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Synonyms: B1287 | E5564
Compound class: Synthetic organic
Comment: Eritoran is a synthetic analogue of lipid A, the bacterial LPS component. It is referred to as a Toll-like receptor 4 (TLR4) antagonist, but rather than direct interaction, eritoran binds to MD-2 and prevents formation of the MD-2.TLR4 protein complex. Thus, eritoran appears to antagonise LPS-induced TLR4 activation.
Eritoran has been investigated as a therapeutic for the management of sepsis, but failed to show sufficient clinical effect .
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
1. Barochia A, Solomon S, Cui X, Natanson C, Eichacker PQ. (2011)
Eritoran tetrasodium (E5564) treatment for sepsis: review of preclinical and clinical studies.
Expert Opin Drug Metab Toxicol, 7 (4): 479-94. [PMID:21323610]
2. Ingalls RR, Monks BG, Savedra R, Christ WJ, Delude RL, Medvedev AE, Espevik T, Golenbock DT. (1998)
CD11/CD18 and CD14 share a common lipid A signaling pathway.
J Immunol, 161 (10): 5413-20. [PMID:9820516]
3. Tidswell M, Tillis W, Larosa SP, Lynn M, Wittek AE, Kao R, Wheeler J, Gogate J, Opal SM, Eritoran Sepsis Study Group. (2010)
Phase 2 trial of eritoran tetrasodium (E5564), a toll-like receptor 4 antagonist, in patients with severe sepsis.
Crit Care Med, 38 (1): 72-83. [PMID:19661804]