Retatrutide
$25.00
Retatrutide (LY-3437943)
Description:
Retatrutide is an advanced, investigational triple-receptor agonist peptide engineered to simultaneously target the GLP-1 (glucagon-like peptide-1) receptor, GIP (glucose-dependent insulinotropic polypeptide) receptor, and the glucagon (GCGR) receptor. Its multi-agonist action is designed to deliver potent metabolic effects in the realms of weight regulation, glycemic control, and energy homeostasis. New England Journal of Medicine+2PMC+2
Key Benefits & Potential Applications:
Supports significant body weight reduction and adiposity loss in clinical testing Wikipedia+2PMC+2
Enhances glucose regulation and insulin sensitivity, aiding in type 2 diabetes control PMC+2New England Journal of Medicine+2
Promotes favorable changes in energy expenditure via glucagon receptor pathway activation PMC+2PubMed+2
Delays gastric emptying and reduces appetite through GLP-1 and GIP receptor effects Peptide Sciences+1
Potential benefits for non-alcoholic fatty liver disease (NAFLD), metabolic dysfunction, and other obesity-associated comorbidities PMC+1
Mechanism of Action:
The triple-agonist design allows Retatrutide to engage three hormonal axes:
GLP-1 receptor agonism: augments insulin release in response to elevated glucose, delays gastric emptying, and suppresses appetite. New England Journal of Medicine+2PMC+2
GIP receptor agonism: enhances insulinotropic responses and may influence adipose tissue metabolism and energy partitioning. PMC+2Peptide Sciences+2
Glucagon receptor agonism: stimulates hepatic glucose output and contributes to increased energy expenditure and lipid metabolism. PMC+3New England Journal of Medicine+3PubMed+3
By combining these receptor activations in a single molecule, Retatrutide seeks synergistic metabolic regulation—reducing body weight while preserving glycemic control. PMC+1
Pharmacokinetic & Structural Features:
Retatrutide is conjugated to a fatty diacid moiety to extend its half-life, enabling less frequent dosing. Wikipedia+3Synapse+3PMC+3
In clinical trials, dosing frequencies have been once weekly, aligned with other long-acting peptides in metabolic therapy. Everlywell+2PMC+2
The molecule (LY-3437943) demonstrates potent potency across the three receptor types, with EC₅₀ values reported in the low nanomolar or sub-nanomolar range. NovoPro Labs+2New England Journal of Medicine+2
Clinical data have shown mean bodyweight reductions exceeding 17.5 % in subjects without diabetes, with some high-dose cohorts reaching ~24 % weight loss over 48 weeks. Wikipedia+2PMC+2
Safety & Side Effects (Observed in Clinical Studies):
Gastrointestinal adverse events (nausea, diarrhea, vomiting, constipation) were among the most frequently reported effects, often dose-dependent. PMC+2PubMed+2
No significant hypoglycemia was reported in trials with non-diabetic individuals. PMC+2PubMed+2
Other side effects were generally mild to moderate; long-term safety data are still under investigation. PubMed+1
Research & Regulatory Status:
Retatrutide remains an investigational compound and has not been approved for commercial use. It is currently advancing through Phase 3 clinical trials for obesity and metabolic disease indications. PubMed+3PMC+3New England Journal of Medicine+3

