Metreleptin
From PeptidePlaza, the free peptide reference · Entry #1137 · Metabolic · Sources fetched 2026-09-11 · Editorial standards
Metreleptin is a metabolic research peptide. Metreleptin is a leptin receptor agonist and a leptin analog, FDA-approved as an adjunct to diet for treating complications of leptin deficiency in patients with congenital or acquired generalized lipodystrophy.
Metreleptin, marketed as Myalept, functions as a leptin receptor agonist, mimicking the action of endogenous leptin. It is approved by the FDA as a replacement therapy to manage complications arising from leptin deficiency in individuals with congenital or acquired generalized lipodystrophy. The compound is administered subcutaneously. Research has explored its potential in conditions such as partial lipodystrophy, obesity, non-alcoholic fatty liver disease, and metabolic syndrome, though its safety and effectiveness for partial lipodystrophy, liver disease, HIV-related lipodystrophy, or metabolic disease without concurrent generalized lipodystrophy have not been established. The literature frequently discusses lipodystrophy syndromes and the pharmacotherapy of obesity.
1 Mechanism of action
Leptin receptor agonist (agonist)
Primary targets: Leptin receptor
2 Reported effects
Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.
2.1 Indicated / studied for
- Complications of leptin deficiency in congenital generalized lipodystrophy
- Complications of leptin deficiency in acquired generalized lipodystrophy
2.2 Side effects
- Headache
- Hypoglycemia
- Decreased weight
- Abdominal pain
- Arthralgia
- Dizziness
3 Chemical and physical properties
| Purity (typical) | Not independently verified |
|---|---|
| Half-life | ~3.8–4.7 hours |
| Brand names | Myalept |
| Route | SUBCUTANEOUS |
| Storage | −20 °C, lyophilised powder, desiccated |
| Solubility | Sterile water / bacteriostatic water |
| Receptors / targets | Leptin receptor |
4 Research dosages
0.06 mg/kg/day SC once daily, increased or decreased by 0.02 mg/kg to a maximum daily dose of 0.13 mg/kg for body weight 40 kg or less; 2.5 mg/day SC once daily, increased or decreased by 1.25 mg to 2.5 mg/day to a maximum dose of 10 mg/day for males greater than 40 kg body weight; 5 mg/day SC once daily, increased or decreased by 1.25 mg to 2.5 mg/day to a maximum dose of 10 mg/day for females greater than 40 kg body weight
5 Research studies (8)
- Lipodystrophy Syndromes
Endocrinology and metabolism clinics of North America (2016) · Review - Established and emerging treatments for eating disorders
Trends in molecular medicine (2024) · Review - The Diagnosis and Management of Lipodystrophy Syndromes: A Multi-Society Practice Guideline
The Journal of clinical endocrinology and metabolism (2016) · Review - Pharmacotherapy of obesity: an update on the available medications and drugs under investigation
EClinicalMedicine (2023) · Review - Lipodystrophies in Children
Hormone research in paediatrics (2022) · Review - Metreleptin: first global approval
Drugs (2013) · Review - Leptin acutely increases hepatic triglyceride secretion in patients with lipodystrophy
Metabolism: clinical and experimental (2025) · RCT - Berardinelli-Seip syndrome
Endokrynologia Polska (2026) · Case Series
6 Safety and risk profile
6.1 Regulatory status
Metreleptin is currently classified as FDA approved. Approval applies to specific clinical indications and dosing; research-grade material is not the approved product.
6.2 Contraindications
Conditions and populations in which use is contraindicated:
- General obesity not associated with congenital leptin deficiency
- Prior severe hypersensitivity reactions to metreleptin or product components
6.3 Drug interactions
| Drug or class | Interaction | Risk |
|---|---|---|
| CYP450 substrates with narrow therapeutic index (e.g., warfarin, cyclosporine, theophylline) | Potential alteration of CYP450 enzyme formation, requiring therapeutic monitoring and dose adjustment upon initiation or discontinuation of metreleptin. | High |
| Oral contraceptives | Potential alteration of CYP450 enzyme formation. | Moderate |
6.4 Long-term risks
- Anti-metreleptin antibodies with neutralizing activity
- T-cell lymphoma
- Hypoglycemia
- Autoimmunity
- Hypersensitivity
6.5 Research best practices
- Store in the refrigerator at 36°F to 46°F (2°C to 8°C)
- Protect from light
- Keep vials in the carton when not in use
- Do not freeze
7 Frequently asked questions
- What is metreleptin used for?
- Metreleptin is used as a replacement therapy alongside diet to treat complications of leptin deficiency in patients diagnosed with congenital or acquired generalized lipodystrophy. It is not indicated for general obesity or other metabolic diseases without concurrent generalized lipodystrophy.
- How does metreleptin work?
- Metreleptin works as a leptin receptor agonist. It is a leptin analog, meaning it mimics the natural hormone leptin, which plays a role in regulating energy balance and metabolism. By activating leptin receptors, it helps address the complications associated with leptin deficiency.
- Is metreleptin FDA approved?
- Yes, metreleptin was approved by the FDA in 2014. It is available through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) due to potential risks, including the development of anti-metreleptin antibodies and lymphoma.
- What are the side effects of metreleptin?
- Common side effects reported in clinical trials include headache, hypoglycemia, decreased weight, and abdominal pain. Other less common adverse reactions may include arthralgia, dizziness, and fatigue. Patients should be monitored for these and other potential reactions.
- What are the contraindications for metreleptin?
- Metreleptin is contraindicated in patients with general obesity not associated with congenital leptin deficiency, as its effectiveness for general obesity has not been shown. It is also contraindicated in individuals with a known severe hypersensitivity to metreleptin or any of its components.
8 References
- Metreleptin — molecule record ChEMBL. View source
- Metreleptin — FDA approved prescribing information U.S. Food and Drug Administration. View source
- Metreleptin — published literature (250 records) PubMed. View source
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