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Triple agonist◑ Limited human

Retatrutide

Retatrutide is an investigational once-weekly injectable triple agonist activating GLP-1, GIP, and glucagon receptors, currently in Phase 3 (TRIUMPH program) obesity trials after producing the largest average weight loss (~24% in Phase 2, up to ~30% in Phase 3 extension) reported for an incretin therapy to date. It is not FDA-approved and is not available as a prescription drug anywhere.

Molecular weight
~4731.33 g/mol (C221H342N46O68)
g/mol
Half-life
~6 days (144-165 hours)
estimated
Form
Lyophilized powder / compounded (trial drug is pharmaceutical-grade; grey-market vials are unregulated research chemical)
FDA status
Investigational only — not approved; Phase 3 TRIUMPH program ongoing

Retatrutide reconstitution calculator

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Typical dosing

GoalRangeRouteFrequency
Obesity, no type 2 diabetes (Phase 2, NEJM 2023)1, 4, 8, or 12 mg (trial arms)SubQ weekly48 weeks, with 12-week dose-escalation to improve tolerability
Obesity with weight-related comorbidity (Phase 3 TRIUMPH-1)4, 9, or 12 mg (trial arms)SubQ weekly80 weeks primary endpoint; extension data to 104 weeks
Obesity + knee osteoarthritis (Phase 3 TRIUMPH-4)up to 12 mg (trial arm)SubQ weekly68 weeks
Liver fat / MASLD (Phase 2a, Nature Medicine)up to 12 mg (trial arms)SubQ weekly24 weeks
Obesity + type 2 diabetes (Phase 3 TRIUMPH-2)not yet publicly reported by doseSubQ weeklytrial ongoing, results not yet published

Ranges compiled from research literature — not a prescription.

How it works

Retatrutide is a single-molecule peptide, 39 amino acids, engineered to simultaneously activate three receptors: the glucagon-like peptide-1 receptor (GLP-1R), the glucose-dependent insulinotropic polypeptide receptor (GIPR), and the glucagon receptor (GCGR). A C20 fatty-acid side chain lets it bind albumin non-covalently, extending its half-life to roughly six days and enabling once-weekly dosing, similar in concept to tirzepatide's fatty-acid conjugation but with glucagon receptor activity added on top.

The rationale for adding glucagon-receptor agonism to the GLP-1/GIP combination already used by tirzepatide is that glucagon receptor activation increases energy expenditure and hepatic fat oxidation, which is proposed to add a thermogenic, calorie-burning effect on top of the appetite suppression and delayed gastric emptying produced by GLP-1/GIP agonism. This is why retatrutide is sometimes called a 'triple-G' or 'GGG' agonist in the literature.

The evidence base is still limited to clinical trials, not real-world prescribing. In the Phase 2 trial published in the New England Journal of Medicine (Jastreboff et al., 2023), 338 adults with obesity or overweight without type 2 diabetes received weekly subcutaneous retatrutide (1, 4, 8, or 12 mg) or placebo for 48 weeks; the 12 mg group lost a mean of about 24.2% of body weight, exceeding results reported at the time for semaglutide 2.4 mg (~15% at 68 weeks) and tirzepatide 15 mg (~22.5% at 72 weeks). A separate Phase 2a trial in metabolic dysfunction-associated steatotic liver disease (MASLD), published in Nature Medicine, reported substantial reductions in liver fat content. Eli Lilly's Phase 3 TRIUMPH-1 trial (obesity with a weight-related comorbidity) later reported average weight loss of up to 30.3% (about 85 lbs) at 104 weeks in a pre-specified extension for participants with BMI >=35, and TRIUMPH-4 (obesity plus knee osteoarthritis) reported ~28.7% weight loss alongside meaningful reductions in WOMAC pain scores at 68 weeks.

Despite these results, retatrutide remains investigational: it has not completed Phase 3, has not been submitted for or granted FDA approval, and no long-term safety or outcomes data beyond the trial periods exist. It is nonetheless sold on the 'research chemical' grey market, produced outside FDA oversight and typically labeled 'not for human consumption,' where independent testing has found meaningful rates of contamination, incorrect peptide sequences, and endotoxin levels above safety thresholds.

Side effects & safety

  • Gastrointestinal side effects (nausea, vomiting, diarrhea) are the most common adverse events across all published trials and tend to increase with dose, consistent with the wider GLP-1 receptor agonist class.
  • Retatrutide is investigational — no long-term (multi-year) safety, cardiovascular outcome, or real-world data exist yet outside the ongoing trial population.
  • It is not FDA-approved for any indication; it cannot legally be prescribed or dispensed as a medicine in the United States or elsewhere at this time.
  • Grey-market vials sold as 'research chemical' or 'not for human consumption' are not FDA-reviewed for identity, strength, purity, or sterility — independent testing of similar grey-market peptides has found high rates of endotoxin contamination and incorrect sequences.
  • Dose-escalation protocols used in trials (gradual titration over roughly 12 weeks) were specifically designed to improve tolerability; ad hoc, unsupervised dosing carries higher risk of adverse effects.
  • Anyone considering retatrutide, in a trial or otherwise, should consult a licensed clinician; this is not a substitute for medical advice, and self-sourced investigational compounds carry risks that clinical-trial material does not.

Research

Primary sources — PubMed.

  1. Jastreboff AM, et al. Triple-Hormone-Receptor Agonist Retatrutide for Obesity — A Phase 2 Trial. N Engl J Med. 2023. https://www.nejm.org/doi/full/10.1056/NEJMoa2301972
  2. Loomba R, et al. Triple hormone receptor agonist retatrutide for metabolic dysfunction-associated steatotic liver disease: a randomized phase 2a trial. Nat Med. 2024. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC11271400/
  3. Eli Lilly and Company. Lilly's triple agonist, retatrutide, delivered powerful weight loss in pivotal Phase 3 obesity trial (TRIUMPH-1). https://investor.lilly.com/news-releases/news-release-details/lillys-triple-agonist-retatrutide-delivered-powerful-weight-loss
  4. AJMC. Retatrutide Achieves Up to 30.3% Average Weight Loss in Phase 3 TRIUMPH-1 Trial. https://www.ajmc.com/view/retatrutide-achieves-up-to-30-3-average-weight-loss-in-phase-3-triumph-1-trial
  5. ClinicalTrials.gov. A Study of Retatrutide (LY3437943) on Renal Function in Participants With Overweight or Obesity and Chronic Kidney Disease. NCT05936151. https://clinicaltrials.gov/study/NCT05936151
  6. MedChemExpress. Retatrutide (LY3437943) Product Data Sheet — CAS 2381089-83-2, molecular formula C221H342N46O68, MW 4731.33. https://www.medchemexpress.com/retatrutide.html
⚠︎Retatrutide may be a research chemical not approved for human use in your country. This page is educational information only — not medical advice, and not an endorsement to use it.
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Related compounds

SemaglutideGLP-1 agonistTirzepatideGIP/GLP-1 agonistMOTS-cMitochondrial peptideGHK-CuCopper peptidePT-141Libido peptide

Retatrutide FAQ

No. Retatrutide is investigational, still in the Phase 3 TRIUMPH program, and has not been approved by the FDA or any other regulator. It cannot legally be prescribed or dispensed as a medicine anywhere. The only legitimate access is enrollment in a clinical trial; anything sold online is grey-market material produced outside regulatory oversight.
In the Phase 2 trial published in NEJM, the 12 mg group lost a mean 24.2% of body weight over 48 weeks. Eli Lilly's Phase 3 TRIUMPH-1 later reported up to 30.3% average weight loss at 104 weeks in a pre-specified extension for participants with BMI 35 or above, and TRIUMPH-4 reported roughly 28.7% at 68 weeks alongside reduced knee osteoarthritis pain scores.
It adds a third receptor target. Tirzepatide activates GIP and GLP-1 receptors; retatrutide activates those plus the glucagon receptor, making it a triple agonist. Glucagon receptor activation is proposed to increase energy expenditure and hepatic fat oxidation, adding a thermogenic component on top of the appetite suppression and delayed gastric emptying that GLP-1 and GIP agonism provide.
Grey-market vials are not reviewed for identity, strength, purity, or sterility, and are typically labeled not for human consumption. Independent testing of comparable grey-market peptides has found meaningful rates of contamination, incorrect peptide sequences, and endotoxin levels above safety thresholds. Trial participants also received gradual dose escalation over roughly 12 weeks specifically to manage tolerability, which unsupervised use bypasses.

Keep reading

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