Metreleptin

Products

Metreleptin was approved in the United States in 2014 as an injectable (Myalept). The drug is not currently registered in many countries.

Structure and properties

Metreleptin is a recombinant human leptin analog derived from E. coli using biotechnological methods. It differs from natural leptin in having an additional methionine at the N terminus. Metreleptin is an unglycosylated polypeptide of 147 amino acids with a disulfide bridge between Cys-97 and Cys-147 and a molecular weight of approximately 16.15 kDa.

Effects

Metreleptin is a derivative of the hormone leptin, which is produced by fat cells and exerts an appetite-suppressing effect in the central nervous system. In lipodystrophy, the lack of leptin contributes to increased caloric intake and metabolic disturbances. Metreleptin promotes sensitivity to insulin and reduces food intake. The half-life is approximately four hours.

Indications

For the treatment of complications of leptin deficiency in patients with congenital or acquired generalized lipodystrophy. Metreleptin has not yet been approved for the treatment of diabetes mellitus.

Dosage

According to the SmPC. The drug is injected subcutaneously.

Contraindications

Metreleptin is contraindicated in hypersensitivity and in overweight or obesity without lipodystrophy. For complete precautions, see the drug label.

Interactions

Metreleptin may affect CYP450 formation and cause corresponding drug-drug interactions.

Adverse effects

The most common potential adverse effects include headache, hypoglycemia, weight loss, and abdominal pain. Metreleptin may lead to the formation of antibodies to leptin.