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ALIMENTARY TRACT AND METABOLISM › OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS › OTHER ALIMENTARY TRACT AND METABOLISM PRODUCTS › Amino acids and derivatives
metreleptin
A16AA07
Forms & Strengths
- Lyophilized powder for injection: 11.3 mg per vial (delivers 9.5 mg/mL after reconstitution)
Adult Dosing
- Weight <= 40 kg: Initial 0.06 mg/kg subcutaneously once daily
- Weight > 40 kg: Initial 2.05 mg subcutaneously once daily
- Maximum dose: 0.13 mg/kg/day for weight <= 40 kg; 5 mg/day for females and 10 mg/day for males > 40 kg
Pediatric Dosing
- Weight <= 40 kg: Initial 0.06 mg/kg subcutaneously once daily
- Weight > 40 kg: Initial 2.05 mg subcutaneously once daily
- Maximum dose: 0.13 mg/kg/day for weight <= 40 kg; 5 mg/day for females and 10 mg/day for males > 40 kg (indicated for pediatric patients aged 2 years and older)
Indications
- As an adjunct to diet as replacement therapy for the treatment of complications of leptin deficiency in patients with congenital or acquired generalized lipodystrophy
Mechanism of Action
- Recombinant analog of human leptin; binds to leptin receptors to regulate energy homeostasis, reducing appetite, decreasing ectopic lipid deposition in liver and muscle, and improving glycemic control and insulin sensitivity
Contraindications
- General obesity not associated with congenital leptin deficiency
- HIV-associated lipodystrophy
- Severe hypersensitivity to metreleptin or its excipients
Adverse Reactions
- Hypoglycemia
- Weight loss
- Headache
- Abdominal pain
- Fatigue
- Injection site reactions
- Development of neutralizing antibodies
- Risk of T-cell lymphoma in patients with acquired generalized lipodystrophy
Drug Interactions
- Substrates of CYP450 enzymes: Leptin alterations may affect CYP450 activities; monitor when coadministered with narrow therapeutic index CYP substrates (e.g., warfarin, phenytoin)
Curated Content: Needs Vetting Before Put to Clinical Use