metreleptin

Adult Dosing

Lipodystrophy

40 kg (males and females): 0.06 mg/kg IV Daily. Dose can be adjusted at 0.02 mg/kg IV. Max: 0.13 mg/kg
>40 kg (males): 2.5 mg IV Daily. Dose can be adjusted up or down by 1.25 mg to 2.5 mg IV Daily. Max: 10 mg (2 mL)
>40 kg (females): 5 mg IV Daily. Dose can be adjusted up or down by 1.25 mg to 2.5 mg IV Daily. Max: 10 mg

Note:

Refer package insert for preparation and reconstitution procedure
Dose adjustment is necessary in some patients to minimize the risk of hypoglycemia
When discontinuing therapy in patients with risk factors for pancreatitis tapering of the dose over a one week period is recommended

Pediatric Dosing

Lipodystrophy

40 kg (males and females): 0.06 mg/kg (0.012 mL/kg) IV qd. Dose can be adjusted at 0.02 mg/kg (0.004 mL/kg) IV. Max: 0.13 mg/kg (0.0026 mL/kg)
>40 kg (males): 2.5 mg (0.5 mL) IV qd. Dose can be adjusted at 1.25 mg (0.25 mL) to 2.5 mg (0.5 mL) IV. Max: 10 mg (2 mL)
>40 kg (females): 5 mg (1 mL) IV qd. Dose can be adjusted at 1.25 mg (0.25 mL) to 2.5 mg (0.5 mL) IV. Max: 10 mg (2 mL)

Note:

Refer package insert for preparation and reconstitution procedure
Dose adjustment is necessary in some patients to minimize the risk of hypoglycemia
When discontinuing therapy in patients with risk factors for pancreatitis tapering of the dose over a one week period is recommended

[Outline]

Adult Dosing
Pediatric Dosing

Indications ⬆ ⬇

Adjunct to diet as replacement therapy to treat the complications of leptin deficiency in patients with congenital or acquired generalized lipodystrophy

Contraindications ⬆ ⬇

Hypersensitivity to any of the ingredients of the product
General obesity not associated with congenital leptin deficiency

Black Box Warnings ⬆ ⬇

Anti-metreleptin antibodies with neutralizing activity have been identified in patients treated with metreleptin, resulting in inhibition of endogenous leptin action and/or loss of metreleptin efficacy
Severe infection and/or worsening metabolic control have been reported. Consider evalution for anti-metreleptin antibodies with neutralizing activity in patients who develop severe infections or show signs suspicious for loss of metreleptin efficacy during treatment. Contact Bristol Myers-Squibb at 1866-216-1526 for neutralizing antibody testing
T-cell lymphoma has been occurred in patients with acquired generalized lipodystrophy, both treated and not treated with metreleptin. Consider the benefits and risks of treatment with metreleptin in patients with significant hematologic abnormalities and/or acquired generalized lipodystrophy
Due to risks associated with the development of anti-metrelept antibodies that neutralize endogenous leptin and/or metreleptin and the risk for lymphoma, MYALEPT is available only through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called the MYALEPT REMS PROGRAM

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Renal impairment: No dose adjustments

Hepatic Dose Adjustment

Hepatic impairment: No dose adjustments

Warnings/Precautions ⬆ ⬇

See Supplemental Patient Information

Anti-metreleptin antibodies with neutralizing activity have been identified in patients treated with metreleptin, resulting in inhibition of endogenous leptin action and/or loss of metreleptin efficacy. Test for neutralizing antibodies in patients with severe infections or loss of efficacy during metreleptin treatment
T-cell lymphoma has been occurred in patients with acquired generalized lipodystrophy, both treated and not treated with metreleptin. Consider the benefits and risks of treatment with metreleptin in patients with significant hematologic abnormalities and/or acquired generalized lipodystrophy
Adjust dose, including possible large reductions, of insulin or insulin secretagogue may be necessary in some patients to minimize the risk of hypoglycemia. Closely monitor blood glucose in patients on concomitant insulin therapy, especially those on high doses, or insulin secretagogue, when treating with metreleptin
Autoimmune disorder progression has been observed in patients treated with metreleptin. Carefully consider the benefits and risks of metreleptin treatment in patients with autoimmune disease
Hypersensitivity reactions, including urticaria or generalized rash have been reported. Patient should promptly seek medical advice regarding suspected reactions
Therapy contains benzyl alcohol when reconstituted with BWFI. Preservative-free WFI is recommended for use in neonates and infants
The safety and effectiveness of metreleptin for the treatment of liver disease, including nonalcoholic steatohepatitis (NASH), have not been established
Metreleptin is not indicated for use in patients with HIV-related lipodystrophy or in patients with metabolic disease, without concurrent evidence of generalized lipodystrophy

Supplemental Patient Information

Be sure and obtain and review the metreleptin for injection Medication Guide

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category:C

Breastfeeding: Safety unknown: Because of the potential for serious adverse reactions in a nursing infants from metreleptin a decision should be made whether to discontinue nursing or discontinue the drug, taking into account importance of drug to the mother

Adverse Reactions ⬆ ⬇

CNS: Headache, dizziness, paresthesia
GI: Abdominal pain. nausea, diarrhea
METABOLIC: Hypoglycemia, decreased weight
MUSC: Arthralgia, back pain
EENT: Ear infection
MISC: Fatigue, pyrexia
GU: Ovarian cyst, proteinuria
RESP: Upper respiratory tract infection
HEMA: Anemia

Clinical Pharmacology ⬆ ⬇

Metabolic agent; recombinant analog of the human hormone leptin; a neurohormone secreted by fat cells that regulates energy metabolism and body weight
Metabolism: Unknown
Excretion: Unknown
Half-life: 3.8-4.7 hours

Brands and Availability ⬆ ⬇