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MACIMORELIN ACETATE
DIR Classification
Classification:Most-DIQT concern
Severity Score:4.0
Description in Drug Labeling: View Full Labeling: SPL in DailyMed | PDF
- WARNINGS AND PRECAUTIONS
- QT Prolongation
- MACRILEN causes an increase of about 11 msec in the corrected QT (QTc) interval [see Clinical Pharmacology (12.2)]. QT prolongation can lead to development of torsade de pointes-type ventricular tachycardia with the risk increasing as the degree of prolongation increases. The concomitant use of MACRILEN with drugs that are known to prolong the QT interval should be avoided [see Dosage and Administration (2.2) and Drug Interactions (7.1)].
- DRUG INTERACTIONS
- Drugs that Prolong QT Interval
- Co-administration 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) may lead to development of torsade de pointes-type ventricular tachycardia. Avoid concomitant use of MACRILEN with drugs that prolong the QT interval. Sufficient washout time of drugs that are known to prolong the QT interval prior to administration of MACRILEN is recommended [see Dosage and Administration (2.2) and Warnings and Precautions (5.1)].
- CLINICAL PHARMACOLOGY
- Pharmacodynamics
- Cardiac electrophysiology
- The effects of macimorelin on ECG parameters were investigated in a dedicated Thorough QT study that investigated in a 3-way cross-over design with 60 healthy subjects the effects of a supra-therapeutic dose of macimorelin (2 mg/kg) (4 times the recommended dosage) in comparison with placebo and with moxifloxacin. This study showed a mean baseline- and placebo-adjusted change (upper single-sided 95% confidence interval) in QTcF of 9.6 msec (11.4 msec) at 4 h post-dose, which occurred after the mean maximum macimorelin plasma concentration (0.5 h). A similar increase in the QTcF interval was also observed in a single-ascending dose study, which included three dose levels (0.5 mg/kg, and 1 mg/kg and 2 mg/kg (2 times and 4 times the recommended dosage, respectively). All three doses levels studied showed a similar magnitude of QTcF prolongation in the Thorough QT study, suggesting an absence of dose dependent changes. The mechanism for the observed QTcF prolongation is unknown [see Warnings and Precautions (5.1)].
Postmarketing Surveillance
Contingency Table:
Current Drug
Other Drugs
QT Prolongation
0
24092
Other ADRs
0
38381587
Odds Ratio = N/A
Drug Property Information
ATC Code(s):
- V04CD06 - macimorelin acetate
- V04CD - Tests for pituitary function
- V04C - OTHER DIAGNOSTIC AGENTS
- V04 - DIAGNOSTIC AGENTS
- V - VARIOUS
Active Ingredient:MACIMORELIN
Active Ingredient UNII:8680B21W73
Drugbank ID:DB13074
PubChem Compound:N/ADIR Classification
CTD ID:C582727
CAS Number:381231-18-1
Dosage Form(s):granule, for solution
Route(s) Of Administrator:oral
Daily Dose:
Chemical Structure: 
SMILE Code:
CC(C)(N)C(=O)N[C@H](CC1=CNC2=CC=CC=C12)C(=O)N[C@H](CC1=CNC2=CC=CC=C12)NC=O
CC(C)(N)C(=O)N[C@H](CC1=CNC2=CC=CC=C12)C(=O)N[C@H](CC1=CNC2=CC=CC=C12)NC=O
Reference
1: Thorough QT/QTc Study Evaluating the Effect of Macimorelin on Cardiac Safety Parameters in Healthy Participants.
[Lissy Michael,Demmel Valentin,Sachse Richard,Ammer Nicola,Kelepouris Nicky,Ostrow Vlady]Clin Pharmacol Drug Dev,2021 May;10(5):494-501. PMID: 32961034
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