Macimorelin acetate

What is Macimorelin acetate?

• Macimorelin acetate (MACRILEN) is a growth hormone (GH) secretagogue receptor agonist used for the diagnosis of adult growth hormone deficiency.

What are the uses of this medicine?

• This medicine is used for the diagnosis of adult growth hormone deficiency.

How does this medicine work?

• Macimorelin stimulates GH release by activating growth hormone secretagogue receptors present in the pituitary and hypothalamus.

Who Should Not Use this medicine ?

• This medcine have no usage limitations.

What drug interactions can this medicine cause?

Avoid concomitant use of MACRILEN with drugs that prolong the QT interval (such as antipsychotic medications (e.g., chlorpromazine, haloperidol, thioridazine, ziprasidone), antibiotics (e.g., moxifloxacin), Class 1A (e.g., quinidine, procainamide) and Class III (e.g., amiodarone, sotalol) antiarrhythmic medications or any other medications known to prolong the QT interval). Co-administration of a strong CYP3A4 inducer with MACRILEN (e.g., carbamazepine, enzalutamide, mitotane, phenytoin, rifampin, St. John's wort, bosentan, efavirenz, etravirine, modafinil, armodafinil, rufinamide) is not recommended. Avoid concomitant use of MACRILEN with the following: Drugs that directly affect the pituitary secretion of growth hormone (such as somatostatin, insulin, glucocorticoids, and cyclooxygenase inhibitors such as aspirin or indomethacin). Drugs that may transiently elevate growth hormone concentrations (such as clonidine, levodopa, and insulin). Drugs that may blunt the growth hormone response to MACRILEN (such as muscarinic antagonists: atropine, anti-thyroid medication: propylthiouracil, and growth hormone products).

Is this medicine FDA approved?

• It was approved for use in the United States in 2017.

How should this medicine be used?

• Discontinue therapy with strong CYP3A4 inducers, growth hormones and drugs that affect GH release for an adequate length of time before administering MACRILEN.
• Adequately replace other hormone deficiencies before administering MACRILEN.

Recommended Dosage

• The recommended dose is a single oral dose of 0.5 mg/kg of macimorelin.
• The dose is administered as a reconstituted solution.

Preparation

• Weigh the patient in kilograms (i.e., kg).
• Determine the number of MACRILEN pouches needed to prepare the dose:
• For a patient weighing up to 120 kg, use 1 pouch.
• For a patient weighing more than 120 kg, use 2 pouches.
• Use a glass or transparent plastic container with graduation in milliliters (i.e., mL) to dissolve the entire contents of the pouch(es) in the appropriate volume of water.
• For 1 pouch dissolve in 120 mL of water (corresponds to 60 mg/120 mL).
• For 2 pouches dissolve in 240 mL of water (corresponds to 120 mg/240 mL).
• Stir the MACRILEN solution gently for about 2 to 3 minutes (a small amount of un-dissolved particles will remain). The solution will have a final concentration of 0.5 mg/mL.
• Use the MACRILEN solution within 30 minutes after preparation.
• Discard any unused MACRILEN solution.
• Determine the recommended dose to be administered by multiplying the patient weight in kilogram by 0.5 mg/kg.
• For example, a 70 kg patient will need a 35 mg dose.

• Determine the volume of prepared MACRILEN solution to be administered by dividing the recommended dose by 0.5 mg/mL.
• For example, a patient requiring a dose of 35 mg will need 70 mL of reconstituted MACRILEN solution.
• Use a syringe (without a needle) with graduations in mL to measure the exact volume of MACRILEN solution to be administered and transfer the required volume of MACRILEN solution into a drinking glass.

Administration

• Have the patient being tested drink the entire volume of MACRILEN solution in the drinking glass (i.e., the dose) within 30 seconds.
• Observe the patient being tested per routine for the duration of the test.
• Draw venous blood samples for GH determination at 30 minutes, 45 minutes, 60 minutes and 90 minutes after administration of MACRILEN.
• Prepare serum samples and send to a laboratory for growth hormone determinations.
• Maximally stimulated serum GH level of less than 2.8 ng/mL (i.e., at the 30, 45, 60 and 90 minute timepoints) following MACRILEN administration confirms the presence of adult growth hormone deficiency.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As oral solution: 60 mg

This medicine is available in fallowing brand namesː

• MACRILEN

What side effects can this medication cause?

The most common side effects of this medicine include:

• dysgeusia
• dizziness
• headache
• fatigue
• nausea
• hunger
• diarrhea
• upper respiratory tract infection
• feeling hot
• hyperhidrosis
• nasopharyngitis
• sinus bradycardia

What special precautions should I follow?

• MACRILEN causes an increase of about 11 msec in the corrected QT (QTc) interval. QT prolongation can lead to development of torsade de pointes-type ventricular tachycardia. Avoid the concomitant use of MACRILEN with drugs that are known to prolong QT interval.
• Concomitant use of strong CYP3A4 inducers with MACRILEN can decrease macimorelin plasma levels significantly and thereby lead to a false positive result. Discontinue and washout strong CYP3A4 inducers before testing.
• Adult growth hormone (GH) deficiency caused by a hypothalamic lesion may not be detected early in the disease process. Consider repeat testing if indicated.

What to do in case of emergency/overdose?

• In the event of an overdose, symptomatic and supportive measures should be employed.

Can this medicine be used in pregnancy?

• There are no available data with MACRILEN use in pregnant women to inform a drug associated risk for adverse developmental outcomes.

Can this medicine be used in children?

• The safety and efficacy of MACRILEN in pediatric patients have not been established.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• MACIMORELIN

Inactive ingredients:

• Lactose Monohydrate
• CROSPOVIDONE, UNSPECIFIED
• Silicon Dioxide
• Sodium Stearyl Fumarate
• Saccharin Sodium

Who manufactures and distributes this medicine?

• Packager: Strongbridge U.S. Inc

What should I know about storage and disposal of this medication?

• Store pouches under refrigeration at 2-8°C (36-46°F).
• The solution must be used within 30 minutes after preparation.
• Discard unused portion.

• Dailymed label info on Macimorelin acetate
• FDA Macimorelin acetate

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