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Description: 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 airways of asthmatic patients. Zileuton relieves such symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems.
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Zileuton is an asthma drug. It blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway. Sulfido-peptide leukotrienes (LTC4, LTD4, LTE4, also known as the slow-releasing substances of anaphylaxis) and LTB4, a chemoattractant for neutrophils and eosinophils, can be measured in a number of biological fluids including bronchoalveolar lavage fluid (BALF) from asthmatic patients. In humans, pretreatment with zileuton attenuated bronchoconstriction caused by cold air challenge in patients with asthma.
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 airways of asthmatic patients. Zileuton relieves such symptoms through its selective inhibition of 5-lipoxygenase, the enzyme that catalyzes the formation of leukotrienes from arachidonic acid. Specifically, it inhibits leukotriene LTB4, LTC4, LTD4, and LTE4 formation. Both the R(+) and S(-) enantiomers are pharmacologically active as 5-lipoxygenase inhibitors in in vitro systems.
Indication: For the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.
Half Life: 2.5 hours
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Data Correlations | 2 studies

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Genes category icon Genes
Score Help
ALOX15 100 100
APOA2 100 100
RPL37A 95 95
LIPC 92 92
BOLA1 90 90
FKBP1A 86 86
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Biogroups category icon Biogroups
Score Help
Lipoxygenase, LH2 100 100
Lipase/lipooxygenase, PLAT/LH2 100 100
Linoleic Acid Metabolism 98 98
Arachidonic Acid Metabolism 97 97
Prostaglandin and Leukotriene Metab… 97 97
Eicosanoid Synthesis 97 97
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Individual Studies

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    The DrugBank database is a unique bioinformatics and cheminformatics resource that combines detailed drug (i.e. chemical, pharmacological and pharmaceutical) data with comprehensive drug target (i.e. sequence, structure, and pathway) information.

    Authors: David S Wishart, Craig Knox, An Chi Guo et al.

    Organization: Department of Computing Science, Univers…

  • Liver Pharmacology and Xenobiotic Response Repertoire

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    A definition of RNA expression changes that correlate with liver response programs and an understanding of the similarities and differences in responses to different classes of chemicals would aid in new chemical or drug characterization and add to our understanding of liver biology.

    Authors: Natsoulis G, Pearson CI, Gollub J et al.

    Organization: Iconix Biosciences 325 E. Middlefield Rd…
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Associated Researchers

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Thought leaders and organizations working on research involving Zileuton.

View All Author iconAuthors
  • L M DubĂ©
  • Karen Walton-Bowen
  • Salvatore Cuzzocrea
  • Rosanna Di Paola
  • Gary D Anderson
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Critical Therapeutics
  • Children's Oncology Group
  • National Heart, Lung, and Blood Institute (NHLBI)
  • Merck
  • Barbara Ann Karmanos Cancer Institute
View All Affiliations icon Organizations
  • University of Virginia
  • Zhejiang University
  • National Institutes of Health
  • University of South Alabama Medical Center
  • University of Messina

Clinical Trials | 35 trials

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