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Macimorelin

Medically reviewed by Drugs.com. Last updated on Aug 2, 2020.

Pronunciation

(ma si moe REL in)

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Packet, Oral:

Macrilen: 60 mg (1 ea) [contains saccharin sodium]

Brand Names: U.S.

  • Macrilen

Pharmacologic Category

  • Diagnostic Agent
  • Growth Hormone Secretagogue Receptor Agonist

Pharmacology

Stimulates GH release by activating GH secretagogue receptors in the pituitary and hypothalamus.

Metabolism

Hepatic via CYP3A4

Time to Peak

0.5 to 1.5 hours

Half-Life Elimination

4.1 hours

Use: Labeled Indications

Diagnostic use: Growth hormone deficiency: Diagnosis of adult growth hormone deficiency.

Limitations of use: The safety and diagnostic performance has not been established for patients with BMI >40 kg/m2.

Contraindications

There are no contraindications listed in the manufacturer's labeling

Dosing: Adult

Diagnostic use: Growth hormone deficiency: Note: Correct other pituitary hormone deficiencies prior to administration (AACE/ACE [Yuen 2019]): Oral:

BMI ≤40 kg/m2: 0.5 mg/kg as single dose.

BMI >40 kg/m2: Dose has not been established.

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Geriatric

Refer to adult dosing.

Reconstitution

After determining dosage and number of pouches needed, dissolve entire contents of each pouch with 120 mL of water (final concentration equals 0.5 mg/1 mL). Stir solution gently for about 2 to 3 minutes (a small amount of undissolved particles will remain). Transfer volume needed for dose using a syringe (without needle) graduated in mL into a drinking glass.

Administration

Oral: Patient must drink entire dose within 30 seconds after fasting for at least 8 hours.

Storage

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

Drug Interactions

Aspirin: May diminish the diagnostic effect of Macimorelin. Avoid combination

Atropine (Systemic): May diminish the diagnostic effect of Macimorelin. Avoid combination

Bosentan: May diminish the diagnostic effect of Macimorelin. Monitor therapy

CloNIDine: May diminish the diagnostic effect of Macimorelin. Avoid combination

Corticosteroids (Systemic): May diminish the diagnostic effect of Macimorelin. Avoid combination

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May decrease the serum concentration of Macimorelin. Avoid combination

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to concomitant therapy when possible. If concomitant therapy cannot be avoided, monitor for reduced clinical effects of the CYP3A4 substrate. Consider therapy modification

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Efavirenz: May diminish the diagnostic effect of Macimorelin. Monitor therapy

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Etravirine: May diminish the diagnostic effect of Macimorelin. Monitor therapy

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of Haloperidol. Monitor therapy

Insulins: May diminish the diagnostic effect of Macimorelin. Avoid combination

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Levodopa-Containing Products: May diminish the diagnostic effect of Macimorelin. Avoid combination

Modafinil: May diminish the diagnostic effect of Macimorelin. Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May diminish the diagnostic effect of Macimorelin. Avoid combination

Products that Affect Growth Hormone: May diminish the diagnostic effect of Macimorelin. Avoid combination

Propylthiouracil: May diminish the diagnostic effect of Macimorelin. Avoid combination

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may enhance the QTc-prolonging effect of QT-prolonging Agents (Highest Risk). Management: Monitor for QTc interval prolongation and ventricular arrhythmias when these agents are combined. Patients with additional risk factors for QTc prolongation may be at even higher risk. Monitor therapy

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Somatostatin Analogs: May diminish the diagnostic effect of Macimorelin. Avoid combination

St John's Wort: May decrease the serum concentration of Macimorelin. Avoid combination

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

1% to 10%:

Cardiovascular: Sinus bradycardia (1%)

Central nervous system: Dizziness (4%), fatigue (4%), headache (4%), feeling hot (1%)

Dermatologic: Hyperhidrosis (1%)

Gastrointestinal: Dysgeusia (5%), hunger (3%), nausea (3%), diarrhea (2%)

Respiratory: Upper respiratory tract infection (2%), nasopharyngitis (1%)

Frequency not defined:

Cardiovascular: Prolonged QT interval on ECG

Warnings/Precautions

Concerns related to adverse effects:

• QT prolongation: Prolongation of the QTc interval (~11 msec) has been observed in clinical trials at doses 2- and 4-times the recommended dosage; avoid concurrent use with other agents known to prolong the QT interval.

Disease-related concerns:

• Endocrine disorders: Correct other pituitary hormone deficiencies prior to administration.

• Hypothalamic disease: Growth hormone deficiency due to hypothalamic lesion may not be detected early in the disease process; macimorelin stimulates release of stored growth hormone from the anterior pituitary, which may lead to false negative result. Repeat testing may be necessary.

Other warnings/precautions:

• Appropriate use: Discontinue growth hormone therapy ≥1 week prior to administration.

Monitoring Parameters

Serum growth hormone at 30, 45, 60, and 90 minutes following administration

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Patient Education

What is this drug used for?

• It is used to test for growth hormone deficiency.

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Fast heartbeat

• Abnormal heartbeat

• Passing out

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.