Purpose | Dosage | Frequency | Administration |
---|---|---|---|
Obesity Treatment | 1-12 mg | Once weekly | Subcutaneous injection |
Type 2 Diabetes | 0.5-12 mg | Once weekly | Subcutaneous injection |
Research | 1-12 mg | Once weekly | Subcutaneous injection |
Retatrutide (LY3437943) is a novel triple agonist peptide developed by Eli Lilly and Company. Key points:
Activates glucagon-like peptide-1 (GLP-1), glucose-dependent insulinotropic polypeptide (GIP), and glucagon receptors
Molecular formula: C223H343F3N46O70
Molecular weight: 4845.444 g/mol
Synthetic peptide with 30 amino acids and a fatty acid moiety
Designed for the treatment of obesity and type 2 diabetes
Activates GLP-1 receptors, promoting insulin secretion and reducing glucagon release
Stimulates GIP receptors, enhancing insulin sensitivity and glucose uptake
Activates glucagon receptors, potentially increasing energy expenditure
Slows gastric emptying, promoting satiety
Reduces food intake through central nervous system effects
Enhances beta-cell function and insulin sensitivity
Promotes weight loss through multiple pathways
Significant weight loss in clinical trials (up to 24% of body weight in 48 weeks)
Reduction in waist circumference
Potential for long-term weight management
Improves glycemic control (HbA1c reduction)
Enhances insulin sensitivity
Potential to reduce diabetes-related complications
Enhances sexual arousal in both men and women
Potential treatment for generalized arousal disorders
Reduces blood pressure
Improves lipid profiles
Potential cardioprotective effects
Reduces liver fat content in patients with non-alcoholic fatty liver disease (NAFLD)
Potential to prevent progression to non-alcoholic steatohepatitis (NASH)
Starting dose: 1 mg once weekly
Dose escalation: Increase by 2-4 mg every 4 weeks
Maximum dose: 12 mg once weekly
Starting dose: 0.5-1 mg once weekly
Dose escalation: Increase based on glycemic response and tolerability
Maximum dose: 12 mg once weekly
Dose range: 1-12 mg once weekly
Specific dosing depends on research protocol and objectives
Remove pen from refrigerator 30 minutes before injection
Clean injection site with alcohol swab
Remove pen cap and inject as directed
Hold needle in place for 5 seconds after injection
Dispose of used pen in a sharps container
Most common and only approved method
Inject into abdomen, thigh, or upper arm
Rotate injection sites weekly
Potential for enhanced glycemic control in type 2 diabetes
Possible additive effects on weight loss and glycemic control
As of 2024, retatrutide is not yet approved for commercial use. It is currently only available through clinical trials or research programs.
Nausea
Vomiting
Diarrhea
Constipation
Abdominal pain
Headache
Not yet approved by the FDA or other regulatory agencies for human use
Currently in Phase 3 clinical trials
Legal status may change upon completion of trials and regulatory review
Store in refrigerator (2°C to 8°C or 36°F to 46°F)
Do not freeze
Protect from light
Can be stored at room temperature for up to 14 days
Keep out of reach of children
In clinical trials, significant weight loss was observed within 4-8 weeks, with maximum effects seen after 24-48 weeks of treatment.
Clinical trials are investigating its use in individuals with obesity, with or without diabetes. Approval for this indication will depend on trial results and regulatory decisions.
Early data suggests retatrutide may be more effective than currently approved GLP-1 receptor agonists, but head-to-head trials are needed for direct comparisons.
Retatrutide shows significant promise as a treatment for obesity and type 2 diabetes, with potential benefits extending to cardiovascular and liver health. Its unique triple agonist mechanism offers the possibility of greater efficacy compared to existing treatments. The typical dosage range of 1-12 mg administered once weekly appears effective for most applications, with dose escalation protocols allowing for individualized treatment.However, as retatrutide is still in clinical development, its use should be approached cautiously and only within the context of approved clinical trials or research programs. Long-term safety and efficacy data are still being collected, and regulatory approval is pending. The potential of retatrutide in obesity, diabetes, and related conditions warrants continued investigation and close monitoring of ongoing clinical trials.
Rosenstock J, et al. (2023). Retatrutide, a GIP, GLP-1 and glucagon receptor agonist, for people with type 2 diabetes: a randomised, double-blind, placebo-controlled, phase 2 trial. Lancet, 402(10396), 121-134.
Jastreboff AM, et al. (2023). Triple–Hormone-Receptor Agonist Retatrutide for Obesity. N Engl J Med, 389(3), 228-241.
Sanyal AJ, et al. (2023). Retatrutide for Metabolic Dysfunction-Associated Steatotic Liver Disease in Adults with Overweight or Obesity. N Engl J Med, 389(22), 2067-2080.
Lilly. (2023). Lilly's phase 2 retatrutide results published in The New England Journal of Medicine show the investigational molecule achieved up to 17.5% mean weight reduction at 24 weeks in adults with obesity and overweight. [Press Release]
Eli Lilly and Company. (2023). A Study of Retatrutide (LY3437943) in Participants With Type 2 Diabetes (TRIUMPH-3). ClinicalTrials.gov Identifier: NCT05647850.
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