Metreleptin Brand Name– MYALEPT
What is Metreleptin
Metreleptin is a recombinant human leptin analog approved as an adjunct to diet as replacement therapy to treat the complications of leptin deficiency in patients with congenital or acquired generalized lipodystrophy.
It is not approved for the treatment of complications of partial lipodystrophy or HIV-related lipodystrophy.
Metreleptin is produced in E. coli and contains an additional methionine residue at its amino terminus, making it slightly different than native human leptin.
Lipodystrophies are acquired or inherited disorders characterized by the selective loss of adipose tissue. Affected patients are predisposed to insulin resistance, including diabetes mellitus, dyslipidemia, hypertriglyceridemia, and hepatic steatosis.
The hormone leptin has a central role in energy homeostasis; serum leptin levels are proportional to adipocyte mass.
In an open-label, single-arm study of 48 patients (median age = 15 years; range, 1—68 years), metreleptin treatment resulted in reductions in HbA1c, fasting glucose, and triglycerides from baseline values.
At 12 months, patients receiving metreleptin (n = 35) had a mean decrease of 2% from their mean baseline HbA1c of 8.7%. The mean baseline fasting glucose (n = 37) was 174 mg/dl, and the mean reduction was 49 mg/dl.
The median baseline fasting triglycerides (n = 36) was 348 mg/dl, which decreased by a median of 185 mg/dl.
The weighted average daily dose for patients weighing > 40 kg was 2.6 mg/day SC for males and 4.6 mg/day for females during the first year of therapy and 3.2 mg/day (males) and 6.3 mg (females) over the entire study period.
The median treatment duration was 2.7 years (range, 3.6 months—10.9 years). Due to the risk of anti-metreleptin antibodies with neutralizing activity and the possible increased risk of lymphoma, metreleptin is available only through a restricted program called the Myalept REMS Program.
The FDA approved metreleptin in February 2014.
- generalized lipodystrophy
General dosing information:
- Limitations of use: Metreleptin is not approved for the treatment of complications of partial lipodystrophy; for the treatment of liver disease, including nonalcoholic steatohepatitis (NASH); for use in patients with HIV-related lipodystrophy; or in patients with metabolic disease, without concurrent evidence of lipodystrophy (generalized).
- Metreleptin should be administered once daily at the same time every day. It can be administered any time of day without regard to the timing of meals.
- When discontinuing metreleptin therapy in patients with risk factors for pancreatitis, taper the dosage over one week. Monitor triglyceride levels and initiate or adjust lipid-lowering therapy as indicated. Promptly evaluate any patient with signs or symptoms of pancreatitis.
- If a dose is missed, administer the dose as soon as noticed, and resume the normal dosing schedule the next day.
- abdominal pain
- antibody formation
- back pain
- injection site reaction
- new primary malignancy
- renal failure (unspecified)
- weight loss
- blood glucose
- serum triglycerides
- abrupt discontinuation
- anti-metreleptin antibodies
- autoimmune disease
- bone marrow suppression
- diabetes mellitus
- new primary malignancy
- requires an experienced clinician
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