Metreleptin
Also known as: A-100, Myalept, Myalepta, r-metHuLeptin, r-metLeptin, Recombinant human leptin, recombinant methionyl human leptin
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Summary
Recombinant human leptin (metreleptin) administered subcutaneously for treatment of generalized lipodystrophy and congenital leptin deficiency to improve metabolic control.
Mechanism of Action
Binds leptin receptor (LEPR) activating JAK-STAT signaling, reducing appetite and modulating energy homeostasis, improving insulin sensitivity and lipid metabolism.
Routes of Administration
Goals & Uses
- Improvement of hyperglycemia and insulin resistanceMetabolic / EndocrineHigh
- Treatment of partial lipodystrophy metabolic complicationsMetabolicLow
- Reduce hypertriglyceridemiaMetabolicHigh
- Control appetite/weightWeight ManagementModerate
- Neuroendocrine restoration in hypothalamic amenorrheaReproductive EndocrinologyLow
- Reduction of hypertriglyceridemia in lipodystrophyMetabolicHigh
- Reduction of hepatic steatosisMetabolicModerate
- Decrease hepatic steatosisMetabolicModerate
- Improve glycemic controlMetabolicHigh
- Appetite and weight regulation in leptin deficiencyWeight ManagementModerate
Contraindications
- General obesity without lipodystrophyOff Label Use RiskHigh
- Active, uncontrolled infectionInfectionModerate
- Hypersensitivity to metreleptin or excipientsAllergyHigh
- Known hypersensitivity to metreleptin or excipientsAllergy / ImmunologicHigh
Adverse Effects
- Anti‑leptin antibodiesImmunologicUncommon
- HypoglycemiaMetabolicCommonAbnormally low blood glucose
- Injection site reactionsLocalCommon
- HeadacheNeurologicCommonPain in the head or upper neck
- Anti-metreleptin antibodies with neutralizing activityImmunologicUncommon
- NauseaGastrointestinalCommonFeeling of sickness or urge to vomit
- Lymphoma (rare)OncologicRare
- Abdominal pain / nauseaGastrointestinalUncommon
- LymphomaOncologyRare
Drug Interactions
- InsulinModerateMay increase risk of low blood sugar
- Immunosuppressants (e.g., cyclosporine)Low
- Oral antidiabetic agents (e.g., sulfonylureas)Moderate
- Warfarin and other narrow therapeutic index drugs metabolized by CYP450Low
- SulfonylureasModerateMay increase risk of low blood sugar
Population Constraints
- PregnancyReproductive SafetyRelative
- Renal impairmentOrgan ImpairmentRelative
- Pediatric patients < 2 yearsAgeRelative
- Pediatric <2 yearsAgeAbsolute
- Patients with history of lymphomaOncologicRelative
- Severe renal impairment (eGFR <30 mL/min)RenalRelative
Regulatory Status
- European UnionApprovedApproved: Generalized lipodystrophy, Congenital leptin deficiencyMarketed as Myalept.
- United StatesApprovedApproved: Generalized lipodystrophy, Congenital leptin deficiencyOrphan drug; dosage 0.06–0.12 mg/kg daily subcutaneously.
- United KingdomApprovedApproved: Generalized lipodystrophy, Congenital leptin deficiencySame as EU approval.
FDA approved (2014) for generalized lipodystrophy and leptin deficiency; granted orphan drug status. Approved in EU (2015) under trade name Myalept.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Metreleptin?
Recombinant human leptin (metreleptin) administered subcutaneously for treatment of generalized lipodystrophy and congenital leptin deficiency to improve metabolic control.
What is Metreleptin used for?
Metreleptin is educationally associated with: Improvement of hyperglycemia and insulin resistance, Treatment of partial lipodystrophy metabolic complications, Reduce hypertriglyceridemia, Control appetite/weight, Neuroendocrine restoration in hypothalamic amenorrhea, Reduction of hypertriglyceridemia in lipodystrophy, Reduction of hepatic steatosis, Decrease hepatic steatosis, Improve glycemic control, Appetite and weight regulation in leptin deficiency. Educational only — not medical advice.
How is Metreleptin administered?
Recorded routes of administration: Subcutaneous.
What are the potential side effects of Metreleptin?
Reported adverse effects include: Anti‑leptin antibodies, Hypoglycemia, Injection site reactions, Headache, Anti-metreleptin antibodies with neutralizing activity, Nausea, Lymphoma (rare), Abdominal pain / nausea, Lymphoma. This list is not exhaustive — consult a qualified clinician.
Who should avoid Metreleptin?
Recorded contraindications: General obesity without lipodystrophy, Active, uncontrolled infection, Hypersensitivity to metreleptin or excipients, Known hypersensitivity to metreleptin or excipients. Consult a qualified clinician before use.