase 3.

For laboratory research use only. The compounds discussed are not approved for human or veterinary use and are not drugs, foods or cosmetics. This article summarises published research and is not medical advice.

Key points

Quick facts

PropertyValue
Development codeLY3437943
ClassLipidated peptide; GIPR/GLP-1R/GCGR triple agonist
Receptor profile (in vitro)GCGR ≈ GLP-1R; GIPR higher
Half-life (human, phase 1b)~6 days
StatusInvestigational; phase 3 results published 2026

Our retatrutide research peptide is supplied as lyophilized powder in 5–60 mg vials with lot-level HPLC and MS data.

Why add glucagon receptor activity?

Glucagon is usually thought of as a hormone that raises blood glucose. It also increases energy expenditure and affects hepatic lipid metabolism. In Lilly’s discovery paper, retatrutide lowered body weight and improved glycaemic control in obese mice, and the authors attributed part of the weight effect to glucagon-receptor-mediated increases in energy expenditure, added to the reduced calorie intake driven by GIP and GLP-1 receptor agonism (Coskun et al., 2022). Pairing glucagon with incretin agonism is intended to capture the energy-expenditure effect while the incretin components offset glucagon’s glucose-raising action.

Pharmacokinetics

In a 12-week phase 1b multiple-ascending-dose trial in 72 adults with type 2 diabetes, retatrutide showed dose-proportional pharmacokinetics and a half-life of about 6 days. Gastrointestinal events were the most frequently reported adverse events (Urva et al., 2022). In the earlier single-ascending-dose study, effects on body weight persisted up to day 43 after a single administration (Coskun et al., 2022). See retatrutide half-life for details.

Clinical trial endpoints

TrialPopulationDurationPrimary endpoint result (range across dose groups)Placebo
Phase 2 (Jastreboff et al., 2023)338 adults with obesity or overweight48 weeksBody weight −8.7% to −24.2% at 48 weeks−2.1%
Phase 3 obesity (Jastreboff et al., 2026)2339 adults with obesity, no diabetes80 weeksBody weight −17.6% to −25.0%−3.9%
Phase 3 type 2 diabetes, TRANSCEND-T2D-1 (Bajaj et al., 2026)537 adults, diet and exercise onlyTreatment period per protocolHbA1c −1.69% to −1.94%−0.81%

The phase 3 obesity trial also included subgroups with knee osteoarthritis (574 participants; WOMAC pain score) and obstructive sleep apnea (243 participants; apnea–hypopnea index), with statistically significant differences versus placebo in both. In all trials the most common adverse events were gastrointestinal and dose-related. These data describe an investigational medicine in controlled clinical trials and do not apply to research material.

Handling research-grade retatrutide

Open questions

Readers following regulatory developments should consult the FDA and EMA directly, since status can change after publication.

Reading the trial numbers: a short glossary

TermMeaning
EstimandA precise definition of the treatment effect being estimated, including how events such as stopping treatment are handled
Treatment-regimen (ITT-like) estimandIncludes all randomised participants regardless of adherence; usually gives smaller effects
Least-squares meanModel-adjusted average used to compare groups
Placebo-adjusted differenceTreatment-group change minus placebo-group change

Two papers on the same molecule can report different numbers simply because they use different estimands, so always check which one a figure refers to.

Related research

Frequently asked questions

What is retatrutide?

Retatrutide (development code LY3437943) is an investigational single peptide with agonist activity at three receptors: the GIP receptor, the GLP-1 receptor and the glucagon receptor.

Why is retatrutide called 'GLP-3'?

‘GLP-3’ is an informal nickname used online because retatrutide acts on three receptors. It is not a scientific name; there is no hormone called GLP-3, and ‘GLP-3 RT’ labels refer to retatrutide.

What is the half-life of retatrutide?

About 6 days in a phase 1b study in people with type 2 diabetes, with dose-proportional pharmacokinetics supporting once-weekly dosing.

How does retatrutide differ from tirzepatide?

Tirzepatide activates GIP and GLP-1 receptors. Retatrutide adds glucagon receptor activity, which in preclinical work increased energy expenditure on top of the reduced calorie intake driven by GIP and GLP-1 receptor agonism.

Is retatrutide approved?

Retatrutide is investigational. Phase 3 results in obesity and type 2 diabetes were published in 2026; regulatory status should be checked with the FDA or EMA for the latest position.

References

  1. Coskun T, et al. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022. PMID: 35985340 https://pubmed.ncbi.nlm.nih.gov/35985340/
  2. Urva S, et al. LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial. Lancet. 2022. PMID: 36354040 https://pubmed.ncbi.nlm.nih.gov/36354040/
  3. Jastreboff AM, et al. Triple-Hormone-Receptor Agonist Retatrutide for Obesity – A Phase 2 Trial. N Engl J Med. 2023. PMID: 37366315 https://pubmed.ncbi.nlm.nih.gov/37366315/
  4. Jastreboff AM, et al. Retatrutide, a Triple Hormone Receptor Agonist, for Treatment of Obesity. N Engl J Med. 2026. PMID: 42814954 https://pubmed.ncbi.nlm.nih.gov/42814954/
  5. Bajaj HS, et al. Efficacy and safety of retatrutide, a GIP, GLP-1, and glucagon receptor agonist, in people with type 2 diabetes and inadequate glycaemic control with diet and exercise (TRANSCEND-T2D-1): a double-blind, randomised, phase 3 trial. Lancet. 2026. PMID: 42250575 https://pubmed.ncbi.nlm.nih.gov/42250575/

For laboratory research use only. The compounds discussed are not approved for human or veterinary use and are not drugs, foods or cosmetics. This article summarises published research and is not medical advice.

Sources

  1. Coskun T, et al. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022. PMID: 35985340
  2. Urva S, et al. LY3437943, a novel triple GIP, GLP-1, and glucagon receptor agonist in people with type 2 diabetes: a phase 1b, multicentre, double-blind, placebo-controlled, randomised, multiple-ascending dose trial. Lancet. 2022. PMID: 36354040
  3. Jastreboff AM, et al. Triple-Hormone-Receptor Agonist Retatrutide for Obesity - A Phase 2 Trial. N Engl J Med. 2023. PMID: 37366315
  4. Jastreboff AM, et al. Retatrutide, a Triple Hormone Receptor Agonist, for Treatment of Obesity. N Engl J Med. 2026. PMID: 42814954
  5. Bajaj HS, et al. Efficacy and safety of retatrutide, a GIP, GLP-1, and glucagon receptor agonist, in people with type 2 diabetes and inadequate glycaemic control with diet and exercise (TRANSCEND-T2D-1): a double-blind, randomised, phase 3 trial. Lancet. 2026. PMID: 42250575
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