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Identification
NameZafirlukast
Accession NumberDB00549  (APRD00377)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionZafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), which is usually taken just once daily. Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages.
Structure
Thumb
Synonyms
4-(5-Cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-O-tolylsulfonylbenzamide
Accolate
Cyclopentyl 3-(2-methoxy-4-((O-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate
ICI-204,219
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Accolatetablet, film coated10 mg/1oralAstra Zeneca Pharmaceuticals Lp1996-10-01Not applicableUs
Accolatetablet, coated20 mg/1oralPar Pharmaceutical Inc.2015-11-01Not applicableUs
Accolatetablet, film coated10 mg/1oralPar Pharmaceutical Inc.2015-01-09Not applicableUs
Accolatetablet, film coated20 mg/1oralAstra Zeneca Pharmaceuticals Lp1996-10-01Not applicableUs
Accolatetablet, film coated20 mg/1oralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
Accolatetablet, film coated20 mg/1oralPar Pharmaceutical Inc.2015-01-09Not applicableUs
Accolatetablet, coated10 mg/1oralPar Pharmaceutical Inc.2015-11-01Not applicableUs
Accolate Tab 20 mgtablet20 mgoralAstrazeneca Canada Inc1997-11-17Not applicableCanada
Zafirlukasttablet, film coated20 mg/1oralPar Pharmaceutical Inc.2010-12-01Not applicableUs
Zafirlukasttablet, coated10 mg/1oralPar Pharmaceutical Inc.2015-12-16Not applicableUs
Zafirlukasttablet, coated20 mg/1oralPar Pharmaceutical Inc.2015-12-16Not applicableUs
Zafirlukasttablet, film coated10 mg/1oralAstra Zeneca Pharmaceuticals Lp2010-11-19Not applicableUs
Zafirlukasttablet, film coated10 mg/1oralPar Pharmaceutical Inc.2010-12-01Not applicableUs
Zafirlukasttablet, film coated20 mg/1oralAstra Zeneca Pharmaceuticals Lp2010-11-19Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Zafirlukasttablet, film coated10 mg/1oralDr. Reddys Laboratories Limited2010-11-18Not applicableUs
Zafirlukasttablet, film coated20 mg/1oralDr. Reddys Laboratories Limited2010-11-18Not applicableUs
Zafirlukasttablet, film coated20 mg/1oralAmerican Health Packaging2013-06-07Not applicableUs
Zafirlukasttablet, film coated20 mg/1oralCarilion Materials Management2010-11-18Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIXZ629S5L50
CAS number107753-78-6
WeightAverage: 575.675
Monoisotopic: 575.209006493
Chemical FormulaC31H33N3O6S
InChI KeyInChIKey=YEEZWCHGZNKEEK-UHFFFAOYSA-N
InChI
InChI=1S/C31H33N3O6S/c1-20-8-4-7-11-29(20)41(37,38)33-30(35)22-13-12-21(28(17-22)39-3)16-23-19-34(2)27-15-14-24(18-26(23)27)32-31(36)40-25-9-5-6-10-25/h4,7-8,11-15,17-19,25H,5-6,9-10,16H2,1-3H3,(H,32,36)(H,33,35)
IUPAC Name
cyclopentyl N-[3-({2-methoxy-4-[(2-methylbenzenesulfonyl)carbamoyl]phenyl}methyl)-1-methyl-1H-indol-5-yl]carbamate
SMILES
COC1=C(CC2=CN(C)C3=C2C=C(NC(=O)OC2CCCC2)C=C3)C=CC(=C1)C(=O)NS(=O)(=O)C1=CC=CC=C1C
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as benzenesulfonamides. These are organic compounds containing a sulfonamide group that is S-linked to a benzene ring.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzenesulfonamides
Direct ParentBenzenesulfonamides
Alternative Parents
Substituents
  • Phenylcarbamate
  • Benzenesulfonamide
  • Indole or derivatives
  • Indole
  • Benzoic acid or derivatives
  • Benzamide
  • Methoxybenzene
  • Phenol ether
  • Benzoyl
  • Anisole
  • Toluene
  • Alkyl aryl ether
  • Substituted pyrrole
  • N-methylpyrrole
  • Heteroaromatic compound
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Pyrrole
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Monocarboxylic acid or derivatives
  • Ether
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Carbonyl group
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the prophylaxis and chronic treatment of asthma.
PharmacodynamicsZafirlukast is a synthetic, selective peptide leukotriene receptor antagonist (LTRA) indicated for the prophylaxis and chronic treatment of asthma. Patients with asthma were found in one study to be 25-100 times more sensitive to the bronchoconstricting activity of inhaled LTD4 than nonasthmatic subjects. In vitro studies demonstrated that zafirlukast antagonized the contractile activity of three leukotrienes (LTC4, LTD4 and LTE4) in conducting airway smooth muscle from laboratory animals and humans. Zafirlukast prevented intradermal LTD4-induced increases in cutaneous vascular permeability and inhibited inhaled LTD4-induced influx of eosinophils into animal lungs.
Mechanism of actionZafirlukast is a selective and competitive receptor antagonist of leukotriene D4 and E4 (LTD4 and LTE4), components of slow-reacting substance of anaphylaxis (SRSA). Cysteinyl leukotriene production and receptor occupation have been correlated with the pathophysiology of asthma, including airway edema, smooth muscle constriction, and altered cellular activity associated with the inflammatory process, which contribute to the signs and symptoms of asthma.
Related Articles
AbsorptionRapidly absorbed following oral administration, reduced following a high-fat or high-protein meal.
Volume of distribution
  • 70 L
Protein binding99%
Metabolism

Hepatic

SubstrateEnzymesProduct
Zafirlukast
Zafirlukast metabolite M5Details
Zafirlukast
Not Available
Zafirlukast metabolite M1Details
Zafirlukast metabolite M1
Zafirlukast metabolite M2Details
Zafirlukast metabolite M2
Not Available
Zafirlukast metabolite M4Details
Zafirlukast metabolite M4
Not Available
Zafirlukast metabolite M3Details
Zafirlukast metabolite M5
Not Available
Zafirlukast metabolite M8Details
Zafirlukast metabolite M8
Not Available
Zafirlukast metabolite M3Details
Route of eliminationThe most common metabolic products are hydroxylated metabolites which are excreted in the feces.
Half life10 hours
Clearance
  • apparent oral CL=20 L/h
  • 11.4 L/h [7-11 yrs]
  • 9.2 L/h [5-6 yrs]
ToxicitySide effects include rash and upset stomach.
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+0.8849
Blood Brain Barrier+0.9153
Caco-2 permeable-0.6613
P-glycoprotein substrateNon-substrate0.7027
P-glycoprotein inhibitor INon-inhibitor0.6249
P-glycoprotein inhibitor IIInhibitor0.8915
Renal organic cation transporterNon-inhibitor0.8475
CYP450 2C9 substrateNon-substrate0.5189
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.5322
CYP450 1A2 substrateNon-inhibitor0.5261
CYP450 2C9 inhibitorInhibitor0.646
CYP450 2D6 inhibitorNon-inhibitor0.8263
CYP450 2C19 inhibitorInhibitor0.5826
CYP450 3A4 inhibitorInhibitor0.7904
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9189
Ames testNon AMES toxic0.6072
CarcinogenicityNon-carcinogens0.7292
BiodegradationNot ready biodegradable0.9972
Rat acute toxicity2.5723 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9216
hERG inhibition (predictor II)Inhibitor0.7693
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Astrazeneca uk ltd
Packagers
Dosage forms
FormRouteStrength
Tablet, film coatedoral10 mg/1
Tablet, film coatedoral20 mg/1
Tabletoral20 mg
Tablet, coatedoral10 mg/1
Tablet, coatedoral20 mg/1
Prices
Unit descriptionCostUnit
Accolate 10 mg tablet1.92USD tablet
Accolate 20 mg tablet1.86USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1340567 No1999-06-012016-06-01Canada
CA2056066 No2002-04-022011-11-22Canada
US4859692 No1993-09-262010-09-26Us
US5612367 No1994-03-182014-03-18Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point139 °CNot Available
logP5.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.000962 mg/mLALOGPS
logP4.84ALOGPS
logP6.4ChemAxon
logS-5.8ALOGPS
pKa (Strongest Acidic)4.29ChemAxon
pKa (Strongest Basic)-1.1ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area115.73 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity158.58 m3·mol-1ChemAxon
Polarizability62.06 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability0ChemAxon
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

Arie Gutman, “Process for the preparation of zafirlukast.” U.S. Patent US20040186300, issued September 23, 2004.

US20040186300
General ReferencesNot Available
External Links
ATC CodesR03DC01
AHFS Codes
  • 48:10.24
PDB EntriesNot Available
FDA labelDownload (233 KB)
MSDSDownload (57.6 KB)
Interactions
Drug Interactions
Drug
AbirateroneThe serum concentration of Zafirlukast can be increased when it is combined with Abiraterone.
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Zafirlukast.
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Zafirlukast.
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Zafirlukast.
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Zafirlukast.
AlosetronThe metabolism of Alosetron can be decreased when combined with Zafirlukast.
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Zafirlukast.
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Zafirlukast.
AminophyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.
AmiodaroneThe metabolism of Amiodarone can be decreased when combined with Zafirlukast.
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Zafirlukast.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Zafirlukast.
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Zafirlukast.
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Zafirlukast.
ApixabanThe metabolism of Apixaban can be decreased when combined with Zafirlukast.
AprepitantThe serum concentration of Zafirlukast can be increased when it is combined with Aprepitant.
Arachidonic AcidThe metabolism of Arachidonic Acid can be decreased when combined with Zafirlukast.
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Zafirlukast.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Zafirlukast.
ArtemetherThe metabolism of Artemether can be decreased when combined with Zafirlukast.
AtazanavirThe metabolism of Zafirlukast can be decreased when combined with Atazanavir.
AtomoxetineThe metabolism of Zafirlukast can be decreased when combined with Atomoxetine.
AzelastineThe metabolism of Azelastine can be decreased when combined with Zafirlukast.
BexaroteneThe serum concentration of Zafirlukast can be decreased when it is combined with Bexarotene.
BexaroteneThe metabolism of Bexarotene can be decreased when combined with Zafirlukast.
BoceprevirThe metabolism of Zafirlukast can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Zafirlukast can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Zafirlukast can be decreased when it is combined with Bosentan.
BosentanThe serum concentration of Bosentan can be increased when it is combined with Zafirlukast.
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Zafirlukast.
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Zafirlukast.
BupropionThe metabolism of Bupropion can be decreased when combined with Zafirlukast.
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Zafirlukast.
CaffeineThe metabolism of Caffeine can be decreased when combined with Zafirlukast.
CandesartanThe metabolism of Candesartan can be decreased when combined with Zafirlukast.
CapecitabineThe metabolism of Zafirlukast can be decreased when combined with Capecitabine.
CarbamazepineThe metabolism of Zafirlukast can be increased when combined with Carbamazepine.
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Zafirlukast.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Zafirlukast.
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Zafirlukast.
CeritinibThe serum concentration of Zafirlukast can be increased when it is combined with Ceritinib.
ChlorpropamideThe metabolism of Chlorpropamide can be decreased when combined with Zafirlukast.
CholecalciferolThe metabolism of Zafirlukast can be decreased when combined with Cholecalciferol.
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Zafirlukast.
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Zafirlukast.
CisaprideThe metabolism of Cisapride can be decreased when combined with Zafirlukast.
ClarithromycinThe metabolism of Zafirlukast can be decreased when combined with Clarithromycin.
ClemastineThe metabolism of Zafirlukast can be decreased when combined with Clemastine.
ClopidogrelThe metabolism of Clopidogrel can be decreased when combined with Zafirlukast.
ClotrimazoleThe metabolism of Zafirlukast can be decreased when combined with Clotrimazole.
ClozapineThe metabolism of Clozapine can be decreased when combined with Zafirlukast.
CobicistatThe metabolism of Zafirlukast can be decreased when combined with Cobicistat.
ConivaptanThe serum concentration of Zafirlukast can be increased when it is combined with Conivaptan.
CrizotinibThe metabolism of Zafirlukast can be decreased when combined with Crizotinib.
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Zafirlukast.
CyclosporineThe metabolism of Zafirlukast can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Zafirlukast can be decreased when it is combined with Dabrafenib.
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Zafirlukast.
DapsoneThe metabolism of Dapsone can be decreased when combined with Zafirlukast.
DarunavirThe metabolism of Zafirlukast can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Zafirlukast can be increased when it is combined with Dasatinib.
DeferasiroxThe serum concentration of Zafirlukast can be decreased when it is combined with Deferasirox.
DelavirdineThe metabolism of Zafirlukast can be decreased when combined with Delavirdine.
DexamethasoneThe serum concentration of Zafirlukast can be decreased when it is combined with Dexamethasone.
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Zafirlukast.
DiazepamThe metabolism of Diazepam can be decreased when combined with Zafirlukast.
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Zafirlukast.
DicoumarolThe serum concentration of Dicoumarol can be increased when it is combined with Zafirlukast.
DihydroergotamineThe metabolism of Zafirlukast can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Zafirlukast can be decreased when combined with Diltiazem.
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Zafirlukast.
DolasetronThe metabolism of Dolasetron can be decreased when combined with Zafirlukast.
DonepezilThe metabolism of Donepezil can be decreased when combined with Zafirlukast.
DopamineThe metabolism of Dopamine can be decreased when combined with Zafirlukast.
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Zafirlukast.
DoxepinThe metabolism of Doxepin can be decreased when combined with Zafirlukast.
DoxycyclineThe metabolism of Zafirlukast can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Zafirlukast.
DronedaroneThe metabolism of Zafirlukast can be decreased when combined with Dronedarone.
DyphyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Dyphylline.
EfavirenzThe serum concentration of Zafirlukast can be decreased when it is combined with Efavirenz.
EletriptanThe metabolism of Eletriptan can be decreased when combined with Zafirlukast.
EnzalutamideThe serum concentration of Zafirlukast can be decreased when it is combined with Enzalutamide.
EpoprostenolThe metabolism of Epoprostenol can be decreased when combined with Zafirlukast.
ErythromycinThe serum concentration of Zafirlukast can be decreased when it is combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Zafirlukast can be decreased when it is combined with Eslicarbazepine acetate.
EstradiolThe metabolism of Estradiol can be decreased when combined with Zafirlukast.
EstroneThe metabolism of Estrone can be decreased when combined with Zafirlukast.
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Zafirlukast.
Ethyl biscoumacetateThe serum concentration of Ethyl biscoumacetate can be increased when it is combined with Zafirlukast.
EtodolacThe metabolism of Etodolac can be decreased when combined with Zafirlukast.
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Zafirlukast.
EtravirineThe serum concentration of Zafirlukast can be decreased when it is combined with Etravirine.
EtravirineThe metabolism of Etravirine can be decreased when combined with Zafirlukast.
FelodipineThe metabolism of Zafirlukast can be decreased when combined with Felodipine.
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Zafirlukast.
FloxuridineThe metabolism of Zafirlukast can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Zafirlukast can be decreased when combined with Fluconazole.
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Zafirlukast.
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Zafirlukast.
FluorouracilThe metabolism of Zafirlukast can be decreased when combined with Fluorouracil.
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Zafirlukast.
FlurbiprofenThe metabolism of Flurbiprofen can be decreased when combined with Zafirlukast.
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Zafirlukast.
FluvoxamineThe metabolism of Zafirlukast can be decreased when combined with Fluvoxamine.
FormoterolThe metabolism of Formoterol can be decreased when combined with Zafirlukast.
FosamprenavirThe metabolism of Zafirlukast can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Zafirlukast can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Zafirlukast can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Zafirlukast can be increased when it is combined with Fusidic Acid.
GavestinelThe metabolism of Gavestinel can be decreased when combined with Zafirlukast.
GemfibrozilThe metabolism of Zafirlukast can be decreased when combined with Gemfibrozil.
GliclazideThe metabolism of Gliclazide can be decreased when combined with Zafirlukast.
GlimepirideThe metabolism of Glimepiride can be decreased when combined with Zafirlukast.
GlipizideThe metabolism of Glipizide can be decreased when combined with Zafirlukast.
GlyburideThe metabolism of Glyburide can be decreased when combined with Zafirlukast.
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Zafirlukast.
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Zafirlukast.
HalothaneThe metabolism of Halothane can be decreased when combined with Zafirlukast.
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Zafirlukast.
Histamine PhosphateThe metabolism of Histamine Phosphate can be decreased when combined with Zafirlukast.
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Zafirlukast.
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Zafirlukast.
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Zafirlukast.
IdelalisibThe serum concentration of Zafirlukast can be increased when it is combined with Idelalisib.
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Zafirlukast.
ImatinibThe metabolism of Zafirlukast can be decreased when combined with Imatinib.
IndinavirThe metabolism of Zafirlukast can be decreased when combined with Indinavir.
indisulamThe metabolism of indisulam can be decreased when combined with Zafirlukast.
IndomethacinThe metabolism of Indomethacin can be decreased when combined with Zafirlukast.
IrbesartanThe metabolism of Irbesartan can be decreased when combined with Zafirlukast.
IsavuconazoniumThe metabolism of Zafirlukast can be decreased when combined with Isavuconazonium.
IsradipineThe metabolism of Zafirlukast can be decreased when combined with Isradipine.
ItraconazoleThe metabolism of Zafirlukast can be decreased when combined with Itraconazole.
IvacaftorThe serum concentration of Zafirlukast can be increased when it is combined with Ivacaftor.
IxazomibThe metabolism of Ixazomib can be decreased when combined with Zafirlukast.
KetamineThe metabolism of Ketamine can be decreased when combined with Zafirlukast.
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Zafirlukast.
KetoconazoleThe metabolism of Zafirlukast can be decreased when combined with Ketoconazole.
KetoprofenThe metabolism of Ketoprofen can be decreased when combined with Zafirlukast.
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Zafirlukast.
LapatinibThe metabolism of Zafirlukast can be decreased when combined with Lapatinib.
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Zafirlukast.
LesinuradThe metabolism of Lesinurad can be decreased when combined with Zafirlukast.
LicofeloneThe metabolism of Licofelone can be decreased when combined with Zafirlukast.
LidocaineThe metabolism of Lidocaine can be decreased when combined with Zafirlukast.
LopinavirThe metabolism of Zafirlukast can be decreased when combined with Lopinavir.
LoratadineThe metabolism of Loratadine can be decreased when combined with Zafirlukast.
LornoxicamThe metabolism of Lornoxicam can be decreased when combined with Zafirlukast.
LosartanThe metabolism of Losartan can be decreased when combined with Zafirlukast.
LovastatinThe metabolism of Zafirlukast can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Zafirlukast can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Zafirlukast can be decreased when it is combined with Lumacaftor.
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Zafirlukast.
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Zafirlukast.
MelatoninThe metabolism of Melatonin can be decreased when combined with Zafirlukast.
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Zafirlukast.
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Zafirlukast.
MestranolThe metabolism of Mestranol can be decreased when combined with Zafirlukast.
MethadoneThe metabolism of Methadone can be decreased when combined with Zafirlukast.
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Zafirlukast.
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Zafirlukast.
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Zafirlukast.
MifepristoneThe metabolism of Zafirlukast can be decreased when combined with Mifepristone.
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Zafirlukast.
MitotaneThe serum concentration of Zafirlukast can be decreased when it is combined with Mitotane.
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Zafirlukast.
ModafinilThe serum concentration of Zafirlukast can be decreased when it is combined with Modafinil.
MontelukastThe metabolism of Montelukast can be decreased when combined with Zafirlukast.
NafcillinThe serum concentration of Zafirlukast can be decreased when it is combined with Nafcillin.
NaproxenThe metabolism of Naproxen can be decreased when combined with Zafirlukast.
NateglinideThe metabolism of Nateglinide can be decreased when combined with Zafirlukast.
NefazodoneThe metabolism of Zafirlukast can be decreased when combined with Nefazodone.
NelfinavirThe metabolism of Zafirlukast can be decreased when combined with Nelfinavir.
NetupitantThe serum concentration of Zafirlukast can be increased when it is combined with Netupitant.
NetupitantThe metabolism of Netupitant can be decreased when combined with Zafirlukast.
NevirapineThe metabolism of Zafirlukast can be decreased when combined with Nevirapine.
NicardipineThe metabolism of Zafirlukast can be decreased when combined with Nicardipine.
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Zafirlukast.
NicotineThe metabolism of Nicotine can be decreased when combined with Zafirlukast.
NilotinibThe metabolism of Zafirlukast can be decreased when combined with Nilotinib.
NintedanibThe serum concentration of Nintedanib can be increased when it is combined with Zafirlukast.
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Zafirlukast.
OlaparibThe metabolism of Zafirlukast can be decreased when combined with Olaparib.
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Zafirlukast.
OmeprazoleThe metabolism of Zafirlukast can be decreased when combined with Omeprazole.
OndansetronThe metabolism of Ondansetron can be decreased when combined with Zafirlukast.
OsimertinibThe serum concentration of Zafirlukast can be increased when it is combined with Osimertinib.
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Zafirlukast.
OxaprozinThe metabolism of Oxaprozin can be decreased when combined with Zafirlukast.
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Zafirlukast.
PalbociclibThe serum concentration of Zafirlukast can be increased when it is combined with Palbociclib.
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Zafirlukast.
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Zafirlukast.
PentobarbitalThe metabolism of Zafirlukast can be increased when combined with Pentobarbital.
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Zafirlukast.
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Zafirlukast.
PhenindioneThe serum concentration of Phenindione can be increased when it is combined with Zafirlukast.
PhenobarbitalThe metabolism of Zafirlukast can be increased when combined with Phenobarbital.
PhenprocoumonThe serum concentration of Phenprocoumon can be increased when it is combined with Zafirlukast.
PhenylbutazoneThe metabolism of Phenylbutazone can be decreased when combined with Zafirlukast.
PhenytoinThe metabolism of Zafirlukast can be increased when combined with Phenytoin.
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Zafirlukast.
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Zafirlukast.
PitavastatinThe metabolism of Pitavastatin can be decreased when combined with Zafirlukast.
PosaconazoleThe metabolism of Zafirlukast can be decreased when combined with Posaconazole.
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Zafirlukast.
PravastatinThe metabolism of Pravastatin can be decreased when combined with Zafirlukast.
PrimidoneThe metabolism of Zafirlukast can be increased when combined with Primidone.
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Zafirlukast.
ProguanilThe metabolism of Proguanil can be decreased when combined with Zafirlukast.
PromazineThe metabolism of Promazine can be decreased when combined with Zafirlukast.
PropofolThe metabolism of Propofol can be decreased when combined with Zafirlukast.
PyrimethamineThe metabolism of Zafirlukast can be decreased when combined with Pyrimethamine.
QuazepamThe metabolism of Quazepam can be decreased when combined with Zafirlukast.
QuinidineThe metabolism of Quinidine can be decreased when combined with Zafirlukast.
QuinineThe metabolism of Zafirlukast can be decreased when combined with Quinine.
RabeprazoleThe metabolism of Zafirlukast can be decreased when combined with Rabeprazole.
RanolazineThe metabolism of Zafirlukast can be decreased when combined with Ranolazine.
RifabutinThe metabolism of Zafirlukast can be increased when combined with Rifabutin.
RifampicinThe metabolism of Zafirlukast can be increased when combined with Rifampicin.
RifapentineThe metabolism of Zafirlukast can be increased when combined with Rifapentine.
RitonavirThe metabolism of Zafirlukast can be decreased when combined with Ritonavir.
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Zafirlukast.
RosiglitazoneThe metabolism of Rosiglitazone can be decreased when combined with Zafirlukast.
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Zafirlukast.
Salicylic acidThe metabolism of Salicylic acid can be decreased when combined with Zafirlukast.
SaquinavirThe metabolism of Zafirlukast can be decreased when combined with Saquinavir.
SecobarbitalThe metabolism of Zafirlukast can be increased when combined with Secobarbital.
SelegilineThe metabolism of Selegiline can be decreased when combined with Zafirlukast.
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Zafirlukast.
SertralineThe metabolism of Sertraline can be decreased when combined with Zafirlukast.
SildenafilThe metabolism of Zafirlukast can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Zafirlukast can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Zafirlukast can be increased when it is combined with Simeprevir.
SitaxentanThe metabolism of Sitaxentan can be decreased when combined with Zafirlukast.
SorafenibThe metabolism of Zafirlukast can be decreased when combined with Sorafenib.
St. John's WortThe serum concentration of Zafirlukast can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Zafirlukast can be increased when it is combined with Stiripentol.
SulfadiazineThe metabolism of Sulfadiazine can be decreased when combined with Zafirlukast.
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Zafirlukast.
SulfamoxoleThe metabolism of Sulfamoxole can be decreased when combined with Zafirlukast.
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Zafirlukast.
SulfisoxazoleThe metabolism of Zafirlukast can be decreased when combined with Sulfisoxazole.
SuprofenThe metabolism of Suprofen can be decreased when combined with Zafirlukast.
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Zafirlukast.
TapentadolThe metabolism of Tapentadol can be decreased when combined with Zafirlukast.
TelaprevirThe metabolism of Zafirlukast can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Zafirlukast can be decreased when combined with Telithromycin.
TemazepamThe metabolism of Temazepam can be decreased when combined with Zafirlukast.
TenoxicamThe metabolism of Tenoxicam can be decreased when combined with Zafirlukast.
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Zafirlukast.
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Zafirlukast.
TeriflunomideThe metabolism of Zafirlukast can be decreased when combined with Teriflunomide.
TestosteroneThe metabolism of Testosterone can be decreased when combined with Zafirlukast.
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Zafirlukast.
TheophyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Theophylline.
TheophyllineThe metabolism of Theophylline can be decreased when combined with Zafirlukast.
ThiamylalThe metabolism of Thiamylal can be decreased when combined with Zafirlukast.
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Zafirlukast.
TicagrelorThe metabolism of Zafirlukast can be decreased when combined with Ticagrelor.
TiclopidineThe metabolism of Zafirlukast can be decreased when combined with Ticlopidine.
TocilizumabThe serum concentration of Zafirlukast can be decreased when it is combined with Tocilizumab.
TolbutamideThe metabolism of Tolbutamide can be decreased when combined with Zafirlukast.
TolterodineThe metabolism of Tolterodine can be decreased when combined with Zafirlukast.
TorasemideThe metabolism of Torasemide can be decreased when combined with Zafirlukast.
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Zafirlukast.
TreprostinilThe metabolism of Treprostinil can be decreased when combined with Zafirlukast.
TretinoinThe metabolism of Tretinoin can be decreased when combined with Zafirlukast.
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Zafirlukast.
TrimethoprimThe metabolism of Zafirlukast can be decreased when combined with Trimethoprim.
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Zafirlukast.
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Zafirlukast.
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Zafirlukast.
Valproic AcidThe metabolism of Zafirlukast can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Zafirlukast can be decreased when combined with Valsartan.
VenlafaxineThe metabolism of Zafirlukast can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Zafirlukast can be decreased when combined with Verapamil.
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Zafirlukast.
VismodegibThe metabolism of Vismodegib can be decreased when combined with Zafirlukast.
VoriconazoleThe metabolism of Voriconazole can be decreased when combined with Zafirlukast.
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Zafirlukast.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Zafirlukast.
XimelagatranThe metabolism of Ximelagatran can be decreased when combined with Zafirlukast.
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Zafirlukast.
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Zafirlukast.
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Zafirlukast.
ZileutonThe metabolism of Zileuton can be decreased when combined with Zafirlukast.
ZiprasidoneThe metabolism of Zafirlukast can be decreased when combined with Ziprasidone.
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Zafirlukast.
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Zafirlukast.
Food Interactions
  • Take on empty stomach: 1 hour before or 2 hours after meals.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
antagonist
General Function:
Leukotriene receptor activity
Specific Function:
Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affini...
Gene Name:
CYSLTR1
Uniprot ID:
Q9Y271
Molecular Weight:
38540.55 Da
References
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  2. Cazzola M, Boveri B, Carlucci P, Santus P, DiMarco F, Centanni S, Allegra L: Lung function improvement in smokers suffering from COPD with zafirlukast, a CysLT(1)-receptor antagonist. Pulm Pharmacol Ther. 2000;13(6):301-5. [PubMed:11061985 ]
  3. Murata Y, Sugimoto O: [Zafirlukast (Accolate): a review of its pharmacological and clinical profile]. Nihon Yakurigaku Zasshi. 2002 Apr;119(4):247-58. [PubMed:11979731 ]
  4. Wang S, Gustafson E, Pang L, Qiao X, Behan J, Maguire M, Bayne M, Laz T: A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization. J Biol Chem. 2000 Dec 29;275(52):40686-94. [PubMed:11006272 ]
  5. O'Byrne PM: Leukotrienes in the pathogenesis of asthma. Chest. 1997 Feb;111(2 Suppl):27S-34S. [PubMed:9042024 ]
  6. Heise CE, O'Dowd BF, Figueroa DJ, Sawyer N, Nguyen T, Im DS, Stocco R, Bellefeuille JN, Abramovitz M, Cheng R, Williams DL Jr, Zeng Z, Liu Q, Ma L, Clements MK, Coulombe N, Liu Y, Austin CP, George SR, O'Neill GP, Metters KM, Lynch KR, Evans JF: Characterization of the human cysteinyl leukotriene 2 receptor. J Biol Chem. 2000 Sep 29;275(39):30531-6. [PubMed:10851239 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
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. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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
substrateinhibitor
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
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. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
Antagonist
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Sun YL, Kathawala RJ, Singh S, Zheng K, Talele TT, Jiang WQ, Chen ZS: Zafirlukast antagonizes ATP-binding cassette subfamily G member 2-mediated multidrug resistance. Anticancer Drugs. 2012 Sep;23(8):865-73. doi: 10.1097/CAD.0b013e328354a196. [PubMed:22614107 ]
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23