Page last updated: 2024-12-06

linotroban

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

Description

Linotroban is a non-steroidal anti-inflammatory drug (NSAID) with a unique mechanism of action. It is a potent and selective inhibitor of the enzyme leukotriene A4 hydrolase (LTA4H). LTA4H is a key enzyme in the biosynthesis of leukotrienes, which are potent inflammatory mediators involved in a variety of inflammatory and allergic diseases. Linotroban inhibits the formation of leukotrienes by blocking the conversion of LTA4 to LTB4, a potent chemoattractant and activator of neutrophils. Linotroban has shown promising preclinical activity in models of inflammatory diseases such as asthma, arthritis, and inflammatory bowel disease. However, clinical trials have been hampered by its poor oral bioavailability and its tendency to cause liver toxicity. Linotroban is studied to understand the role of leukotrienes in inflammation and to explore its potential as a therapeutic agent for inflammatory diseases. Linotroban is synthesized by a multi-step process involving several chemical reactions. Its importance lies in its ability to selectively inhibit LTA4H and its potential to treat various inflammatory diseases.'

linotroban: structure in first source; a thromboxane A2 receptor antagonist [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID65940
CHEMBL ID1742437
SCHEMBL ID635680
MeSH IDM0230123

Synonyms (25)

Synonym
linotroban
hn-11500
NCGC00160350-01
AKOS000277492
2-[5-[2-(benzenesulfonamido)ethyl]thiophen-2-yl]oxyacetic acid
L003572
6o2o36ol57 ,
((5-(2-benzenesulfonamidoethyl)-2-thienyl)oxy)acetic acid
unii-6o2o36ol57
linotroban [inn]
120824-08-0
tox21_111755
dtxsid4046103 ,
dtxcid2026103
cas-120824-08-0
CHEMBL1742437
hn11500
cl 87-15-01
hn 11500
cl-87-15-01
141443-73-4
SCHEMBL635680
2-[5-[2-(phenylsulfonylamino)ethyl]thiophen-2-yl]oxyacetic acid
2-((5-(2-(phenylsulfonamido)ethyl)thiophen-2-yl)oxy)acetic acid
Q27265212

Research Excerpts

Bioavailability

ExcerptReferenceRelevance
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" The washout period between each dosage applied was at least 12 days."( Antiplatelet and anticoagulant effects of "HN-11 500," a selective thromboxane receptor antagonist.
Breddin, HK; Fellier, H; Radziwon, P; Schenk, JF, 2001
)
0.31
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency35.03560.004023.8416100.0000AID485290; AID489007
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.16230.035520.977089.1251AID504332
nuclear receptor subfamily 1, group I, member 2Rattus norvegicus (Norway rat)Potency11.22020.10009.191631.6228AID1346983
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency89.12510.354828.065989.1251AID504847
DNA polymerase kappa isoform 1Homo sapiens (human)Potency11.22020.031622.3146100.0000AID588579
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (4)

Assay IDTitleYearJournalArticle
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (8)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's3 (37.50)18.2507
2000's2 (25.00)29.6817
2010's2 (25.00)24.3611
2020's1 (12.50)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (12.50%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other7 (87.50%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]