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QuickView for zileuton (compound)

Name: zileuton
PubChem Compound ID: 10220327
Molecular formula: C11H12N2O2S
Molecular weight: 236.291 g/mol
Name: zileuton
Name (isomeric): DB00744
Drug Type: small molecule
Zileutonum [INN-Latin]
Brand: Leutrol, Zyflo, Zyflo CR
Category: Lipoxygenase Inhibitors, Leukotriene Antagonists
CAS number: 111406-87-2
Indication: For the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.
Zileuton is an asthma drug that differs chemically and pharmacologically from other antiasthmatic agents. It blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway. Current data indicates that asthma is a chronic inflammatory disorder of the airways involving the production and activity of several e...
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Mechanism of Action:
Leukotrienes are substances that induce numerous biological effects including augmentation of neutrophil and eosinophil migration, neutrophil and monocyte aggregation, leukocyte adhesion, increased capillary permeability, and smooth muscle contraction. These effects contribute to inflammation, edema, mucus secretion, and bronchoconstriction in the ...
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Absorption: Rapidly and almost completely absorbed. The absolute bioavailability is unknown.
Protein binding: 93% bound to plasma proteins, primarily to albumin.
Biotransformation: Hepatic. Zileuton and its N-dehydroxylated metabolite are oxidatively metabolized by the cytochrome P450 isoenzymes 1A2, 2C9 and 3A4.
Route of elimination: Elimination of zileuton is predominantly via metabolism with a mean terminal half-life of 2.5 hours. The urinary excretion of the inactive N-dehydroxylated metabolite and unchanged zileuton each accounted for less than 0.5% of the dose.
Half Life: 2.5 hours
Clearance: Apparent oral cl=7 mL/min/kg
Toxicity: The oral minimum lethal doses in mice and rats were 500-4000 and 300-1000 mg/kg in various preparations, respectively (providing greater than 3 and 9 times the systemic exposure [AUC] achieved at the maximum recommended human daily oral dose, respectively).
Affected organisms: Humans and other mammals
Drug interaction:
OxtriphyllineZileuton increases the effect and toxicity of theophylline
AminophyllineZileuton increases the effect and toxicity of theophylline
PimozideIncreased risk of cardiotoxicity and arrhythmias
DihydroergotaminePossible ergotism and severe ischemia with this combination
RamelteonZileuton increases levels/toxicity of ramelteon
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