ﺑﺎﺯﮔﺸﺖ ﺑﻪ ﺻﻔﺤﻪ ﻗﺒﻠﯽ
خرید پکیج
تعداد آیتم قابل مشاهده باقیمانده : -41 مورد

Macimorelin (United States: Not available): Drug information

Macimorelin (United States: Not available): Drug information
2025© UpToDate, Inc. and its affiliates and/or licensors. All Rights Reserved.
For additional information see "Macimorelin (United States: Not available): Patient drug information"

For abbreviations, symbols, and age group definitions show table
Brand Names: US
  • Macrilen [DSC]
Pharmacologic Category
  • Diagnostic Agent;
  • Growth Hormone Secretagogue Receptor Agonist
Dosing: Adult

Dosage guidance:

Dosage form information: Macrilen has been discontinued in the United States for >1 year.

Diagnostic aid, growth hormone deficiency, adult

Diagnostic aid, growth hormone deficiency, adult: Note: Correct other pituitary hormone deficiencies prior to administration (Ref). Discontinue growth hormone therapy at least 1 week prior to administration.

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

BMI >40 kg/m2: Oral: 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: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Liver Impairment: Adult

There are no dosage adjustments provided in the manufacturer's labeling.

Dosing: Older Adult

Refer to adult dosing.

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

Contraindications

There are no contraindications listed in the manufacturer's labeling

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:

• 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.

Product Availability

Macrilen has been discontinued in the United States for >1 year.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product

Packet, Oral:

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

Generic Equivalent Available: US

No

Pricing: US

Pack (Macrilen Oral)

60 mg (per each): $5,400.00

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

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

Use: Labeled Indications

Diagnostic aid, growth hormone deficiency, adult: 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.

Medication Safety Issues

Sound-alike/look-alike issues:

Macimorelin may be confused with tesamorelin

Metabolism/Transport Effects

Substrate of CYP3A4 (Major with inducers), CYP3A4 (Minor with inhibitors); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential;

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the drug interactions program by clicking on the “Launch drug interactions program” link above.

Aspirin: Coadministration of Aspirin and Macimorelin may alter diagnostic results. Risk X: Avoid

Atropine (Systemic): Coadministration of Atropine (Systemic) and Macimorelin may alter diagnostic results. Risk X: Avoid

Bosentan: Coadministration of Bosentan and Macimorelin may alter diagnostic results. Risk C: Monitor

CloNIDine: Coadministration of CloNIDine and Macimorelin may alter diagnostic results. Risk X: Avoid

Corticosteroids (Systemic): Coadministration of Corticosteroids (Systemic) and Macimorelin may alter diagnostic results. Risk X: Avoid

CYP3A4 Inducers (Strong): May decrease serum concentration of Macimorelin. Risk X: Avoid

Efavirenz: Coadministration of Efavirenz and Macimorelin may alter diagnostic results. Risk C: Monitor

Etravirine: Coadministration of Etravirine and Macimorelin may alter diagnostic results. Risk C: Monitor

Haloperidol: QT-prolonging Agents (Indeterminate Risk - Avoid) may increase QTc-prolonging effects of Haloperidol. Risk C: Monitor

Insulin: Coadministration of Insulin and Macimorelin may alter diagnostic results. Risk X: Avoid

Levodopa-Foslevodopa: Coadministration of Levodopa-Foslevodopa and Macimorelin may alter diagnostic results. Risk X: Avoid

Levoketoconazole: QT-prolonging Agents (Indeterminate Risk - Avoid) may increase QTc-prolonging effects of Levoketoconazole. 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. Risk C: Monitor

Modafinil: Coadministration of Modafinil and Macimorelin may alter diagnostic results. Risk C: Monitor

Nonsteroidal Anti-Inflammatory Agents: Coadministration of Nonsteroidal Anti-Inflammatory Agents and Macimorelin may alter diagnostic results. Risk X: Avoid

Products that Affect Growth Hormone: Coadministration of Products that Affect Growth Hormone and Macimorelin may alter diagnostic results. Risk X: Avoid

Propylthiouracil: Coadministration of Propylthiouracil and Macimorelin may alter diagnostic results. Risk X: Avoid

QT-prolonging Agents (Highest Risk): QT-prolonging Agents (Indeterminate Risk - Avoid) may increase QTc-prolonging effects 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. Risk C: Monitor

Somatostatin Analogs: Coadministration of Somatostatin Analogs and Macimorelin may alter diagnostic results. Risk X: Avoid

St John's Wort: May decrease serum concentration of Macimorelin. Risk X: Avoid

Food Interactions

Liquid meal decreased macimorelin Cmax and AUC by 55% and 49% respectively. Patient should fast for at least 8 hours prior to macimorelin administration.

Pregnancy Considerations

Animal reproduction studies have not been conducted.

Breastfeeding Considerations

It is not known if macimorelin is present in breast milk. According to the manufacturer, the decision to breastfeed following administration should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.

Monitoring Parameters

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

Reference Range

According to the manufacturer, serum growth hormone (GH) levels <2.8 ng/mL (SI: <2.8 mcg/L) at 30, 45, 60, and 90 minutes following macimorelin administration confirm the presence of adult GH deficiency. However, using a GH cutoff level <5.1 ng/mL (SI: <5.1 mcg/L) may more optimally balance sensitivity and specificity (Garcia 2018).

Mechanism of Action

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

Pharmacokinetics (Adult Data Unless Noted)

Metabolism: Hepatic via CYP3A4

Half-life elimination: 4.1 hours

Time to peak (plasma): 0.5 to 1.5 hours

  1. Garcia JM, Biller BMK, Korbonits M, et al. Macimorelin as a diagnostic test for adult GH deficiency. J Clin Endocrinol Metab. 2018;103(8):3083-3093. doi:10.1210/jc.2018-00665 [PubMed 29860473]
  2. Macrilen (macimorelin) [prescribing information]. Plainsboro, NJ: Novo Nordisk Inc; July 2021.
  3. Yuen KCJ, Biller BMK, Radovick S, et al. American Association of Clinical Endocrinologists and American College of Endocrinology guidelines for management of growth hormone deficiency in adults and patients transitioning from pediatric to adult care. Endocr Pract. 2019;25(11):1191-1232. doi:10.4158/GL-2019-0405 [PubMed 31760824]
Topic 116182 Version 72.0