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Synonyms: A-64077 | ZYFLO®
zileuton is an approved drug (FDA (1996))
Compound class: Synthetic organic
Comment: Zileuton is an orally active 5-LOX inhibitor.
The approved drug is a racemic mixture of R(+) and S(-) enantiomers (PubChem CID 10681296 and CID 10220327 respectively), which are both pharmacologically active. The structure shown here does not specify stereochemistry and represents the mixture.
The hepatotoxicity of zileuton is suggested to be due to the N-hydroxyurea group .
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.✖
View more information in the IUPHAR Pharmacology Education Project: zileuton
|No information available.|
|Summary of Clinical Use|
|Used in the prophylaxis and chronic treatment of asthma.|
|Mechanism Of Action and Pharmacodynamic Effects|
|Through its inhibition of 5-lipoxygenase, zileuton inhibits the formation of leukotrienes LTB4, LTC4, LTD4, and LTE4, which are formed from arachidonic acid in the reaction catalysed by this enzyme. An additional activity of zileuton is direct reduction of sebaceous lipids production .|
|Organ function impairment|
|Zileuton should not be prescribed for patients with liver function impairment as it causes side effects including liver enzyme elevation.|
For extended ADME data see the following: