Page last updated: 2024-11-12

terutroban

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

Description

terutroban: a thromboxan receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID9938840
CHEMBL ID2107786
SCHEMBL ID1896773
MeSH IDM0290640

Synonyms (28)

Synonym
terutroban
bdbm50026753
s18886 ,
SCHEMBL1896773
s 18886
((6r)-6-(4-chlorobenzenesulfonamido)-2-methyl-5,6,7,8-tetrahydronaphthalen-1-yl)propanoic acid
165538-40-9
terutroban [inn]
a6wx9391d8 ,
unii-a6wx9391d8
CHEMBL2107786
gtpl6073
triplion
3-((6r)-6-(4-chlorobenzenesulfonamido)-2-methyl-5,6,7,8-tetrahydronaphthalen-1-yl)propanoic acid
terutroban [who-dd]
CS-4806
AKOS025293445
HY-16991
(6r)-6-[[(4-chlorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydro-2-methyl-1-naphthalenepropanoic acid
BS-16000
(r)-3-(6-((4-chlorophenyl)sulfonamido)-2-methyl-5,6,7,8-tetrahydronaphthalen-1-yl)propanoic acid
Q7705345
1-naphthalenepropanoic acid, 6-[[(4-chlorophenyl)sulfonyl]amino]-5,6,7,8-tetrahydro-2-methyl-, (6r)-
D83664
EX-A6004
BT163710
DTXSID30870091
3-[(6r)-6-(4-chlorobenzenesulfonamido)-2-methyl-5,6,7,8-tetrahydronaphthalen-1-yl]propanoic acid

Research Excerpts

Overview

Terutroban is a selective prostaglandin endoperoxide (TP) receptor antagonist with antithrombotic, antivasoconstrictive and antiatherosclerotic properties. It is currently in development for long-term cardiovascular secondary prevention.

ExcerptReferenceRelevance
"Terutroban is a specific TP receptor antagonist with antithrombotic, antivasoconstrictive, and antiatherosclerotic properties, which may be of interest for the secondary prevention of ischemic stroke."( Rationale and design of a randomized, double-blind, parallel-group study of terutroban 30 mg/day versus aspirin 100 mg/day in stroke patients: the prevention of cerebrovascular and cardiovascular events of ischemic origin with terutroban in patients with
Amarenco, P; Bousser, MG; Chamorro, A; Fisher, M; Ford, I; Fox, K; Hennerici, MG; Mattle, HP; Rothwell, PM, 2009
)
1.3
"Terutroban is a specific thromboxane A2 receptor antagonist with antithrombotic, antivasoconstrictive, and antiatherosclerotic properties, which make it a promising tool for secondary prevention of ischemic stroke."( Rationale and design of the Prevention of Cerebrovascular and Cardiovascular Events of Ischemic Origin with Terutroban in Patients with a History of Ischemic Stroke or Transient Ischemic Attack (PERFORM) Study.
Hennerici, MG, 2009
)
1.29
"Terutroban is a selective prostaglandin endoperoxide (TP) receptor antagonist with antithrombotic, antivasoconstrictive and antiatherosclerotic properties and is currently in development for long-term cardiovascular secondary prevention."( Thromboxane Antagonism with terutroban in Peripheral Arterial Disease: the TAIPAD study.
Bounameaux, H; Cairols, MA; Clement, DL; Coccheri, S; Fiessinger, JN; Fletcher, JP; Hoffmann, U; Turpie, AG, 2010
)
2.1
"• Terutroban is a selective TP receptor antagonist, i.e. "( Daily administration of the TP receptor antagonist terutroban improved endothelial function in high-cardiovascular-risk patients with atherosclerosis.
Adnot, S; Akakpo, S; Boyer, L; Covali-Noroc, A; Dubois-Randé, JL; Lesault, PF; Pelle, G; Rideau, D; Teiger, E, 2011
)
1.34
"Terutroban (S 18886) is a selective antagonist of TP receptors, the receptors for TXA2, that are present on platelets and on vascular smooth muscle cells, but also on endothelial cells."( [Terutroban and endothelial TP receptors in atherogenesis].
Verbeuren, TJ, 2006
)
1.97

Compound-Compound Interactions

ExcerptReferenceRelevance
" Thus, combination with a TP antagonist might reveal an antiinflammatory effect of a COX-2 inhibitor in this disease."( Cyclooxygenases, thromboxane, and atherosclerosis: plaque destabilization by cyclooxygenase-2 inhibition combined with thromboxane receptor antagonism.
Egan, KM; FitzGerald, GA; Fries, S; Lawson, JA; Lucitt, MB; Puré, E; Wang, M; Zukas, AM, 2005
)
0.33
" Combination with the COX-2 inhibitor failed to augment the impact of TP antagonism alone on lesion area."( Cyclooxygenases, thromboxane, and atherosclerosis: plaque destabilization by cyclooxygenase-2 inhibition combined with thromboxane receptor antagonism.
Egan, KM; FitzGerald, GA; Fries, S; Lawson, JA; Lucitt, MB; Puré, E; Wang, M; Zukas, AM, 2005
)
0.33
" Despite early intervention, selective inhibition of COX-2, alone or in combination with a TP antagonist, failed to modify disease progression but may undermine plaque stability when combined with the antagonist."( Cyclooxygenases, thromboxane, and atherosclerosis: plaque destabilization by cyclooxygenase-2 inhibition combined with thromboxane receptor antagonism.
Egan, KM; FitzGerald, GA; Fries, S; Lawson, JA; Lucitt, MB; Puré, E; Wang, M; Zukas, AM, 2005
)
0.33

Dosage Studied

ExcerptRelevanceReference
" COX selectivity was determined from dose-response curves by calculating a ratio (COX-2/COX-1) of IC50 values."( In vitro pharmacological evaluation of multitarget agents for thromboxane prostanoid receptor antagonism and COX-2 inhibition.
Bertinaria, M; Buccellati, C; Capra, V; Carnevali, S; Cena, C; Fruttero, R; Garella, D; Hoxha, M; Rolando, B; Rovati, GE; Sala, A, 2016
)
0.43
[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)
Thromboxane A2 receptor Homo sapiens (human)IC50 (µMol)0.01640.00110.71065.2000AID1164309
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (17)

Processvia Protein(s)Taxonomy
smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to nutrientThromboxane A2 receptor Homo sapiens (human)
response to xenobiotic stimulusThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood coagulationThromboxane A2 receptor Homo sapiens (human)
response to testosteroneThromboxane A2 receptor Homo sapiens (human)
thromboxane A2 signaling pathwayThromboxane A2 receptor Homo sapiens (human)
response to ethanolThromboxane A2 receptor Homo sapiens (human)
positive regulation of angiogenesisThromboxane A2 receptor Homo sapiens (human)
positive regulation of smooth muscle contractionThromboxane A2 receptor Homo sapiens (human)
cellular response to lipopolysaccharideThromboxane A2 receptor Homo sapiens (human)
negative regulation of cell migration involved in sprouting angiogenesisThromboxane A2 receptor Homo sapiens (human)
inflammatory responseThromboxane A2 receptor Homo sapiens (human)
positive regulation of blood pressureThromboxane A2 receptor Homo sapiens (human)
positive regulation of vasoconstrictionThromboxane A2 receptor Homo sapiens (human)
positive regulation of cytosolic calcium ion concentrationThromboxane A2 receptor Homo sapiens (human)
adenylate cyclase-activating G protein-coupled receptor signaling pathwayThromboxane A2 receptor Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Processvia Protein(s)Taxonomy
thromboxane A2 receptor activityThromboxane A2 receptor Homo sapiens (human)
guanyl-nucleotide exchange factor activityThromboxane A2 receptor Homo sapiens (human)
protein bindingThromboxane A2 receptor Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (3)

Processvia Protein(s)Taxonomy
acrosomal vesicleThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
nuclear speckThromboxane A2 receptor Homo sapiens (human)
plasma membraneThromboxane A2 receptor Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1164309Antagonist activity against human thromboxane A2 receptor alpha expressed in QBI-HEK293A cells assessed as reduction in I-BOP-induced inositol monophosphate production incubated for 15 to 60 mins before I-BOP addition by HTRF assay2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
Potent, long-acting cyclopentane-1,3-Dione thromboxane (A2)-receptor antagonists.
AID1346422Human TP receptor (Prostanoid receptors)1998Bioorganic & medicinal chemistry letters, Jun-02, Volume: 8, Issue:11
Synthesis and biological evaluation of new tetrahydronaphthalene derivatives as thromboxane receptor antagonists.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (61)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's2 (3.28)18.2507
2000's30 (49.18)29.6817
2010's27 (44.26)24.3611
2020's2 (3.28)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 26.97

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index26.97 (24.57)
Research Supply Index4.32 (2.92)
Research Growth Index5.50 (4.65)
Search Engine Demand Index31.58 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (26.97)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials13 (21.31%)5.53%
Reviews9 (14.75%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other39 (63.93%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]