metreleptin (Rx)

Brand and Other Names:Myalept
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

lyophylized powder for reconstitution

  • 11.3mg (5mg/mL when reconstituted with 2.2 mL water for injection)

Lipodystrophy

Indicated as replacement therapy (in addition to diet) for the complications of leptin deficiency in patients with congenital generalized or acquired generalized lipodystrophy

Administer by SC injection once daily at the same time each day

≤40 kg (males or females)

  • Initial daily dose: 0.06 mg/kg (0.012 mL/kg) SC
  • Dose adjustments: 0.02 mg/kg (0.004 mL/kg)
  • Maximum daily dose: 0.13 mg/kg (0.026 mL/kg)

Males >40 kg

  • Initial daily dose: 2.5 mg (0.5 mL) SC
  • Dose adjustments: 1.25-2.5 mg (0.25-0.5 mL)
  • Maximum daily dose: 10 mg (2 mL)

Females >40 kg

  • Initial daily dose: 5 mg (1 mL) SC
  • Dose adjustments: 1.25-2.5 mg (0.25-0.5 mL)
  • Maximum daily dose: 10 mg (2 mL)

Dosage Modifications

Coadministration with insulin or insulin secretagogue (eg, sulfonylurea, meglitinide derivatives): Dosage adjustments, including possible large reductions, of insulin or insulin secretagogue may be necessary in some patients to minimize the risk of hypoglycemia

Dosing Considerations

Safety and efficacy not established for

  • Treatment of complications of partial lipodystrophy
  • Treatment of liver disease, including nonalcoholic steatohepatitis (NASH)
  • HIV-related lipodystrophy
  • Use in patients with metabolic disease, including diabetes mellitus and hypertriglyceridemia, without concurrent evidence of generalized lipodystrophy

Discontinuing due to pancreatitis risk

  • When discontinuing therapy in patients with risk factors for pancreatitis (eg, history of pancreatitis, severe hypertriglyceridemia), taper the dose over a 1-week period
  • During tapering, monitor triglyceride levels and consider initiating or adjusting the dose of lipid-lowering medications as needed
  • Signs and/or symptoms consistent with pancreatitis should prompt an appropriate clinical evaluation

Dosage Forms & Strengths

lyophylized powder for reconstitution

  • 11.3mg (5mg/mL when reconstituted with 2.2 mL water for injection)

Lipodystrophy

Indicated as replacement therapy (in addition to diet) for the complications of leptin deficiency in patients with congenital generalized or acquired generalized lipodystrophy

Administer by SC injection once daily at the same time each day

≤40 kg (males or females)

  • Initial daily dose: 0.06 mg/kg (0.012 mL/kg) SC
  • Dose adjustments: 0.02 mg/kg (0.004 mL/kg)
  • Maximum daily dose: 0.13 mg/kg (0.026 mL/kg)

Males >40 kg

  • Initial daily dose: 2.5 mg (0.5 mL) SC
  • Dose adjustments: 1.25-2.5 mg (0.25-0.5 mL)
  • Maximum daily dose: 10 mg (2 mL)

Females >40 kg

  • Initial daily dose: 5 mg (1 mL) SC
  • Dose adjustments: 1.25-2.5 mg (0.25-0.5 mL)
  • Maximum daily dose: 10 mg (2 mL)

Dosage Modifications

Coadministration with insulin or insulin secretagogue (eg, sulfonylurea, meglitinide derivatives): Dosage adjustments, including possible large reductions, of insulin or insulin secretagogue may be necessary in some patients to minimize the risk of hypoglycemia

Dosing Considerations

Safety and efficacy not established for

  • Treatment of complications of partial lipodystrophy
  • Treatment of liver disease, including nonalcoholic steatohepatitis (NASH)
  • HIV-related lipodystrophy
  • Use in patients with metabolic disease, including diabetes mellitus and hypertriglyceridemia, without concurrent evidence of generalized lipodystrophy

Discontinuing due to pancreatitis risk

  • When discontinuing therapy in patients with risk factors for pancreatitis (eg, history of pancreatitis, severe hypertriglyceridemia), taper the dose over a 1-week period
  • During tapering, monitor triglyceride levels and consider initiating or adjusting the dose of lipid-lowering medications as needed
  • Signs and/or symptoms consistent with pancreatitis should prompt an appropriate clinical evaluation
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Interactions

Interaction Checker

and metreleptin

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      Serious - Use Alternative

        Significant - Monitor Closely

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            Contraindicated (0)

              Serious - Use Alternative (0)

                Monitor Closely (15)

                • chlorpropamide

                  chlorpropamide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • glimepiride

                  glimepiride, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • glipizide

                  glipizide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • glyburide

                  glyburide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin aspart

                  insulin aspart, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin detemir

                  insulin detemir, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin glargine

                  insulin glargine, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin glulisine

                  insulin glulisine, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin lispro

                  insulin lispro, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin NPH

                  insulin NPH, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • insulin regular human

                  insulin regular human, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • nateglinide

                  nateglinide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • repaglinide

                  repaglinide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • tolazamide

                  tolazamide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                • tolbutamide

                  tolbutamide, metreleptin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Coadministration of metreleptin with insulin and/or insulin secretagogues (eg, sulfonylureas, meglitinide derivatives) may increase risk for hypoglycemia; may require lower dose of insulin or insulin secretagogue.

                Minor (0)

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                  Adverse Effects

                  >10%

                  Headache (13%)

                  Hypoglycemia (13%)

                  Decreased weight (13%)

                  1-10%

                  Abdominal pain (10%)

                  Arthralgia (8%)

                  Dizziness (8%)

                  Ear infection (8%)

                  Fatigue (8%)

                  Nausea (8%)

                  Ovarian cyst (8%)

                  Upper respiratory tract infection (8%)

                  Anemia (6%)

                  Back pain (6%)

                  Diarrhea (6%)

                  Paresthesia (6%)

                  Proteinuria (6%)

                  Pyrexia (6%)

                  Antibodies with neutralizing activity (6%)

                  Injection site erythema and urticaria (4%)

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                  Warnings

                  Black Box Warnings

                  Neutralizing antibodies

                  • Antimetreleptin antibodies with neutralizing activity have been identified in patients treated with metreleptin
                  • The consequences of these neutralizing antibodies are not well characterized but could include inhibition of endogenous leptin action and/or loss of efficacy
                  • Severe infection and/or worsening metabolic control reported
                  • Test for antimetreleptin antibodies with neutralizing activity in patients who develop severe infections or show signs suspicious for loss of efficacy during treatment

                  Lymphoma

                  • T-cell lymphoma has been reported in patients with acquired generalized lipodystrophy, both treated and not treated with metreleptin
                  • Carefully consider the benefits and risks of treatment in patients with significant hematologic abnormalities and/or acquired generalized lipodystrophy

                  Myalept Risk Evaluation and Mitigation Strategy (REMS) Program

                  • Because of the risk for autoantibodies and lymphoma, prescribers must be certified with the Myalept REMS Program by enrolling in and completing training
                  • Pharmacies must be certified with the program and only dispense metreleptin after receipt of the REMS prescription authorization form for each new prescription

                  Contraindications

                  Hypersensitivity, including urticaria and generalized rash

                  General obesity not associated with congenital leptin deficiency; has not been shown to be effective in treating general obesity, and the development of antimetreleptin antibodies with neutralizing activity has been reported in obese patients treated with metreleptin

                  Cautions

                  For SC injection only; instruct patients and caregivers on the proper SC injection technique (see Administration)

                  Neutralizing antibody activity to leptin and/or metreleptin may develop, which could result in severe infections or loss of treatment effectiveness (see Black Box Warnings)

                  T-cell lymphoma reported in patients with acquired generalized lipodystrophy, both treated and not treated with metreleptin (see Black Box Warnings)

                  Dosage adjustments, including possible large reductions, of insulin or insulin secretagogue (eg, sulfonylurea, meglitinide derivatives) may be necessary in some patients to minimize the risk of hypoglycemia (see Dosage Modifications)

                  Hypersensitivity reported; promptly discontinue if hypersensitivity occurs

                  Benzoyl alcohol

                  • Contains benzyl alcohol when reconstituted with bacteriostatic water for injection
                  • Reconstitute with preservative-free water for injection when used in neonates and infants
                  • Benzoyl alcohol doses >99 mg/kg/day in neonates and low-birth-weight infants is associated with gasping syndrome
                  • Gasping syndrome is characterized by CNS depression, metabolic acidosis, gasping respirations, and high levels of benzyl alcohol and its metabolites found in the blood and urine

                  Autoimmunity

                  • Leptin plays a role in immune system homeostasis
                  • Acquired lipodystrophies are associated with autoimmune disorders (eg, autoimmune hepatitis, membranoproliferative glomerulonephritis)
                  • Cases of progression of autoimmune hepatitis and membranoproliferative glomerulonephritis (associated with massive proteinuria and renal failure) were observed in some patients with acquired generalized lipodystrophy treated with metreleptin
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                  Pregnancy & Lactation

                  Pregnancy

                  A program monitors outcomes in women exposed to MYALEPT during pregnancy; women who become pregnant during MYALEPT treatment are encouraged to enroll; patients or their physicians should call 1-855-669-2537 to enroll

                  Available pharmacovigilance reports in pregnant women are insufficient to evaluate for any drug-associated risk for major birth defects, miscarriage, or adverse maternal or fetal outcomes; these reports describe similar adverse pregnancy outcomes as those documented in women with lipodystrophy

                  Drug contains benzyl alcohol when reconstituted with BWFI; it contains no preservative when reconstituted with WFI; because benzyl alcohol is rapidly metabolized by a pregnant woman, benzyl alcohol exposure in the fetus is unlikely; however, adverse reactions have occurred in premature neonates and low birth weight infants who received intravenously administered benzyl alcohol-containing drugs; if therapy is needed during pregnancy, consider using preservative-free WFI when reconstituting

                  Lipodystrophy in pregnancy can result in an increased rate of gestational diabetes, macrosomia, eclampsia, intrauterine growth retardation, intrauterine death, and miscarriage

                  Effects on labor and delivery in pregnant women are unknown; in a published in vitro study of human myometrial tissue exposed to a recombinant leptin, human uterine contractility was inhibited; in animal studies, prolonged gestation and dystocia were observed

                  Animal data

                  • In an animal reproduction study, no adverse developmental effects were observed with subcutaneous administration of drug to pregnant mice during organogenesis at doses 7-and 15-fold maximum recommended clinical dose, based on body surface area of a 20-and 60-kg patient, respectively
                  • In a pre-and postnatal development study in mice, subcutaneous administration caused prolonged gestation and dystocia resulting in maternal death during parturition and lower survival of offspring in immediate postnatal period at doses starting approximately at maximum recommended clinical dose

                  Lactation

                  There are no available data on presence of drug in human milk; however, endogenous leptin is present in human milk; there are no available data on effects of drug on breastfed infant or effects on milk production

                  Developmental and health benefits of breastfeeding should be considered along with mother’s clinical need for therapy and any potential adverse effects on breastfed child from drug or from underlying maternal condition

                  Pregnancy Categories

                  A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

                  B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

                  C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

                  D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

                  X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

                  NA: Information not available.

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                  Pharmacology

                  Mechanism of Action

                  Recombinant analog of the human hormone leptin; binds to and activates the human leptin receptor (ObR), which belongs to the class I cytokine family of receptors that signals through the JAK/STAT transduction pathway

                  Deficiency of adipose tissue leads to hypertriglyceridemia and ectopic deposition of fat in nonadipose tissues (eg, liver, muscle), contributing to metabolic abnormalities including insulin resistance

                  Native leptin is a hormone predominantly secreted by adipose tissue that informs the CNS of the status of energy stores in the body; in patients with generalized lipodystrophy, leptin deficiency, resulting from the loss of adipose tissue, contributes to excess caloric intake, which exacerbates the metabolic abnormalities

                  Absorption

                  Peak plasma time: 4-4.3 hr

                  Distribution

                  Vd: 370, 398, and 463 mL/kg for 0.3, 1, and 3 mg/kg/day doses, respectively

                  Metabolism

                  No formal metabolism studies have been conducted

                  Nonclinical data indicate renal clearance is the major route of metreleptin elimination, with no apparent contribution of systemic metabolism or degradation

                  Elimination

                  Half-life: 3.8-4.7 hr

                  Clearance delayed in presence of leptin antibodies

                  Excretion: Predominantly renal

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                  Administration

                  SC Preparation

                  Remove the vial from the refrigerator and allow vial to warm to room temperature prior to use

                  Do not use if the white lyophilized cake is discolored

                  Reconstitute aseptically with 2.2 mL of sterile bacteriostatic water for injection (BWFI) USP (0.9% benzyl alcohol) or 2.2 mL of sterile water for injection (WFI)

                  For use in neonates and infants, reconstitute with preservative-free sterile WFI (see Cautions)

                  Slowly inject diluent down the side of the vial; it is normal for some bubbles to form

                  Gently swirl the contents to reconstitute; do not shake or vigorously agitate

                  When properly mixed, the reconstituted solution should be clear and free of clumps or dry powder, bubbles, or foam

                  After reconstitution, the mixture should be clear and colorless; do not use if visible particulates are present in the solution

                  After reconstitution, the vials should not be frozen (below 0°C) or shaken vigorously; if the reconstituted product is inadvertently frozen, it should be thrown away

                  SC Administration

                  Instruct patients and caregivers on the proper SC injection technique with care to avoid IM injection in patients with minimal subcutaneous adipose tissue

                  Never administer IV or IM

                  Do not mix with insulin; use a separate syringe for each medication

                  If metreleptin and insulin are administered at the same time of day, they may be injected in the same body area using 2 different injection sites

                  Can be administered without regard to the timing of meals

                  If a dose is missed, administer the dose as soon as noticed, and resume the normal dosing schedule the next day

                  SC injection technique

                  • Using a 1-mL syringe with a needle appropriate for SC injection, withdraw the prescribed dose of metreleptin reconstituted solution
                  • Remove any large air pockets or large bubbles from the filled syringe prior to administration; some small bubbles may remain in the syringe
                  • Administer into the SC tissue of the abdomen, thigh, or upper arm
                  • Advise patients to use a different injection site each day when injecting in the same region
                  • After choosing an injection site, pinch the skin and at a 45° angle, inject SC
                  • Avoid IM injection, especially in patients with minimal subcutaneous adipose tissue
                  • Doses exceeding 1 mL can be administered as 2 injections (the total daily dose divided equally) to minimize potential injection-site discomfort due to injection volume
                  • When dividing doses due to volume, doses can be administered one after the other

                  Storage

                  Unopened vials

                  • Store refrigerated between 2-8°C (36-46°F) in original carton
                  • Do not freeze

                  Reconstituted vials

                  • Reconstituted with water for injection (no preservatives): Use for a single dose and should be administered immediately; unused reconstituted solution cannot be saved for later use and should be discarded
                  • Reconstituted with bacteriostatic water for injection: Can be used for multiple doses within 3 days when refrigerated at 2-8°C (36-46°F) and protected from light; do not freeze
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                  Images

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                  Patient Handout

                  Patient Education
                  metreleptin subcutaneous

                  NO MONOGRAPH AVAILABLE AT THIS TIME

                  USES: Consult your pharmacist.

                  HOW TO USE: Consult your pharmacist.

                  SIDE EFFECTS: Consult your pharmacist.In the US -Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088 or at www.fda.gov/medwatch.In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

                  PRECAUTIONS: Consult your pharmacist.

                  DRUG INTERACTIONS: Consult your pharmacist.Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

                  OVERDOSE: If someone has overdosed and has serious symptoms such as passing out or trouble breathing, call 911. Otherwise, call a poison control center right away. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

                  NOTES: No monograph available at this time.

                  MISSED DOSE: Consult your pharmacist.

                  STORAGE: Consult your pharmacist.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

                  Information last revised July 2016. Copyright(c) 2021 First Databank, Inc.

                  IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

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                  Formulary

                  FormularyPatient Discounts

                  Adding plans allows you to compare formulary status to other drugs in the same class.

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                  Adding plans allows you to:

                  • View the formulary and any restrictions for each plan.
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                  • Compare formulary status to other drugs in the same class.
                  • Access your plan list on any device – mobile or desktop.

                  The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

                  Tier Description
                  1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
                  2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
                  3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
                  4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
                  NC NOT COVERED – Drugs that are not covered by the plan.
                  Code Definition
                  PA Prior Authorization
                  Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
                  QL Quantity Limits
                  Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
                  ST Step Therapy
                  Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
                  OR Other Restrictions
                  Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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                  Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.