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]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 1 Molecular Weight (mw) 474.6
Topological Polar Surface Area (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 [4]
Metabolism
The drug is metabolized via the liver [4]
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 [5]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

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) Jump to Detail Molecular Expression Atlas of This Drug

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] [16]
Oliceridine DM6MDCF Major Increased risk of prolong QT interval by the combination of Macimorelin and Oliceridine. Acute pain [MG31] [17]
Levalbuterol DM5YBO1 Major Increased risk of prolong QT interval by the combination of Macimorelin and Levalbuterol. Asthma [CA23] [16]
Eslicarbazepine DMZREFQ Moderate Increased metabolism of Macimorelin caused by Eslicarbazepine mediated induction of CYP450 enzyme. Epilepsy/seizure [8A61-8A6Z] [17]
Selpercatinib DMZR15V Major Increased risk of prolong QT interval by the combination of Macimorelin and Selpercatinib. Lung cancer [2C25] [16]

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
Pharmaceutical Formulation
Formulation Name Drug Dosage Dosage Form Route
Macimorelin 60 mg solution 60 mg Solution Oral
Jump to Detail Pharmaceutical Formulation Page of This Drug

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 FDA approval: ado-trastuzumab emtansine for the treatment of patients with HER2-positive metastatic breast cancer. Clin Cancer Res. 2014 Sep 1;20(17):4436-41.
5 National Cancer Institute Drug Dictionary (drug id 735530).
6 GH-releasing peptide-2 increases fat mass in mice lacking NPY: indication for a crucial mediating role of hypothalamic agouti-related protein. Endocrinology. 2002 Feb;143(2):558-68.
7 Design and biological activities of L-163,191 (MK-0677): a potent, orally active growth hormone secretagogue. Proc Natl Acad Sci U S A. 1995 Jul 18;92(15):7001-5.
8 Pharmacodynamic hormonal effects of anamorelin, a novel oral ghrelin mimetic and growth hormone secretagogue in healthy volunteers. Growth Horm IGF Res. 2009 Jun;19(3):267-73.
9 Contribution of protein binding to the pharmacokinetics of the ghrelin receptor agonist TZP-101 in healthy volunteers and adults with symptomatic gastroparesis: two randomized, double-blind studies and a binding profile study. Clin Drug Investig. 2009;29(6):409-18.
10 Orphan GPCR research. Br J Pharmacol. 2008 March; 153(Suppl 1): S339-S346.
11 Hypotensive effects of ghrelin receptor agonists mediated through a novel receptor. Br J Pharmacol. 2014 Mar;171(5):1275-86.
12 Pharmacological characterisation of a new oral GH secretagogue, NN703. Eur J Endocrinol. 1999 Aug;141(2):180-9.
13 Efficacy of ipamorelin, a novel ghrelin mimetic, in a rodent model of postoperative ileus.J Pharmacol Exp Ther.2009 Jun;329(3):1110-6.
14 A gift for research. SciBX 7(6); doi:10.1038/scibx.2014.160. Feb. 13 2014
15 The Prokinetic Face of Ghrelin. International Journal of Peptides Volume 2010 (2010), Article ID 493614, Page(11).
16 Product Information. Fycompa (perampanel). Eisai Inc, Teaneck, NJ.
17 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.