Details of the Drug

General Information of Drug (ID: DMQYJIR)

Drug Name

Macimorelin

Synonyms

Solorel; AEZS-130; ARD-07; ARD-0705; EP-01572; EP-1572; JMV-1843

Indication

Disease Entry	ICD 11	Status	REF
Growth hormone deficiency	5A61.3	Approved	[1]
Somatotropin deficiency	5A61.0	Approved	[2]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 1

Molecular Weight (mw)

474.6

Logarithm of the Partition Coefficient (xlogp)

1.8

Rotatable Bond Count (rotbonds)

9

Hydrogen Bond Donor Count (hbonddonor)

6

Hydrogen Bond Acceptor Count (hbondacc)

4

ADMET Property

Absorption Tmax: The time to maximum plasma concentration (Tmax) is 0.5-1.5 h [3]
Clearance: The clearance of drug is 37,411.0 +/- 4,554.6 mL/min [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 4.1 hours []
Metabolism: The drug is metabolized via the liver []
Vd: The volume of distribution (Vd) of drug is 5,733.4 +/- 565.7 L [3]

Chemical Identifiers

Formula: C26H30N6O3
IUPAC Name: 2-amino-N-[(2R)-1-[[(1R)-1-formamido-2-(1H-indol-3-yl)ethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-2-methylpropanamide
Canonical SMILES: CC(C)(C(=O)N[C@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@H](CC3=CNC4=CC=CC=C43)NC=O)N
InChI: InChI=1S/C26H30N6O3/c1-26(2,27)25(35)31-22(11-16-13-28-20-9-5-3-7-18(16)20)24(34)32-23(30-15-33)12-17-14-29-21-10-6-4-8-19(17)21/h3-10,13-15,22-23,28-29H,11-12,27H2,1-2H3,(H,30,33)(H,31,35)(H,32,34)/t22-,23-/m1/s1
InChIKey: UJVDJAPJQWZRFR-DHIUTWEWSA-N

Cross-matching ID

PubChem CID: 9804938
CAS Number: 381231-18-1
DrugBank ID: DB13074
TTD ID: D0BV3J
ACDINA ID: D01233

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Growth hormone secretagogue receptor 1 (GHSR)	TTWDC17	GHSR_HUMAN	Agonist	[4]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Molecular Expression Atlas of This Drug

The Studied Disease

Growth hormone deficiency

ICD Disease Classification

5A61.3

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Growth hormone secretagogue receptor 1 (GHSR)	DTT	GHSR	4.56E-01	-0.14	-0.74

Molecular Expression Atlas (MEA)

MEA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from Macimorelin (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Major	Increased risk of prolong QT interval by the combination of Macimorelin and Ivosidenib.	Acute myeloid leukaemia [2A60]	[5]
Oliceridine	DM6MDCF	Major	Increased risk of prolong QT interval by the combination of Macimorelin and Oliceridine.	Acute pain [MG31]	[6]
Levalbuterol	DM5YBO1	Major	Increased risk of prolong QT interval by the combination of Macimorelin and Levalbuterol.	Asthma [CA23]	[5]
Eslicarbazepine	DMZREFQ	Moderate	Increased metabolism of Macimorelin caused by Eslicarbazepine mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[6]
Selpercatinib	DMZR15V	Major	Increased risk of prolong QT interval by the combination of Macimorelin and Selpercatinib.	Lung cancer [2C25]	[5]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Saccharin sodium anhydrous	E00443	656582	Flavoring agent
Sodium stearyl fumarate	E00545	23665634	lubricant
Crospovidone	E00626	Not Available	Disintegrant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Hydrophobic colloidal silica	E00285	24261	Anticaking agent; Emulsion stabilizing agent; Glidant; Suspending agent; Viscosity-controlling agent
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Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Macimorelin 60 mg solution	60 mg	Solution	Oral

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References

1	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
2	2017 FDA drug approvals.Nat Rev Drug Discov. 2018 Feb;17(2):81-85.
3	Piccoli F, Degen L, MacLean C, Peter S, Baselgia L, Larsen F, Beglinger C, Drewe J: Pharmacokinetics and pharmacodynamic effects of an oral ghrelin agonist in healthy subjects. J Clin Endocrinol Metab. 2007 May;92(5):1814-20. doi: 10.1210/jc.2006-2160. Epub 2007 Feb 6.
4	National Cancer Institute Drug Dictionary (drug id 735530).
5	Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
6	Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.