Page last updated: 2024-12-11

macimorelin

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID9804938
CHEMBL ID278623
SCHEMBL ID1984708
MeSH IDM0586808

Synonyms (51)

Synonym
bdbm50125886
2-amino-n-{(r)-1-[(r)-1-formylamino-2-(1h-indol-3-yl)-ethylcarbamoyl]-2-1h-indol-3-yl-ethyl}-2-methyl-propionamide
ep-1572
ep-01572
CHEMBL278623 ,
macimorelin
jmv 1843
ard-07
ep01572
jmv-1843
aezs-130
aminoisobutyryl-tryptophyl-tryptophanamine-formyl
unii-8680b21w73
ep1572
d-87575
381231-18-1
macimorelin [usan:inn]
jmv1843
ep 1572
8680b21w73 ,
macimorelin [mi]
macimorelin [inn]
macimorelin [usan]
macimorelin [who-dd]
n(sup 2)-(2-amino-2-methylpropanoyl-n1-((1r)-1-formamido-2-(1h-indol-3-yl)ethyl)-d-tryptophanamide
ard07
SCHEMBL1984708
macimorelin (usan)
D10563
gtpl9745
aib-dtrp-dgtrp-cho
aezs130
umv1843
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
DB13074
solorel
Q15624037
2-amino-n-((r)-1-(((r)-1-formamido-2-(1h-indol-3-yl)ethyl)amino)-3-(1h-indol-3-yl)-1-oxopropan-2-yl)-2-methylpropanamide
381231-18-1 (free base)
ep 1572; jmv 1843; macimorelin
EN300-24449845
(2r)-2-(2-amino-2-methylpropanamido)-3-(1h-indol-3-yl)-n-[(1r)-2-(1h-indol-3-yl)-1-formamidoethyl]propanamide
CS-0003577
HY-14820
d-tryptophanamide,2-methylalanyl-n-((1r)-1-(formylamino)-2-(1h-indol-3-yl)ethyl)-
macimorelinum
macimoreline
v04cd06
macimorelina
DTXSID601045766
GLXC-25240

Research Excerpts

Overview

Macimorelin is a simple, well-tolerated, reproducible, and safe diagnostic test for AGHD with accuracy comparable to that of the ITT. It is a novel, orally active ghrelin mimetic that stimulates GH secretion.

ExcerptReferenceRelevance
"Macimorelin is an orally active growth hormone secretagogue indicated for the diagnosis of adult growth hormone deficiency. "( Thorough QT/QTc Study Evaluating the Effect of Macimorelin on Cardiac Safety Parameters in Healthy Participants.
Ammer, N; Demmel, V; Kelepouris, N; Lissy, M; Ostrow, V; Sachse, R, 2021
)
2.32
"Oral macimorelin is a simple, well-tolerated, reproducible, and safe diagnostic test for AGHD with accuracy comparable to that of the ITT. "( Macimorelin as a Diagnostic Test for Adult GH Deficiency.
Ammer, N; Biller, BMK; Blevins, T; Bolanowski, M; Chanson, P; Garcia, JM; Korbonits, M; Luger, A; Marcelli, M; Medic-Stojanoska, M; Pekic, S; Popovic, V; Sachse, R; Schopohl, J; Strasburger, CJ; Swerdloff, R; Wang, C; Yuen, KCJ; Zakrzewska, A, 2018
)
2.44
"Macimorelin is a novel, orally active ghrelin mimetic that stimulates GH secretion."( Macimorelin (AEZS-130)-stimulated growth hormone (GH) test: validation of a novel oral stimulation test for the diagnosis of adult GH deficiency.
Biller, BM; Bonert, V; Cook, D; Dobs, A; Garcia, JM; Kipnes, M; Kyle, M; Merriam, GR; Molitch, ME; Swerdloff, R; Wang, C; Yuen, KC, 2013
)
2.55

Toxicity

Daily oral macimorelin for 1 week was safe and numerically improved body weight and QOL in patients with cancer cachexia compared with placebo. No Macimorelin-related adverse events were reported, and the drug was well tolerated.

ExcerptReferenceRelevance
" No macimorelin-related adverse events were reported, and macimorelin was well tolerated."( Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of Macimorelin in Children with Suspected Growth Hormone Deficiency: An Open-Label, Group Comparison, Dose-Escalation Trial.
Ammer, N; Bagci, EB; Bolshova, OV; Chaychenko, T; Csákváry, V; Damholt, BB; Katanic, D; Mikhailova, E; Muzsnai, Á; Raduk, D; Senatorova, G; Szalecki, M; Teifel, M; Vajda, Z; Zelinska, N, 2021
)
1.42
" No related serious or non-serious adverse events were reported."( Pilot clinical trial of macimorelin to assess safety and efficacy in patients with cancer cachexia.
Ammer, N; Anderson, LJ; Garcia, JM; Graf, SA; Herodes, M; Marcelli, M; Salas, R; Schur, EA; Shober, S, 2023
)
1.22
"Daily oral macimorelin for 1 week was safe and numerically improved body weight and QOL in patients with cancer cachexia compared with placebo."( Pilot clinical trial of macimorelin to assess safety and efficacy in patients with cancer cachexia.
Ammer, N; Anderson, LJ; Garcia, JM; Graf, SA; Herodes, M; Marcelli, M; Salas, R; Schur, EA; Shober, S, 2023
)
1.61

Pharmacokinetics

ExcerptReferenceRelevance
" In addition, the pharmacodynamic effects (growth hormone release, insulin-like growth factor-1 concentrations) and the tolerability of ARD-07 are investigated in this open-label, randomized, crossover study."( Effect of food on the pharmacokinetics and pharmacodynamics of an oral ghrelin agonist (ARD-07) in healthy subjects.
Baselgia-Jeker, L; Beglinger, C; Casanova, AT; Drewe, J; Larsen, F; MacLean, CM; Neave, N; Skillern, L, 2009
)
0.35

Bioavailability

ExcerptReferenceRelevance
" The primary objective of this study is to determine the effects of a meal on the oral bioavailability of ARD-07 after a single oral dose (0."( Effect of food on the pharmacokinetics and pharmacodynamics of an oral ghrelin agonist (ARD-07) in healthy subjects.
Baselgia-Jeker, L; Beglinger, C; Casanova, AT; Drewe, J; Larsen, F; MacLean, CM; Neave, N; Skillern, L, 2009
)
0.35
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Growth hormone secretagogue receptor type 1Homo sapiens (human)IC50 (µMol)0.07300.00040.58926.0000AID75332; AID75345
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (47)

Processvia Protein(s)Taxonomy
G protein-coupled receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
spermatogenesisGrowth hormone secretagogue receptor type 1Homo sapiens (human)
learning or memoryGrowth hormone secretagogue receptor type 1Homo sapiens (human)
actin polymerization or depolymerizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
adult feeding behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
hormone-mediated signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of norepinephrine secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
growth hormone secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to foodGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of appetiteGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of appetiteGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to follicle-stimulating hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to estradiolGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of interleukin-1 beta productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of interleukin-6 productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of tumor necrosis factor productionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to insulin stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
ghrelin secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of multicellular organism growthGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of hindgut contractionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of insulin-like growth factor receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of fatty acid metabolic processGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of insulin secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
decidualizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
insulin-like growth factor receptor signaling pathwayGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of inflammatory responseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of synapse assemblyGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of transmission of nerve impulseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of growth hormone secretionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to growth hormoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to lipopolysaccharideGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to dexamethasoneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of locomotion involved in locomotory behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to thyroid hormone stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of neurotransmitter receptor localization to postsynaptic specialization membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
postsynaptic modulation of chemical synaptic transmissionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of postsynapse organizationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of small intestinal transitGrowth hormone secretagogue receptor type 1Homo sapiens (human)
response to L-glutamateGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of sprouting angiogenesisGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of eating behaviorGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of small intestine smooth muscle contractionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
regulation of gastric motilityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
positive regulation of vascular endothelial cell proliferationGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cellular response to insulin-like growth factor stimulusGrowth hormone secretagogue receptor type 1Homo sapiens (human)
negative regulation of macrophage apoptotic processGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (4)

Processvia Protein(s)Taxonomy
growth hormone secretagogue receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
G protein-coupled receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
growth hormone-releasing hormone receptor activityGrowth hormone secretagogue receptor type 1Homo sapiens (human)
peptide hormone bindingGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
plasma membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
cell surfaceGrowth hormone secretagogue receptor type 1Homo sapiens (human)
neuron projectionGrowth hormone secretagogue receptor type 1Homo sapiens (human)
membrane raftGrowth hormone secretagogue receptor type 1Homo sapiens (human)
synaptic membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
Schaffer collateral - CA1 synapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
postsynapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
glutamatergic synapseGrowth hormone secretagogue receptor type 1Homo sapiens (human)
plasma membraneGrowth hormone secretagogue receptor type 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (6)

Assay IDTitleYearJournalArticle
AID75332Binding affinity towards human pituitary Growth hormone secretagogue receptor using [125I][Tyr4]-ghrelin as radioligand2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID9511Concentration in dogs after oral administration at dose of 1 mg/kg after 180 min.2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID60863Stimulating GH secretion in dogs after oral administration at dose of 1 mg/kg2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID75345Binding affinity towards cloned human Growth hormone secretagogue receptor type I in LLC PK-1 cells using [125I][His9]-ghrelin as radioligand2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID187245Ratio of GH release stimulated by 300 ug/kg of compound to that of GH release stimulated by 300 ug/kg of hexarelin in infant rat (sc injection)2003Journal of medicinal chemistry, Mar-27, Volume: 46, Issue:7
New active series of growth hormone secretagogues.
AID1346009Human ghrelin receptor (Ghrelin receptor)2002Journal of endocrinological investigation, Sep, Volume: 25, Issue:8
EP1572: a novel peptido-mimetic GH secretagogue with potent and selective GH-releasing activity in man.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (23)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (21.74)29.6817
2010's11 (47.83)24.3611
2020's7 (30.43)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 44.30

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index44.30 (24.57)
Research Supply Index3.37 (2.92)
Research Growth Index4.85 (4.65)
Search Engine Demand Index62.99 (26.88)
Search Engine Supply Index1.96 (0.95)

This Compound (44.30)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials5 (21.74%)5.53%
Reviews2 (8.70%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other16 (69.57%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]