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Identification
NameZileuton
Accession NumberDB00744  (APRD00265)
TypeSmall Molecule
GroupsApproved, Investigational, Withdrawn
DescriptionLeukotrienes 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. The immediate release tablet of Zileuton has been withdrawn from the US market.
Structure
Thumb
Synonyms
(+-)-1-(1-Benzo[b]thien-2-ylethyl)-1-hydroxyurea
Leutrol
N-(1-Benzo(b)thien-2-ylethyl)-N-hydroxyurea
N-[1-(Benzo[b]thiophen-2-yl)ethyl]-N-hydroxyurea
Zileuton
Zileuton
Zileutonum
Zyflo
External Identifiers
  • A 64077
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zyflotablet600 mg/1oralChiesi USA, Inc.1996-12-06Not applicableUs
Zyflo CRtablet, multilayer, extended release600 mg/1oralChiesi USA, Inc.2007-05-30Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIV1L22WVE2S
CAS number111406-87-2
WeightAverage: 236.29
Monoisotopic: 236.061948328
Chemical FormulaC11H12N2O2S
InChI KeyInChIKey=MWLSOWXNZPKENC-UHFFFAOYSA-N
InChI
InChI=1S/C11H12N2O2S/c1-7(13(15)11(12)14)10-6-8-4-2-3-5-9(8)16-10/h2-7,15H,1H3,(H2,12,14)
IUPAC Name
1-[1-(1-benzothiophen-2-yl)ethyl]-1-hydroxyurea
SMILES
CC(N(O)C(N)=O)C1=CC2=CC=CC=C2S1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzothiophenes. These are organic compounds containing a benzene fused to a thiepine ring (a five-membered ring with six carbon atoms and one sulfur atom).
KingdomOrganic compounds
Super ClassOrganoheterocyclic compounds
ClassBenzothiophenes
Sub ClassNot Available
Direct ParentBenzothiophenes
Alternative Parents
Substituents
  • Benzothiophene
  • 2,3,5-trisubstituted thiophene
  • Benzenoid
  • Heteroaromatic compound
  • Thiophene
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External DescriptorsNot Available
Pharmacology
IndicationFor the prophylaxis and chronic treatment of asthma in adults and children 12 years of age and older.
PharmacodynamicsZileuton 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 endogenous inflammatory mediators, including leukotrienes. Sulfido-peptide leukotrienes (LTC4, LTD4, LTE4, also known as the slow-releasing substances of anaphylaxis) and LTB4, a chemoattractant for neutrophils and eosinophils, are derived from the initial unstable product of arachidonic acid metabolism, leukotriene A4 (LTA4), and 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 actionLeukotrienes 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. Due to the role of leukotrienes in the pathogenesis of asthma, modulation of leukotriene formation by interruption of 5-lipoxygenase activity may reduce airway symptoms, decrease bronchial smooth muscle tone, and improve asthma control.
Related Articles
AbsorptionRapidly and almost completely absorbed. The absolute bioavailability is unknown.
Volume of distribution
  • 1.2 L/kg
Protein binding93% bound to plasma proteins, primarily to albumin.
Metabolism

Hepatic. Zileuton and its N-dehydroxylated metabolite are oxidatively metabolized by the cytochrome P450 isoenzymes 1A2, 2C9 and 3A4.

SubstrateEnzymesProduct
Zileuton
HydroxyzileutonDetails
Zileuton
Zileuton sulfoxideDetails
Zileuton
DehydroxyzyleutonDetails
Zileuton
Zileuton O-glucuronideDetails
Dehydroxyzyleuton
Dehydroxyzileuton sulfoxideDetails
Route of eliminationElimination 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 life2.5 hours
Clearance
  • Apparent oral cl=7 mL/min/kg
ToxicityThe 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
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9915
Blood Brain Barrier+0.8846
Caco-2 permeable-0.5793
P-glycoprotein substrateNon-substrate0.6789
P-glycoprotein inhibitor INon-inhibitor0.9684
P-glycoprotein inhibitor IINon-inhibitor0.9765
Renal organic cation transporterNon-inhibitor0.9583
CYP450 2C9 substrateNon-substrate0.5907
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateNon-substrate0.6384
CYP450 1A2 substrateInhibitor0.5318
CYP450 2C9 inhibitorNon-inhibitor0.7975
CYP450 2D6 inhibitorNon-inhibitor0.8866
CYP450 2C19 inhibitorNon-inhibitor0.6451
CYP450 3A4 inhibitorNon-inhibitor0.7062
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5821
Ames testAMES toxic0.5865
CarcinogenicityNon-carcinogens0.7968
BiodegradationNot ready biodegradable0.985
Rat acute toxicity2.2646 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9884
hERG inhibition (predictor II)Non-inhibitor0.9051
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Cornerstone therapeutics inc
Packagers
Dosage forms
FormRouteStrength
Tabletoral600 mg/1
Tablet, multilayer, extended releaseoral600 mg/1
Prices
Unit descriptionCostUnit
Zyflo 600 mg tablet6.49USD tablet
Zyflo CR 600 mg 12 Hour tablet6.23USD tablet
Zyflo 600 mg filmtab5.99USD tablet
Zyflo cr 600 mg tablet5.99USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4873259 No1993-12-092010-12-09Us
US5422123 No1995-06-062012-06-06Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point144.2-145.2 °CNot Available
water solubilityPractically insoluble (0.5 mg/ml)Not Available
logP0.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0539 mg/mLALOGPS
logP2.01ALOGPS
logP2.01ChemAxon
logS-3.6ALOGPS
pKa (Strongest Acidic)8.84ChemAxon
pKa (Strongest Basic)-5.5ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area66.56 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity61.96 m3·mol-1ChemAxon
Polarizability24.14 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
References
Synthesis Reference

Emanuele ATTOLINA, Gianmaria Dell’Anna, Roberto Rossi, Pietro Allegrini, Gabriele Razzetti, “PROCESS FOR THE PREPARATION OF ZILEUTON.” U.S. Patent US20090286996, issued November 19, 2009.

US20090286996
General References
  1. Berger W, De Chandt MT, Cairns CB: Zileuton: clinical implications of 5-Lipoxygenase inhibition in severe airway disease. Int J Clin Pract. 2007 Apr;61(4):663-76. [PubMed:17394438 ]
  2. Wenzel SE, Kamada AK: Zileuton: the first 5-lipoxygenase inhibitor for the treatment of asthma. Ann Pharmacother. 1996 Jul-Aug;30(7-8):858-64. [PubMed:8826571 ]
  3. Malo PE, Bell RL, Shaughnessy TK, Summers JB, Brooks DW, Carter GW: The 5-lipoxygenase inhibitory activity of zileuton in in vitro and in vivo models of antigen-induced airway anaphylaxis. Pulm Pharmacol. 1994 Apr;7(2):73-9. [PubMed:8081074 ]
External Links
ATC CodesNot Available
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (129 KB)
MSDSDownload (14.8 KB)
Interactions
Drug Interactions
Drug
AbciximabZileuton may increase the anticoagulant activities of Abciximab.
AbirateroneThe serum concentration of Zileuton can be increased when it is combined with Abiraterone.
AcebutololZileuton may decrease the antihypertensive activities of Acebutolol.
AceclofenacThe risk or severity of adverse effects can be increased when Zileuton is combined with Aceclofenac.
AcenocoumarolZileuton may increase the anticoagulant activities of Acenocoumarol.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Acetylsalicylic acid.
AdapaleneThe risk or severity of adverse effects can be increased when Adapalene is combined with Zileuton.
Alendronic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Alendronic acid.
AliskirenZileuton may decrease the antihypertensive activities of Aliskiren.
AlprenololZileuton may decrease the antihypertensive activities of Alprenolol.
AlprostadilThe therapeutic efficacy of Alprostadil can be decreased when used in combination with Zileuton.
AmikacinZileuton may decrease the excretion rate of Amikacin which could result in a lower serum level and potentially a reduction in efficacy.
AmilorideZileuton may decrease the antihypertensive activities of Amiloride.
AmiodaroneThe metabolism of Zileuton can be decreased when combined with Amiodarone.
AncrodZileuton may increase the anticoagulant activities of Ancrod.
AntipyrineThe risk or severity of adverse effects can be increased when Zileuton is combined with Antipyrine.
Antithrombin III humanZileuton may increase the anticoagulant activities of Antithrombin III human.
ApixabanZileuton may increase the anticoagulant activities of Apixaban.
ApremilastThe risk or severity of adverse effects can be increased when Zileuton is combined with Apremilast.
AprepitantThe serum concentration of Zileuton can be increased when it is combined with Aprepitant.
ArdeparinZileuton may increase the anticoagulant activities of Ardeparin.
ArgatrobanZileuton may increase the anticoagulant activities of Argatroban.
ArotinololZileuton may decrease the antihypertensive activities of Arotinolol.
AtazanavirThe metabolism of Zileuton can be decreased when combined with Atazanavir.
AtenololZileuton may decrease the antihypertensive activities of Atenolol.
AtomoxetineThe metabolism of Zileuton can be decreased when combined with Atomoxetine.
AzapropazoneThe risk or severity of adverse effects can be increased when Zileuton is combined with Azapropazone.
AzelastineThe risk or severity of adverse effects can be increased when Zileuton is combined with Azelastine.
Azilsartan medoxomilThe risk or severity of adverse effects can be increased when Azilsartan medoxomil is combined with Zileuton.
AzithromycinThe metabolism of Zileuton can be decreased when combined with Azithromycin.
BalsalazideZileuton may increase the nephrotoxic activities of Balsalazide.
BalsalazideThe risk or severity of adverse effects can be increased when Balsalazide is combined with Zileuton.
BecaplerminZileuton may increase the anticoagulant activities of Becaplermin.
BefunololZileuton may decrease the antihypertensive activities of Befunolol.
BenazeprilThe risk or severity of adverse effects can be increased when Benazepril is combined with Zileuton.
BendroflumethiazideThe therapeutic efficacy of Bendroflumethiazide can be decreased when used in combination with Zileuton.
BenoxaprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Benoxaprofen.
BetaxololZileuton may decrease the antihypertensive activities of Betaxolol.
BevantololZileuton may decrease the antihypertensive activities of Bevantolol.
BexaroteneThe serum concentration of Zileuton can be decreased when it is combined with Bexarotene.
BimatoprostThe therapeutic efficacy of Bimatoprost can be decreased when used in combination with Zileuton.
BisoprololZileuton may decrease the antihypertensive activities of Bisoprolol.
BivalirudinZileuton may increase the anticoagulant activities of Bivalirudin.
BoceprevirThe metabolism of Zileuton can be decreased when combined with Boceprevir.
BopindololZileuton may decrease the antihypertensive activities of Bopindolol.
BortezomibThe metabolism of Zileuton can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Zileuton can be decreased when it is combined with Bosentan.
BromfenacThe risk or severity of adverse effects can be increased when Zileuton is combined with Bromfenac.
BufuralolZileuton may decrease the antihypertensive activities of Bufuralol.
BumetanideZileuton may decrease the diuretic activities of Bumetanide.
BupranololZileuton may decrease the antihypertensive activities of Bupranolol.
CaffeineThe metabolism of Zileuton can be decreased when combined with Caffeine.
CandesartanThe risk or severity of adverse effects can be increased when Candesartan is combined with Zileuton.
CandoxatrilThe risk or severity of adverse effects can be increased when Candoxatril is combined with Zileuton.
CapecitabineThe metabolism of Zileuton can be decreased when combined with Capecitabine.
CaptoprilThe risk or severity of adverse effects can be increased when Captopril is combined with Zileuton.
CarbamazepineThe metabolism of Zileuton can be increased when combined with Carbamazepine.
Carboprost TromethamineThe therapeutic efficacy of Carboprost Tromethamine can be decreased when used in combination with Zileuton.
CarprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Carprofen.
CarteololZileuton may decrease the antihypertensive activities of Carteolol.
CarvedilolZileuton may decrease the antihypertensive activities of Carvedilol.
CastanospermineThe risk or severity of adverse effects can be increased when Zileuton is combined with Castanospermine.
CelecoxibThe risk or severity of adverse effects can be increased when Celecoxib is combined with Zileuton.
CeliprololZileuton may decrease the antihypertensive activities of Celiprolol.
CeritinibThe serum concentration of Zileuton can be increased when it is combined with Ceritinib.
CertoparinZileuton may increase the anticoagulant activities of Certoparin.
ChloroquineThe risk or severity of adverse effects can be increased when Chloroquine is combined with Zileuton.
ChlorothiazideThe therapeutic efficacy of Chlorothiazide can be decreased when used in combination with Zileuton.
ChlorthalidoneThe therapeutic efficacy of Chlorthalidone can be decreased when used in combination with Zileuton.
CholecalciferolThe metabolism of Zileuton can be decreased when combined with Cholecalciferol.
CholestyramineCholestyramine can cause a decrease in the absorption of Zileuton resulting in a reduced serum concentration and potentially a decrease in efficacy.
CilazaprilThe risk or severity of adverse effects can be increased when Cilazapril is combined with Zileuton.
CitalopramThe metabolism of Zileuton can be decreased when combined with Citalopram.
Citric AcidZileuton may increase the anticoagulant activities of Citric Acid.
ClarithromycinThe metabolism of Zileuton can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Zileuton can be decreased when combined with Clemastine.
ClodronateThe risk or severity of adverse effects can be increased when Zileuton is combined with Clodronate.
ClonixinThe risk or severity of adverse effects can be increased when Zileuton is combined with Clonixin.
CloprostenolThe therapeutic efficacy of Cloprostenol can be decreased when used in combination with Zileuton.
ClotrimazoleThe metabolism of Zileuton can be decreased when combined with Clotrimazole.
CobicistatThe metabolism of Zileuton can be decreased when combined with Cobicistat.
ColesevelamColesevelam can cause a decrease in the absorption of Zileuton resulting in a reduced serum concentration and potentially a decrease in efficacy.
ColestipolColestipol can cause a decrease in the absorption of Zileuton resulting in a reduced serum concentration and potentially a decrease in efficacy.
ConivaptanThe serum concentration of Zileuton can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Zileuton can be decreased when combined with Crizotinib.
CyclosporineZileuton may increase the nephrotoxic activities of Cyclosporine.
CyclosporineThe metabolism of Zileuton can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Zileuton can be decreased when it is combined with Cyproterone acetate.
D-LimoneneThe risk or severity of adverse effects can be increased when Zileuton is combined with D-Limonene.
Dabigatran etexilateZileuton may increase the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Zileuton can be decreased when it is combined with Dabrafenib.
DalteparinZileuton may increase the anticoagulant activities of Dalteparin.
DanaparoidZileuton may increase the anticoagulant activities of Danaparoid.
DarunavirThe metabolism of Zileuton can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Zileuton can be increased when it is combined with Dasatinib.
DaunorubicinZileuton may decrease the excretion rate of Daunorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DeferasiroxThe serum concentration of Zileuton can be decreased when it is combined with Deferasirox.
DeferasiroxThe risk or severity of adverse effects can be increased when Zileuton is combined with Deferasirox.
DelavirdineThe metabolism of Zileuton can be decreased when combined with Delavirdine.
DesirudinZileuton may increase the anticoagulant activities of Desirudin.
DesmopressinThe risk or severity of adverse effects can be increased when Zileuton is combined with Desmopressin.
DexamethasoneThe serum concentration of Zileuton can be decreased when it is combined with Dexamethasone.
DexketoprofenThe risk or severity of adverse effects can be increased when Dexketoprofen is combined with Zileuton.
DextranZileuton may increase the anticoagulant activities of Dextran.
Dextran 40Zileuton may increase the anticoagulant activities of Dextran 40.
Dextran 70Zileuton may increase the anticoagulant activities of Dextran 70.
Dextran 75Zileuton may increase the anticoagulant activities of Dextran 75.
DiclofenacThe risk or severity of adverse effects can be increased when Diclofenac is combined with Zileuton.
DicoumarolZileuton may increase the anticoagulant activities of Dicoumarol.
DiflunisalThe risk or severity of adverse effects can be increased when Zileuton is combined with Diflunisal.
DigoxinThe serum concentration of Digoxin can be increased when it is combined with Zileuton.
DihydroergotamineThe metabolism of Zileuton can be decreased when combined with Dihydroergotamine.
DihydrostreptomycinZileuton may decrease the excretion rate of Dihydrostreptomycin which could result in a lower serum level and potentially a reduction in efficacy.
DiltiazemThe metabolism of Zileuton can be decreased when combined with Diltiazem.
DinoprostoneThe therapeutic efficacy of Dinoprostone can be decreased when used in combination with Zileuton.
DoxorubicinZileuton may decrease the excretion rate of Doxorubicin which could result in a lower serum level and potentially a reduction in efficacy.
DoxycyclineThe metabolism of Zileuton can be decreased when combined with Doxycycline.
DronedaroneThe metabolism of Zileuton can be decreased when combined with Dronedarone.
DrospirenoneZileuton may increase the hyperkalemic activities of Drospirenone.
DroxicamThe risk or severity of adverse effects can be increased when Zileuton is combined with Droxicam.
Edetic AcidZileuton may increase the anticoagulant activities of Edetic Acid.
EdoxabanZileuton may increase the anticoagulant activities of Edoxaban.
EfavirenzThe serum concentration of Zileuton can be decreased when it is combined with Efavirenz.
EnalaprilThe risk or severity of adverse effects can be increased when Enalapril is combined with Zileuton.
EnalaprilatThe risk or severity of adverse effects can be increased when Enalaprilat is combined with Zileuton.
EnoxaparinZileuton may increase the anticoagulant activities of Enoxaparin.
EnzalutamideThe serum concentration of Zileuton can be decreased when it is combined with Enzalutamide.
EpirizoleThe risk or severity of adverse effects can be increased when Zileuton is combined with Epirizole.
EpirubicinZileuton may decrease the excretion rate of Epirubicin which could result in a lower serum level and potentially a reduction in efficacy.
EplerenoneZileuton may decrease the antihypertensive activities of Eplerenone.
EpoprostenolThe therapeutic efficacy of Epoprostenol can be decreased when used in combination with Zileuton.
EprosartanThe risk or severity of adverse effects can be increased when Eprosartan is combined with Zileuton.
ErythromycinThe metabolism of Zileuton can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Zileuton can be decreased when it is combined with Eslicarbazepine acetate.
EsmololZileuton may decrease the antihypertensive activities of Esmolol.
Etacrynic acidZileuton may decrease the diuretic activities of Etacrynic acid.
EtanerceptThe risk or severity of adverse effects can be increased when Etanercept is combined with Zileuton.
Ethyl biscoumacetateZileuton may increase the anticoagulant activities of Ethyl biscoumacetate.
Etidronic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Etidronic acid.
EtodolacThe risk or severity of adverse effects can be increased when Zileuton is combined with Etodolac.
EtofenamateThe risk or severity of adverse effects can be increased when Zileuton is combined with Etofenamate.
EtoricoxibThe risk or severity of adverse effects can be increased when Zileuton is combined with Etoricoxib.
EtravirineThe serum concentration of Zileuton can be decreased when it is combined with Etravirine.
Evening primrose oilThe risk or severity of adverse effects can be increased when Zileuton is combined with Evening primrose oil.
exisulindThe risk or severity of adverse effects can be increased when Zileuton is combined with exisulind.
FenbufenThe risk or severity of adverse effects can be increased when Zileuton is combined with Fenbufen.
FenoprofenThe risk or severity of adverse effects can be increased when Fenoprofen is combined with Zileuton.
FloctafenineThe risk or severity of adverse effects can be increased when Floctafenine is combined with Zileuton.
FloxuridineThe metabolism of Zileuton can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Zileuton can be decreased when combined with Fluconazole.
FlunixinThe risk or severity of adverse effects can be increased when Zileuton is combined with Flunixin.
FluorouracilThe metabolism of Zileuton can be decreased when combined with Fluorouracil.
FlurbiprofenThe risk or severity of adverse effects can be increased when Flurbiprofen is combined with Zileuton.
FluvastatinThe metabolism of Zileuton can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Zileuton can be decreased when combined with Fluvoxamine.
Folic AcidThe therapeutic efficacy of Folic Acid can be decreased when used in combination with Zileuton.
Fondaparinux sodiumZileuton may increase the anticoagulant activities of Fondaparinux sodium.
ForasartanThe risk or severity of adverse effects can be increased when Forasartan is combined with Zileuton.
FosamprenavirThe metabolism of Zileuton can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Zileuton can be increased when it is combined with Fosaprepitant.
FosinoprilThe risk or severity of adverse effects can be increased when Fosinopril is combined with Zileuton.
FosphenytoinThe metabolism of Zileuton can be increased when combined with Fosphenytoin.
FramycetinZileuton may decrease the excretion rate of Framycetin which could result in a lower serum level and potentially a reduction in efficacy.
FurosemideZileuton may decrease the diuretic activities of Furosemide.
Fusidic AcidThe serum concentration of Zileuton can be increased when it is combined with Fusidic Acid.
GemeprostThe therapeutic efficacy of Gemeprost can be decreased when used in combination with Zileuton.
GemfibrozilThe metabolism of Zileuton can be decreased when combined with Gemfibrozil.
GentamicinZileuton may decrease the excretion rate of Gentamicin which could result in a lower serum level and potentially a reduction in efficacy.
HaloperidolThe risk or severity of adverse effects can be increased when Zileuton is combined with Haloperidol.
HeparinZileuton may increase the anticoagulant activities of Heparin.
HirulogZileuton may increase the anticoagulant activities of Hirulog.
HMPL-004The risk or severity of adverse effects can be increased when Zileuton is combined with HMPL-004.
HydralazineZileuton may decrease the antihypertensive activities of Hydralazine.
HydrochlorothiazideThe therapeutic efficacy of Hydrochlorothiazide can be decreased when used in combination with Zileuton.
HydroflumethiazideThe therapeutic efficacy of Hydroflumethiazide can be decreased when used in combination with Zileuton.
Hygromycin BZileuton may decrease the excretion rate of Hygromycin B which could result in a lower serum level and potentially a reduction in efficacy.
IbandronateThe risk or severity of adverse effects can be increased when Zileuton is combined with Ibandronate.
IbuprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Ibuprofen.
IbuproxamThe risk or severity of adverse effects can be increased when Zileuton is combined with Ibuproxam.
IcatibantThe risk or severity of adverse effects can be increased when Zileuton is combined with Icatibant.
IdarubicinZileuton may decrease the excretion rate of Idarubicin which could result in a lower serum level and potentially a reduction in efficacy.
IdelalisibThe serum concentration of Zileuton can be increased when it is combined with Idelalisib.
IloprostThe therapeutic efficacy of Iloprost can be decreased when used in combination with Zileuton.
ImatinibThe metabolism of Zileuton can be decreased when combined with Imatinib.
IndapamideThe therapeutic efficacy of Indapamide can be decreased when used in combination with Zileuton.
IndenololZileuton may decrease the antihypertensive activities of Indenolol.
IndinavirThe metabolism of Zileuton can be decreased when combined with Indinavir.
IndomethacinThe risk or severity of adverse effects can be increased when Indomethacin is combined with Zileuton.
IndoprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Indoprofen.
IrbesartanThe risk or severity of adverse effects can be increased when Irbesartan is combined with Zileuton.
IsavuconazoniumThe metabolism of Zileuton can be decreased when combined with Isavuconazonium.
IsoxicamThe risk or severity of adverse effects can be increased when Zileuton is combined with Isoxicam.
IsradipineThe metabolism of Zileuton can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Zileuton can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Zileuton can be increased when it is combined with Ivacaftor.
KanamycinZileuton may decrease the excretion rate of Kanamycin which could result in a lower serum level and potentially a reduction in efficacy.
KebuzoneThe risk or severity of adverse effects can be increased when Zileuton is combined with Kebuzone.
KetoconazoleThe metabolism of Zileuton can be decreased when combined with Ketoconazole.
KetoprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Ketoprofen.
KetorolacThe risk or severity of adverse effects can be increased when Ketorolac is combined with Zileuton.
LabetalolZileuton may decrease the antihypertensive activities of Labetalol.
LeflunomideThe risk or severity of adverse effects can be increased when Zileuton is combined with Leflunomide.
LepirudinZileuton may increase the anticoagulant activities of Lepirudin.
LevobunololZileuton may decrease the antihypertensive activities of Levobunolol.
LidocaineThe metabolism of Zileuton can be decreased when combined with Lidocaine.
LisinoprilThe risk or severity of adverse effects can be increased when Lisinopril is combined with Zileuton.
LithiumThe serum concentration of Lithium can be increased when it is combined with Zileuton.
LopinavirThe metabolism of Zileuton can be decreased when combined with Lopinavir.
LornoxicamThe risk or severity of adverse effects can be increased when Zileuton is combined with Lornoxicam.
LosartanThe risk or severity of adverse effects can be increased when Losartan is combined with Zileuton.
LovastatinThe metabolism of Zileuton can be decreased when combined with Lovastatin.
LoxoprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Loxoprofen.
LubiprostoneThe therapeutic efficacy of Lubiprostone can be decreased when used in combination with Zileuton.
LuliconazoleThe serum concentration of Zileuton can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Zileuton can be decreased when it is combined with Lumacaftor.
LumiracoxibThe risk or severity of adverse effects can be increased when Zileuton is combined with Lumiracoxib.
Magnesium salicylateThe risk or severity of adverse effects can be increased when Zileuton is combined with Magnesium salicylate.
MasoprocolThe risk or severity of adverse effects can be increased when Masoprocol is combined with Zileuton.
Meclofenamic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Meclofenamic acid.
Mefenamic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Mefenamic acid.
MeloxicamThe risk or severity of adverse effects can be increased when Zileuton is combined with Meloxicam.
MesalazineZileuton may increase the nephrotoxic activities of Mesalazine.
MesalazineThe risk or severity of adverse effects can be increased when Mesalazine is combined with Zileuton.
MetamizoleThe risk or severity of adverse effects can be increased when Zileuton is combined with Metamizole.
MethotrexateThe serum concentration of Methotrexate can be increased when it is combined with Zileuton.
MethyclothiazideThe therapeutic efficacy of Methyclothiazide can be decreased when used in combination with Zileuton.
MetipranololZileuton may decrease the antihypertensive activities of Metipranolol.
MetolazoneThe therapeutic efficacy of Metolazone can be decreased when used in combination with Zileuton.
MetoprololZileuton may decrease the antihypertensive activities of Metoprolol.
MetrizamideZileuton may decrease the excretion rate of Metrizamide which could result in a lower serum level and potentially a reduction in efficacy.
MexiletineThe metabolism of Zileuton can be decreased when combined with Mexiletine.
MifepristoneThe metabolism of Zileuton can be decreased when combined with Mifepristone.
MisoprostolThe therapeutic efficacy of Misoprostol can be decreased when used in combination with Zileuton.
MitotaneThe serum concentration of Zileuton can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Zileuton can be decreased when it is combined with Modafinil.
MoexiprilThe risk or severity of adverse effects can be increased when Moexipril is combined with Zileuton.
MorniflumateThe risk or severity of adverse effects can be increased when Morniflumate is combined with Zileuton.
Mycophenolate mofetilThe risk or severity of adverse effects can be increased when Mycophenolate mofetil is combined with Zileuton.
Mycophenolic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Mycophenolic acid.
NabumetoneThe risk or severity of adverse effects can be increased when Nabumetone is combined with Zileuton.
NadololZileuton may decrease the antihypertensive activities of Nadolol.
NadroparinZileuton may increase the anticoagulant activities of Nadroparin.
NafcillinThe serum concentration of Zileuton can be decreased when it is combined with Nafcillin.
NaftifineThe risk or severity of adverse effects can be increased when Naftifine is combined with Zileuton.
NaproxenThe risk or severity of adverse effects can be increased when Zileuton is combined with Naproxen.
NCX 4016The risk or severity of adverse effects can be increased when Zileuton is combined with NCX 4016.
NefazodoneThe metabolism of Zileuton can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Zileuton can be decreased when combined with Nelfinavir.
NeomycinZileuton may decrease the excretion rate of Neomycin which could result in a lower serum level and potentially a reduction in efficacy.
NepafenacThe risk or severity of adverse effects can be increased when Zileuton is combined with Nepafenac.
NetilmicinZileuton may decrease the excretion rate of Netilmicin which could result in a lower serum level and potentially a reduction in efficacy.
NetupitantThe serum concentration of Zileuton can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Zileuton can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Zileuton can be decreased when combined with Nicardipine.
Niflumic AcidThe risk or severity of adverse effects can be increased when Zileuton is combined with Niflumic Acid.
NilotinibThe metabolism of Zileuton can be decreased when combined with Nilotinib.
NimesulideThe risk or severity of adverse effects can be increased when Zileuton is combined with Nimesulide.
OlaparibThe metabolism of Zileuton can be decreased when combined with Olaparib.
OlmesartanThe risk or severity of adverse effects can be increased when Olmesartan is combined with Zileuton.
OlopatadineThe risk or severity of adverse effects can be increased when Zileuton is combined with Olopatadine.
OlsalazineZileuton may increase the nephrotoxic activities of Olsalazine.
OlsalazineThe risk or severity of adverse effects can be increased when Olsalazine is combined with Zileuton.
Omacetaxine mepesuccinateThe risk or severity of adverse effects can be increased when Zileuton is combined with Omacetaxine mepesuccinate.
OmapatrilatThe risk or severity of adverse effects can be increased when Omapatrilat is combined with Zileuton.
OmeprazoleThe metabolism of Zileuton can be decreased when combined with Omeprazole.
OrgoteinThe risk or severity of adverse effects can be increased when Zileuton is combined with Orgotein.
OsimertinibThe serum concentration of Zileuton can be increased when it is combined with Osimertinib.
OtamixabanZileuton may increase the anticoagulant activities of Otamixaban.
OxaprozinThe risk or severity of adverse effects can be increased when Zileuton is combined with Oxaprozin.
OxprenololZileuton may decrease the antihypertensive activities of Oxprenolol.
OxyphenbutazoneThe risk or severity of adverse effects can be increased when Zileuton is combined with Oxyphenbutazone.
PalbociclibThe serum concentration of Zileuton can be increased when it is combined with Palbociclib.
PamidronateThe risk or severity of adverse effects can be increased when Zileuton is combined with Pamidronate.
ParecoxibThe risk or severity of adverse effects can be increased when Zileuton is combined with Parecoxib.
ParomomycinZileuton may decrease the excretion rate of Paromomycin which could result in a lower serum level and potentially a reduction in efficacy.
Peginterferon alfa-2bThe serum concentration of Zileuton can be increased when it is combined with Peginterferon alfa-2b.
PenbutololZileuton may decrease the antihypertensive activities of Penbutolol.
PentobarbitalThe metabolism of Zileuton can be increased when combined with Pentobarbital.
Pentosan PolysulfateZileuton may increase the anticoagulant activities of Pentosan Polysulfate.
PerindoprilThe risk or severity of adverse effects can be increased when Perindopril is combined with Zileuton.
PhenindioneZileuton may increase the anticoagulant activities of Phenindione.
PhenobarbitalThe metabolism of Zileuton can be increased when combined with Phenobarbital.
PhenprocoumonZileuton may increase the anticoagulant activities of Phenprocoumon.
PhenylbutazoneThe risk or severity of adverse effects can be increased when Zileuton is combined with Phenylbutazone.
PhenytoinThe metabolism of Zileuton can be increased when combined with Phenytoin.
PimecrolimusThe risk or severity of adverse effects can be increased when Pimecrolimus is combined with Zileuton.
PimozideThe serum concentration of Pimozide can be increased when it is combined with Zileuton.
PindololZileuton may decrease the antihypertensive activities of Pindolol.
PiretanideZileuton may decrease the diuretic activities of Piretanide.
PirfenidoneThe risk or severity of adverse effects can be increased when Zileuton is combined with Pirfenidone.
PiroxicamThe risk or severity of adverse effects can be increased when Piroxicam is combined with Zileuton.
PlicamycinZileuton may decrease the excretion rate of Plicamycin which could result in a lower serum level and potentially a reduction in efficacy.
PolythiazideThe therapeutic efficacy of Polythiazide can be decreased when used in combination with Zileuton.
PosaconazoleThe metabolism of Zileuton can be decreased when combined with Posaconazole.
PractololZileuton may decrease the antihypertensive activities of Practolol.
PralatrexateThe serum concentration of Pralatrexate can be increased when it is combined with Zileuton.
PrimidoneThe metabolism of Zileuton can be increased when combined with Primidone.
ProbenecidThe serum concentration of Zileuton can be increased when it is combined with Probenecid.
PropacetamolThe risk or severity of adverse effects can be increased when Zileuton is combined with Propacetamol.
PropranololThe serum concentration of Propranolol can be increased when it is combined with Zileuton.
Prostaglandin D2The therapeutic efficacy of Prostaglandin D2 can be decreased when used in combination with Zileuton.
Protein CZileuton may increase the anticoagulant activities of Protein C.
ProtocatechualdehydeZileuton may increase the anticoagulant activities of Protocatechualdehyde.
PTC299The risk or severity of adverse effects can be increased when Zileuton is combined with PTC299.
PuromycinZileuton may decrease the excretion rate of Puromycin which could result in a lower serum level and potentially a reduction in efficacy.
PyrimethamineThe metabolism of Zileuton can be decreased when combined with Pyrimethamine.
QuinaprilThe risk or severity of adverse effects can be increased when Quinapril is combined with Zileuton.
QuinethazoneThe therapeutic efficacy of Quinethazone can be decreased when used in combination with Zileuton.
QuinineThe metabolism of Zileuton can be decreased when combined with Quinine.
RamiprilThe risk or severity of adverse effects can be increased when Ramipril is combined with Zileuton.
RanolazineThe metabolism of Zileuton can be decreased when combined with Ranolazine.
RescinnamineThe risk or severity of adverse effects can be increased when Rescinnamine is combined with Zileuton.
ResveratrolThe risk or severity of adverse effects can be increased when Zileuton is combined with Resveratrol.
ReviparinZileuton may increase the anticoagulant activities of Reviparin.
RibostamycinZileuton may decrease the excretion rate of Ribostamycin which could result in a lower serum level and potentially a reduction in efficacy.
RifabutinThe metabolism of Zileuton can be increased when combined with Rifabutin.
RifampicinThe metabolism of Zileuton can be increased when combined with Rifampicin.
RifapentineThe metabolism of Zileuton can be increased when combined with Rifapentine.
RisedronateThe risk or severity of adverse effects can be increased when Zileuton is combined with Risedronate.
RitonavirThe metabolism of Zileuton can be decreased when combined with Ritonavir.
RivaroxabanZileuton may increase the anticoagulant activities of Rivaroxaban.
RofecoxibThe risk or severity of adverse effects can be increased when Rofecoxib is combined with Zileuton.
RopiniroleThe metabolism of Zileuton can be decreased when combined with Ropinirole.
SalicylamideThe risk or severity of adverse effects can be increased when Zileuton is combined with Salicylamide.
Salicylic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Salicylic acid.
SalsalateThe risk or severity of adverse effects can be increased when Zileuton is combined with Salsalate.
SaprisartanThe risk or severity of adverse effects can be increased when Saprisartan is combined with Zileuton.
SaquinavirThe metabolism of Zileuton can be decreased when combined with Saquinavir.
SaralasinThe risk or severity of adverse effects can be increased when Saralasin is combined with Zileuton.
SecobarbitalThe metabolism of Zileuton can be increased when combined with Secobarbital.
SeratrodastThe risk or severity of adverse effects can be increased when Zileuton is combined with Seratrodast.
SildenafilThe metabolism of Zileuton can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Zileuton can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Zileuton can be increased when it is combined with Simeprevir.
SorafenibThe metabolism of Zileuton can be decreased when combined with Sorafenib.
SotalolZileuton may decrease the antihypertensive activities of Sotalol.
SpectinomycinZileuton may decrease the excretion rate of Spectinomycin which could result in a lower serum level and potentially a reduction in efficacy.
SpiraprilThe risk or severity of adverse effects can be increased when Spirapril is combined with Zileuton.
SpironolactoneZileuton may decrease the antihypertensive activities of Spironolactone.
SRT501The risk or severity of adverse effects can be increased when Zileuton is combined with SRT501.
St. John's WortThe serum concentration of Zileuton can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Zileuton can be increased when it is combined with Stiripentol.
StreptomycinZileuton may decrease the excretion rate of Streptomycin which could result in a lower serum level and potentially a reduction in efficacy.
StreptozocinZileuton may decrease the excretion rate of Streptozocin which could result in a lower serum level and potentially a reduction in efficacy.
SulfadiazineThe metabolism of Zileuton can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Zileuton can be decreased when combined with Sulfamethoxazole.
SulfasalazineZileuton may increase the nephrotoxic activities of Sulfasalazine.
SulfasalazineThe risk or severity of adverse effects can be increased when Sulfasalazine is combined with Zileuton.
SulfisoxazoleThe metabolism of Zileuton can be decreased when combined with Sulfisoxazole.
SulindacThe risk or severity of adverse effects can be increased when Sulindac is combined with Zileuton.
SulodexideZileuton may increase the anticoagulant activities of Sulodexide.
SuprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Suprofen.
TacrolimusZileuton may increase the nephrotoxic activities of Tacrolimus.
TalniflumateThe risk or severity of adverse effects can be increased when Talniflumate is combined with Zileuton.
TasosartanThe risk or severity of adverse effects can be increased when Tasosartan is combined with Zileuton.
Technetium Tc-99m MedronateThe risk or severity of adverse effects can be increased when Zileuton is combined with Technetium Tc-99m Medronate.
TelaprevirThe metabolism of Zileuton can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Zileuton can be decreased when combined with Telithromycin.
TelmisartanThe risk or severity of adverse effects can be increased when Telmisartan is combined with Zileuton.
TemocaprilThe risk or severity of adverse effects can be increased when Temocapril is combined with Zileuton.
TenofovirThe risk or severity of adverse effects can be increased when Zileuton is combined with Tenofovir.
TenofovirThe metabolism of Zileuton can be decreased when combined with Tenofovir.
TenoxicamThe risk or severity of adverse effects can be increased when Tenoxicam is combined with Zileuton.
TepoxalinThe risk or severity of adverse effects can be increased when Zileuton is combined with Tepoxalin.
TeriflunomideThe serum concentration of Zileuton can be decreased when it is combined with Teriflunomide.
TeriflunomideThe risk or severity of adverse effects can be increased when Zileuton is combined with Teriflunomide.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Zileuton.
TheophyllineThe metabolism of Zileuton can be decreased when combined with Theophylline.
Tiaprofenic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Tiaprofenic acid.
TicagrelorThe metabolism of Zileuton can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Zileuton can be decreased when combined with Ticlopidine.
TiludronateThe risk or severity of adverse effects can be increased when Zileuton is combined with Tiludronate.
TimololZileuton may decrease the antihypertensive activities of Timolol.
TobramycinZileuton may decrease the excretion rate of Tobramycin which could result in a lower serum level and potentially a reduction in efficacy.
TocilizumabThe serum concentration of Zileuton can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Zileuton can be decreased when combined with Tolbutamide.
Tolfenamic AcidThe risk or severity of adverse effects can be increased when Zileuton is combined with Tolfenamic Acid.
TolmetinThe risk or severity of adverse effects can be increased when Tolmetin is combined with Zileuton.
TorasemideZileuton may decrease the diuretic activities of Torasemide.
TrandolaprilThe risk or severity of adverse effects can be increased when Trandolapril is combined with Zileuton.
TranilastThe risk or severity of adverse effects can be increased when Zileuton is combined with Tranilast.
TravoprostThe therapeutic efficacy of Travoprost can be decreased when used in combination with Zileuton.
TreprostinilThe risk or severity of adverse effects can be increased when Treprostinil is combined with Zileuton.
TriamtereneZileuton may decrease the antihypertensive activities of Triamterene.
TrichlormethiazideThe therapeutic efficacy of Trichlormethiazide can be decreased when used in combination with Zileuton.
TrimethoprimThe metabolism of Zileuton can be decreased when combined with Trimethoprim.
Trisalicylate-cholineThe risk or severity of adverse effects can be increased when Zileuton is combined with Trisalicylate-choline.
ValdecoxibThe risk or severity of adverse effects can be increased when Valdecoxib is combined with Zileuton.
Valproic AcidThe metabolism of Zileuton can be decreased when combined with Valproic Acid.
ValsartanThe risk or severity of adverse effects can be increased when Valsartan is combined with Zileuton.
VancomycinThe serum concentration of Vancomycin can be increased when it is combined with Zileuton.
VemurafenibThe serum concentration of Zileuton can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Zileuton can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Zileuton can be decreased when combined with Verapamil.
VoriconazoleThe metabolism of Zileuton can be decreased when combined with Voriconazole.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Zileuton.
XimelagatranZileuton may increase the anticoagulant activities of Ximelagatran.
ZafirlukastThe metabolism of Zileuton can be decreased when combined with Zafirlukast.
ZaltoprofenThe risk or severity of adverse effects can be increased when Zileuton is combined with Zaltoprofen.
ZiprasidoneThe metabolism of Zileuton can be decreased when combined with Ziprasidone.
Zoledronic acidThe risk or severity of adverse effects can be increased when Zileuton is combined with Zoledronic acid.
ZomepiracThe risk or severity of adverse effects can be increased when Zileuton is combined with Zomepirac.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Iron ion binding
Specific Function:
Catalyzes the first step in leukotriene biosynthesis, and thereby plays a role in inflammatory processes.
Gene Name:
ALOX5
Uniprot ID:
P09917
Molecular Weight:
77982.595 Da
References
  1. Wenzel SE: Leukotriene receptor antagonists and related compounds. Can Respir J. 1999 Mar-Apr;6(2):189-93. [PubMed:10322101 ]
  2. Hardy DB, Pereria LE, Yang K: Prostaglandins and leukotriene B4 are potent inhibitors of 11beta-hydroxysteroid dehydrogenase type 2 activity in human choriocarcinoma JEG-3 cells. Biol Reprod. 1999 Jul;61(1):40-5. [PubMed:10377029 ]
  3. Yamashita M, Kushihara M, Hirasawa N, Takasaki W, Takahagi H, Takayanagi M, Ohuchi K: Inhibition by troglitazone of the antigen-induced production of leukotrienes in immunoglobulin E-sensitized RBL-2H3 cells. Br J Pharmacol. 2000 Jan;129(2):367-73. [PubMed:10694244 ]
  4. Qian C, Hwang SB, Libertine-Garahan L, Eckman JB, Cai X, Scannell RT, Yeh CG: Anti-inflammatory activities of LDP-392, a dual PAF receptor antagonist and 5-lipoxygenase inhibitor. Pharmacol Res. 2001 Sep;44(3):213-20. [PubMed:11529688 ]
  5. Coffey MJ, Phare SM, Peters-Golden M: Peroxynitrite-induced nitrotyrosination of proteins is blocked by direct 5-lipoxygenase inhibitor zileuton. J Pharmacol Exp Ther. 2001 Oct;299(1):198-203. [PubMed:11561080 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Zouboulis CC: Zileuton, a new efficient and safe systemic anti-acne drug. Dermatoendocrinol. 2009 May;1(3):188-92. [PubMed:20436887 ]
  8. Zouboulis CC, Seltmann H, Alestas T: Zileuton prevents the activation of the leukotriene pathway and reduces sebaceous lipogenesis. Exp Dermatol. 2010 Feb;19(2):148-50. doi: 10.1111/j.1600-0625.2009.00929.x. Epub 2009 Jul 23. [PubMed:19645854 ]
  9. Berger W, De Chandt MT, Cairns CB: Zileuton: clinical implications of 5-Lipoxygenase inhibition in severe airway disease. Int J Clin Pract. 2007 Apr;61(4):663-76. [PubMed:17394438 ]
  10. Guidot DM, Repine MJ, Westcott JY, Repine JE: Intrinsic 5-lipoxygenase activity is required for neutrophil responsivity. Proc Natl Acad Sci U S A. 1994 Aug 16;91(17):8156-9. [PubMed:8058773 ]
  11. Wenzel SE, Kamada AK: Zileuton: the first 5-lipoxygenase inhibitor for the treatment of asthma. Ann Pharmacother. 1996 Jul-Aug;30(7-8):858-64. [PubMed:8826571 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Wang B, Zhou SF: Synthetic and natural compounds that interact with human cytochrome P450 1A2 and implications in drug development. Curr Med Chem. 2009;16(31):4066-218. [PubMed:19754423 ]
  2. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  3. Machinist JM, Mayer MD, Shet MS, Ferrero JL, Rodrigues AD: Identification of the human liver cytochrome P450 enzymes involved in the metabolism of zileuton (ABT-077) and its N-dehydroxylated metabolite, Abbott-66193. Drug Metab Dispos. 1995 Oct;23(10):1163-74. [PubMed:8654206 ]
  4. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Machinist JM, Mayer MD, Shet MS, Ferrero JL, Rodrigues AD: Identification of the human liver cytochrome P450 enzymes involved in the metabolism of zileuton (ABT-077) and its N-dehydroxylated metabolite, Abbott-66193. Drug Metab Dispos. 1995 Oct;23(10):1163-74. [PubMed:8654206 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Retinoic acid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks transferase activity but acts as a negative regulator of isoform 1.
Gene Name:
UGT1A9
Uniprot ID:
O60656
Molecular Weight:
59940.495 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23