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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 KeyYEEZWCHGZNKEEK-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
Pharmacology
IndicationFor the prophylaxis and chronic treatment of asthma.
Structured Indications
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.
TargetKindPharmacological actionActionsOrganismUniProt ID
Cysteinyl leukotriene receptor 1Proteinyes
antagonist
HumanQ9Y271 details
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
Interactions
Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Zafirlukast can be increased when it is combined with Abiraterone.Approved
AceclofenacThe metabolism of Aceclofenac can be decreased when combined with Zafirlukast.Approved
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Zafirlukast.Approved
AcetaminophenThe metabolism of Acetaminophen can be decreased when combined with Zafirlukast.Approved
Acetylsalicylic acidThe metabolism of Acetylsalicylic acid can be decreased when combined with Zafirlukast.Approved, Vet Approved
AlosetronThe metabolism of Alosetron can be decreased when combined with Zafirlukast.Approved, Withdrawn
AlprazolamThe metabolism of Alprazolam can be decreased when combined with Zafirlukast.Approved, Illicit, Investigational
Ambroxol acefyllinateThe serum concentration of Zafirlukast can be decreased when it is combined with Ambroxol acefyllinate.Experimental
AminophenazoneThe metabolism of Aminophenazone can be decreased when combined with Zafirlukast.Approved, Withdrawn
AminophyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.Approved
AmiodaroneThe metabolism of Zafirlukast can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe metabolism of Amitriptyline can be decreased when combined with Zafirlukast.Approved
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Zafirlukast.Approved
AmprenavirThe metabolism of Amprenavir can be decreased when combined with Zafirlukast.Approved
AntipyrineThe metabolism of Antipyrine can be decreased when combined with Zafirlukast.Approved
ApixabanThe metabolism of Apixaban can be decreased when combined with Zafirlukast.Approved
AprepitantThe serum concentration of Zafirlukast can be increased when it is combined with Aprepitant.Approved, Investigational
Arachidonic AcidThe metabolism of Arachidonic Acid can be decreased when combined with Zafirlukast.Experimental
ArformoterolThe metabolism of Arformoterol can be decreased when combined with Zafirlukast.Approved, Investigational
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Zafirlukast.Approved, Investigational
ArtemetherThe metabolism of Artemether can be decreased when combined with Zafirlukast.Approved
AtazanavirThe metabolism of Zafirlukast can be decreased when combined with Atazanavir.Approved, Investigational
AtomoxetineThe metabolism of Zafirlukast can be decreased when combined with Atomoxetine.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Zafirlukast.Approved
BexaroteneThe serum concentration of Zafirlukast can be decreased when it is combined with Bexarotene.Approved, Investigational
BoceprevirThe metabolism of Zafirlukast can be decreased when combined with Boceprevir.Approved
BortezomibThe metabolism of Zafirlukast can be decreased when combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Bosentan can be increased when it is combined with Zafirlukast.Approved, Investigational
BrompheniramineThe metabolism of Brompheniramine can be decreased when combined with Zafirlukast.Approved
BuprenorphineThe metabolism of Buprenorphine can be decreased when combined with Zafirlukast.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Bupropion can be decreased when combined with Zafirlukast.Approved
CabozantinibThe metabolism of Cabozantinib can be decreased when combined with Zafirlukast.Approved
CaffeineThe metabolism of Caffeine can be decreased when combined with Zafirlukast.Approved
CandesartanThe metabolism of Candesartan can be decreased when combined with Zafirlukast.Approved
CapecitabineThe metabolism of Zafirlukast can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Zafirlukast can be increased when combined with Carbamazepine.Approved, Investigational
CarbinoxamineThe metabolism of Carbinoxamine can be decreased when combined with Zafirlukast.Approved
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Zafirlukast.Approved, Investigational
CelecoxibThe metabolism of Celecoxib can be decreased when combined with Zafirlukast.Approved, Investigational
CeritinibThe serum concentration of Zafirlukast can be increased when it is combined with Ceritinib.Approved
ChlorpropamideThe metabolism of Chlorpropamide can be decreased when combined with Zafirlukast.Approved
CholecalciferolThe metabolism of Zafirlukast can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CilostazolThe serum concentration of Cilostazol can be increased when it is combined with Zafirlukast.Approved
CinnarizineThe metabolism of Cinnarizine can be decreased when combined with Zafirlukast.Approved
CisaprideThe metabolism of Cisapride can be decreased when combined with Zafirlukast.Approved, Investigational, Withdrawn
ClarithromycinThe metabolism of Zafirlukast can be decreased when combined with Clarithromycin.Approved
ClemastineThe metabolism of Zafirlukast can be decreased when combined with Clemastine.Approved
ClopidogrelThe metabolism of Zafirlukast can be decreased when combined with Clopidogrel.Approved, Nutraceutical
ClotrimazoleThe metabolism of Zafirlukast can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Clozapine can be decreased when combined with Zafirlukast.Approved
CobicistatThe metabolism of Zafirlukast can be decreased when combined with Cobicistat.Approved
ConivaptanThe serum concentration of Zafirlukast can be increased when it is combined with Conivaptan.Approved, Investigational
CrizotinibThe metabolism of Zafirlukast can be decreased when combined with Crizotinib.Approved
CyclophosphamideThe metabolism of Cyclophosphamide can be decreased when combined with Zafirlukast.Approved, Investigational
CyclosporineThe metabolism of Zafirlukast can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Zafirlukast can be decreased when it is combined with Dabrafenib.Approved
DapagliflozinThe metabolism of Dapagliflozin can be decreased when combined with Zafirlukast.Approved
DapsoneThe metabolism of Dapsone can be decreased when combined with Zafirlukast.Approved, Investigational
DarunavirThe metabolism of Zafirlukast can be decreased when combined with Darunavir.Approved
DasatinibThe serum concentration of Zafirlukast can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Zafirlukast can be decreased when it is combined with Deferasirox.Approved, Investigational
DelavirdineThe metabolism of Zafirlukast can be decreased when combined with Delavirdine.Approved
DexamethasoneThe serum concentration of Zafirlukast can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DextromethorphanThe metabolism of Dextromethorphan can be decreased when combined with Zafirlukast.Approved
DiazepamThe metabolism of Diazepam can be decreased when combined with Zafirlukast.Approved, Illicit, Vet Approved
DiclofenacThe metabolism of Diclofenac can be decreased when combined with Zafirlukast.Approved, Vet Approved
DicoumarolThe serum concentration of Dicoumarol can be increased when it is combined with Zafirlukast.Approved
DihydroergotamineThe metabolism of Zafirlukast can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Zafirlukast can be decreased when combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Zafirlukast.Approved
DolasetronThe metabolism of Dolasetron can be decreased when combined with Zafirlukast.Approved
DonepezilThe metabolism of Donepezil can be decreased when combined with Zafirlukast.Approved
DopamineThe metabolism of Dopamine can be decreased when combined with Zafirlukast.Approved
DorzolamideThe metabolism of Dorzolamide can be decreased when combined with Zafirlukast.Approved
DoxepinThe metabolism of Doxepin can be decreased when combined with Zafirlukast.Approved
DoxycyclineThe metabolism of Zafirlukast can be decreased when combined with Doxycycline.Approved, Investigational, Vet Approved
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Zafirlukast.Approved, Illicit
DronedaroneThe metabolism of Zafirlukast can be decreased when combined with Dronedarone.Approved
DyphyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Dyphylline.Approved
EfavirenzThe serum concentration of Zafirlukast can be decreased when it is combined with Efavirenz.Approved, Investigational
EletriptanThe metabolism of Eletriptan can be decreased when combined with Zafirlukast.Approved, Investigational
EnzalutamideThe serum concentration of Zafirlukast can be decreased when it is combined with Enzalutamide.Approved
EpoprostenolThe metabolism of Epoprostenol can be decreased when combined with Zafirlukast.Approved
ErythromycinThe metabolism of Zafirlukast can be decreased when combined with Erythromycin.Approved, Vet Approved
ErythromycinThe serum concentration of Zafirlukast can be decreased when it is combined with Erythromycin.Approved, Vet Approved
Eslicarbazepine acetateThe serum concentration of Zafirlukast can be decreased when it is combined with Eslicarbazepine acetate.Approved
EstradiolThe metabolism of Estradiol can be decreased when combined with Zafirlukast.Approved, Investigational, Vet Approved
EstroneThe metabolism of Estrone can be decreased when combined with Zafirlukast.Approved
EszopicloneThe metabolism of Eszopiclone can be decreased when combined with Zafirlukast.Approved
Ethyl biscoumacetateThe serum concentration of Ethyl biscoumacetate can be increased when it is combined with Zafirlukast.Withdrawn
EtodolacThe metabolism of Etodolac can be decreased when combined with Zafirlukast.Approved, Investigational, Vet Approved
EtoricoxibThe metabolism of Etoricoxib can be decreased when combined with Zafirlukast.Approved, Investigational
EtravirineThe serum concentration of Zafirlukast can be decreased when it is combined with Etravirine.Approved
FelodipineThe metabolism of Zafirlukast can be decreased when combined with Felodipine.Approved, Investigational
FesoterodineThe serum concentration of the active metabolites of Fesoterodine can be increased when Fesoterodine is used in combination with Zafirlukast.Approved
FloxuridineThe metabolism of Zafirlukast can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Zafirlukast can be decreased when combined with Fluconazole.Approved
FluindioneThe serum concentration of Fluindione can be increased when it is combined with Zafirlukast.Investigational
FlunarizineThe metabolism of Flunarizine can be decreased when combined with Zafirlukast.Approved
FlunitrazepamThe metabolism of Flunitrazepam can be decreased when combined with Zafirlukast.Approved, Illicit
FluorouracilThe metabolism of Zafirlukast can be decreased when combined with Fluorouracil.Approved
FluoxetineThe metabolism of Fluoxetine can be decreased when combined with Zafirlukast.Approved, Vet Approved
FlurbiprofenThe metabolism of Flurbiprofen can be decreased when combined with Zafirlukast.Approved, Investigational
FluvastatinThe metabolism of Fluvastatin can be decreased when combined with Zafirlukast.Approved
FluvoxamineThe metabolism of Zafirlukast can be decreased when combined with Fluvoxamine.Approved, Investigational
FormoterolThe metabolism of Formoterol can be decreased when combined with Zafirlukast.Approved, Investigational
FosamprenavirThe metabolism of Zafirlukast can be decreased when combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Zafirlukast can be increased when it is combined with Fosaprepitant.Approved
FosphenytoinThe metabolism of Zafirlukast can be increased when combined with Fosphenytoin.Approved
Fusidic AcidThe serum concentration of Zafirlukast can be increased when it is combined with Fusidic Acid.Approved
GavestinelThe metabolism of Gavestinel can be decreased when combined with Zafirlukast.Investigational
GemfibrozilThe metabolism of Zafirlukast can be decreased when combined with Gemfibrozil.Approved
GliclazideThe metabolism of Gliclazide can be decreased when combined with Zafirlukast.Approved
GlimepirideThe metabolism of Glimepiride can be decreased when combined with Zafirlukast.Approved
GlipizideThe metabolism of Glipizide can be decreased when combined with Zafirlukast.Approved
GlyburideThe metabolism of Glyburide can be decreased when combined with Zafirlukast.Approved
GuanfacineThe metabolism of Guanfacine can be decreased when combined with Zafirlukast.Approved, Investigational
HaloperidolThe metabolism of Haloperidol can be decreased when combined with Zafirlukast.Approved
HalothaneThe metabolism of Halothane can be decreased when combined with Zafirlukast.Approved, Vet Approved
HexobarbitalThe metabolism of Hexobarbital can be decreased when combined with Zafirlukast.Approved
Histamine PhosphateThe metabolism of Histamine Phosphate can be decreased when combined with Zafirlukast.Approved
HydromorphoneThe metabolism of Hydromorphone can be decreased when combined with Zafirlukast.Approved, Illicit
IbuprofenThe metabolism of Ibuprofen can be decreased when combined with Zafirlukast.Approved
IdarubicinThe metabolism of Idarubicin can be decreased when combined with Zafirlukast.Approved
IdelalisibThe serum concentration of Zafirlukast can be increased when it is combined with Idelalisib.Approved
IfosfamideThe metabolism of Ifosfamide can be decreased when combined with Zafirlukast.Approved
ImatinibThe metabolism of Zafirlukast can be decreased when combined with Imatinib.Approved
IndinavirThe metabolism of Zafirlukast can be decreased when combined with Indinavir.Approved
indisulamThe metabolism of indisulam can be decreased when combined with Zafirlukast.Investigational
IndomethacinThe metabolism of Indomethacin can be decreased when combined with Zafirlukast.Approved, Investigational
IrbesartanThe metabolism of Irbesartan can be decreased when combined with Zafirlukast.Approved, Investigational
IsavuconazoniumThe metabolism of Zafirlukast can be decreased when combined with Isavuconazonium.Approved, Investigational
IsradipineThe metabolism of Zafirlukast can be decreased when combined with Isradipine.Approved
ItraconazoleThe metabolism of Zafirlukast can be decreased when combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Zafirlukast can be increased when it is combined with Ivacaftor.Approved
IxazomibThe metabolism of Ixazomib can be decreased when combined with Zafirlukast.Approved
KetamineThe metabolism of Ketamine can be decreased when combined with Zafirlukast.Approved, Vet Approved
KetobemidoneThe metabolism of Ketobemidone can be decreased when combined with Zafirlukast.Approved
KetoconazoleThe metabolism of Zafirlukast can be decreased when combined with Ketoconazole.Approved, Investigational
KetoprofenThe metabolism of Ketoprofen can be decreased when combined with Zafirlukast.Approved, Vet Approved
LansoprazoleThe metabolism of Lansoprazole can be decreased when combined with Zafirlukast.Approved, Investigational
LapatinibThe metabolism of Zafirlukast can be decreased when combined with Lapatinib.Approved, Investigational
LeflunomideThe metabolism of Leflunomide can be decreased when combined with Zafirlukast.Approved, Investigational
LesinuradThe metabolism of Lesinurad can be decreased when combined with Zafirlukast.Approved
LicofeloneThe metabolism of Licofelone can be decreased when combined with Zafirlukast.Investigational
LidocaineThe metabolism of Lidocaine can be decreased when combined with Zafirlukast.Approved, Vet Approved
LopinavirThe metabolism of Zafirlukast can be decreased when combined with Lopinavir.Approved
LoratadineThe metabolism of Loratadine can be decreased when combined with Zafirlukast.Approved
LornoxicamThe metabolism of Lornoxicam can be decreased when combined with Zafirlukast.Approved
LosartanThe metabolism of Losartan can be decreased when combined with Zafirlukast.Approved
LovastatinThe metabolism of Zafirlukast can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Zafirlukast is combined with Loxapine.Approved
LuliconazoleThe serum concentration of Zafirlukast can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Zafirlukast can be increased when it is combined with Lumacaftor.Approved
LumiracoxibThe metabolism of Lumiracoxib can be decreased when combined with Zafirlukast.Approved, Investigational
Mefenamic acidThe metabolism of Mefenamic acid can be decreased when combined with Zafirlukast.Approved
MelatoninThe metabolism of Melatonin can be decreased when combined with Zafirlukast.Approved, Nutraceutical, Vet Approved
MeloxicamThe metabolism of Meloxicam can be decreased when combined with Zafirlukast.Approved, Vet Approved
MephenytoinThe metabolism of Mephenytoin can be decreased when combined with Zafirlukast.Investigational, Withdrawn
MestranolThe metabolism of Mestranol can be decreased when combined with Zafirlukast.Approved
MethadoneThe metabolism of Methadone can be decreased when combined with Zafirlukast.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Zafirlukast.Approved, Vet Approved
MetoprololThe serum concentration of Metoprolol can be increased when it is combined with Zafirlukast.Approved, Investigational
MetronidazoleThe metabolism of Metronidazole can be decreased when combined with Zafirlukast.Approved
MifepristoneThe serum concentration of Zafirlukast can be increased when it is combined with Mifepristone.Approved, Investigational
MirtazapineThe metabolism of Mirtazapine can be decreased when combined with Zafirlukast.Approved
MitotaneThe serum concentration of Zafirlukast can be decreased when it is combined with Mitotane.Approved
MoclobemideThe metabolism of Moclobemide can be decreased when combined with Zafirlukast.Approved
ModafinilThe serum concentration of Zafirlukast can be decreased when it is combined with Modafinil.Approved, Investigational
MontelukastThe metabolism of Montelukast can be decreased when combined with Zafirlukast.Approved
NafcillinThe serum concentration of Zafirlukast can be decreased when it is combined with Nafcillin.Approved
NaproxenThe metabolism of Naproxen can be decreased when combined with Zafirlukast.Approved, Vet Approved
NateglinideThe metabolism of Nateglinide can be decreased when combined with Zafirlukast.Approved, Investigational
NefazodoneThe metabolism of Zafirlukast can be decreased when combined with Nefazodone.Approved, Withdrawn
NelfinavirThe metabolism of Zafirlukast can be decreased when combined with Nelfinavir.Approved
NetupitantThe serum concentration of Zafirlukast can be increased when it is combined with Netupitant.Approved
NevirapineThe metabolism of Zafirlukast can be increased when combined with Nevirapine.Approved
NicardipineThe metabolism of Zafirlukast can be decreased when combined with Nicardipine.Approved
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Zafirlukast.Approved, Vet Approved
NicotineThe metabolism of Nicotine can be decreased when combined with Zafirlukast.Approved
NilotinibThe metabolism of Zafirlukast can be decreased when combined with Nilotinib.Approved, Investigational
NortriptylineThe metabolism of Nortriptyline can be decreased when combined with Zafirlukast.Approved
OlaparibThe metabolism of Zafirlukast can be decreased when combined with Olaparib.Approved
OlodaterolThe metabolism of Olodaterol can be decreased when combined with Zafirlukast.Approved
OmeprazoleThe metabolism of Zafirlukast can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronThe metabolism of Ondansetron can be decreased when combined with Zafirlukast.Approved
OsimertinibThe serum concentration of Zafirlukast can be increased when it is combined with Osimertinib.Approved
OspemifeneThe metabolism of Ospemifene can be decreased when combined with Zafirlukast.Approved
OxaprozinThe metabolism of Oxaprozin can be decreased when combined with Zafirlukast.Approved
PaclitaxelThe metabolism of Paclitaxel can be decreased when combined with Zafirlukast.Approved, Vet Approved
PalbociclibThe serum concentration of Zafirlukast can be increased when it is combined with Palbociclib.Approved
ParamethadioneThe metabolism of Paramethadione can be decreased when combined with Zafirlukast.Approved
ParecoxibThe metabolism of Parecoxib can be decreased when combined with Zafirlukast.Approved
PentobarbitalThe metabolism of Zafirlukast can be increased when combined with Pentobarbital.Approved, Vet Approved
PerphenazineThe metabolism of Perphenazine can be decreased when combined with Zafirlukast.Approved
PhenacetinThe metabolism of Phenacetin can be decreased when combined with Zafirlukast.Withdrawn
PhenindioneThe serum concentration of Phenindione can be increased when it is combined with Zafirlukast.Approved
PhenobarbitalThe metabolism of Zafirlukast can be increased when combined with Phenobarbital.Approved
PhenprocoumonThe serum concentration of Phenprocoumon can be increased when it is combined with Zafirlukast.Approved
PhenylbutazoneThe metabolism of Phenylbutazone can be decreased when combined with Zafirlukast.Approved, Vet Approved
PhenytoinThe metabolism of Zafirlukast can be increased when combined with Phenytoin.Approved, Vet Approved
PioglitazoneThe metabolism of Pioglitazone can be decreased when combined with Zafirlukast.Approved, Investigational
PiroxicamThe metabolism of Piroxicam can be decreased when combined with Zafirlukast.Approved, Investigational
PitavastatinThe metabolism of Pitavastatin can be decreased when combined with Zafirlukast.Approved
PosaconazoleThe metabolism of Zafirlukast can be decreased when combined with Posaconazole.Approved, Investigational, Vet Approved
PrasugrelThe metabolism of Prasugrel can be decreased when combined with Zafirlukast.Approved
PravastatinThe metabolism of Pravastatin can be decreased when combined with Zafirlukast.Approved
PrimidoneThe metabolism of Zafirlukast can be increased when combined with Primidone.Approved, Vet Approved
ProgesteroneThe metabolism of Progesterone can be decreased when combined with Zafirlukast.Approved, Vet Approved
ProguanilThe metabolism of Proguanil can be decreased when combined with Zafirlukast.Approved
PromazineThe metabolism of Promazine can be decreased when combined with Zafirlukast.Approved, Vet Approved
PropofolThe metabolism of Propofol can be decreased when combined with Zafirlukast.Approved, Investigational, Vet Approved
PyrimethamineThe metabolism of Zafirlukast can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuazepamThe metabolism of Quazepam can be decreased when combined with Zafirlukast.Approved, Illicit
QuinidineThe metabolism of Quinidine can be decreased when combined with Zafirlukast.Approved
QuinineThe metabolism of Zafirlukast can be decreased when combined with Quinine.Approved
RabeprazoleThe metabolism of Zafirlukast can be decreased when combined with Rabeprazole.Approved, Investigational
RanolazineThe metabolism of Zafirlukast can be decreased when combined with Ranolazine.Approved, Investigational
RifabutinThe metabolism of Zafirlukast can be increased when combined with Rifabutin.Approved
RifampicinThe metabolism of Zafirlukast can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Zafirlukast can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Zafirlukast can be decreased when combined with Ritonavir.Approved, Investigational
RofecoxibThe metabolism of Rofecoxib can be decreased when combined with Zafirlukast.Investigational, Withdrawn
RosiglitazoneThe metabolism of Rosiglitazone can be decreased when combined with Zafirlukast.Approved, Investigational
RosuvastatinThe metabolism of Rosuvastatin can be decreased when combined with Zafirlukast.Approved
Salicylic acidThe metabolism of Salicylic acid can be decreased when combined with Zafirlukast.Approved, Vet Approved
SaquinavirThe metabolism of Zafirlukast can be decreased when combined with Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Zafirlukast can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe metabolism of Selegiline can be decreased when combined with Zafirlukast.Approved, Investigational, Vet Approved
SeratrodastThe metabolism of Seratrodast can be decreased when combined with Zafirlukast.Approved, Investigational
SertralineThe metabolism of Sertraline can be decreased when combined with Zafirlukast.Approved
SildenafilThe metabolism of Zafirlukast can be decreased when combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Zafirlukast can be decreased when it is combined with Siltuximab.Approved
SimeprevirThe serum concentration of Zafirlukast can be increased when it is combined with Simeprevir.Approved
SitaxentanThe metabolism of Sitaxentan can be decreased when combined with Zafirlukast.Approved, Investigational, Withdrawn
SorafenibThe metabolism of Zafirlukast can be decreased when combined with Sorafenib.Approved, Investigational
St. John's WortThe serum concentration of Zafirlukast can be decreased when it is combined with St. John's Wort.Nutraceutical
StiripentolThe serum concentration of Zafirlukast can be increased when it is combined with Stiripentol.Approved
SulfadiazineThe metabolism of Zafirlukast can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Sulfamethoxazole can be decreased when combined with Zafirlukast.Approved
SulfamoxoleThe metabolism of Sulfamoxole can be decreased when combined with Zafirlukast.Approved
SulfinpyrazoneThe metabolism of Sulfinpyrazone can be decreased when combined with Zafirlukast.Approved
SulfisoxazoleThe metabolism of Zafirlukast can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
SuprofenThe metabolism of Suprofen can be decreased when combined with Zafirlukast.Approved, Withdrawn
TamoxifenThe metabolism of Tamoxifen can be decreased when combined with Zafirlukast.Approved
TapentadolThe metabolism of Tapentadol can be decreased when combined with Zafirlukast.Approved
TelaprevirThe metabolism of Zafirlukast can be decreased when combined with Telaprevir.Approved
TelithromycinThe metabolism of Zafirlukast can be decreased when combined with Telithromycin.Approved
TemazepamThe metabolism of Temazepam can be decreased when combined with Zafirlukast.Approved
TenoxicamThe metabolism of Tenoxicam can be decreased when combined with Zafirlukast.Approved
TerbinafineThe metabolism of Terbinafine can be decreased when combined with Zafirlukast.Approved, Investigational, Vet Approved
TerfenadineThe metabolism of Terfenadine can be decreased when combined with Zafirlukast.Withdrawn
TeriflunomideThe metabolism of Zafirlukast can be decreased when combined with Teriflunomide.Approved
TestosteroneThe metabolism of Testosterone can be decreased when combined with Zafirlukast.Approved, Investigational
ThalidomideThe metabolism of Thalidomide can be decreased when combined with Zafirlukast.Approved, Investigational, Withdrawn
TheophyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Theophylline.Approved
ThiamylalThe metabolism of Thiamylal can be decreased when combined with Zafirlukast.Approved, Vet Approved
ThioridazineThe serum concentration of Thioridazine can be increased when it is combined with Zafirlukast.Approved
TicagrelorThe metabolism of Zafirlukast can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Zafirlukast can be decreased when combined with Ticlopidine.Approved
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Zafirlukast.Approved
TocilizumabThe serum concentration of Zafirlukast can be decreased when it is combined with Tocilizumab.Approved
TolbutamideThe metabolism of Zafirlukast can be decreased when combined with Tolbutamide.Approved
TolterodineThe metabolism of Tolterodine can be decreased when combined with Zafirlukast.Approved, Investigational
TorasemideThe metabolism of Torasemide can be decreased when combined with Zafirlukast.Approved
TrabectedinThe metabolism of Trabectedin can be decreased when combined with Zafirlukast.Approved, Investigational
TreprostinilThe metabolism of Treprostinil can be decreased when combined with Zafirlukast.Approved, Investigational
TretinoinThe metabolism of Tretinoin can be decreased when combined with Zafirlukast.Approved, Investigational, Nutraceutical
TrimethadioneThe metabolism of Trimethadione can be decreased when combined with Zafirlukast.Approved
TrimethoprimThe metabolism of Zafirlukast can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe metabolism of Trimipramine can be decreased when combined with Zafirlukast.Approved
TroglitazoneThe metabolism of Troglitazone can be decreased when combined with Zafirlukast.Withdrawn
ValdecoxibThe metabolism of Valdecoxib can be decreased when combined with Zafirlukast.Investigational, Withdrawn
Valproic AcidThe metabolism of Zafirlukast can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Zafirlukast can be decreased when combined with Valsartan.Approved, Investigational
VenlafaxineThe metabolism of Zafirlukast can be decreased when combined with Venlafaxine.Approved
VerapamilThe metabolism of Zafirlukast can be decreased when combined with Verapamil.Approved
VicrivirocThe metabolism of Vicriviroc can be decreased when combined with Zafirlukast.Investigational
VismodegibThe metabolism of Vismodegib can be decreased when combined with Zafirlukast.Approved
VoriconazoleThe metabolism of Zafirlukast can be decreased when combined with Voriconazole.Approved, Investigational
VortioxetineThe metabolism of Vortioxetine can be decreased when combined with Zafirlukast.Approved
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Zafirlukast.Approved
XimelagatranThe metabolism of Ximelagatran can be decreased when combined with Zafirlukast.Approved, Investigational, Withdrawn
ZalcitabineThe metabolism of Zalcitabine can be decreased when combined with Zafirlukast.Approved
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Zafirlukast.Approved
ZidovudineThe metabolism of Zidovudine can be decreased when combined with Zafirlukast.Approved
ZileutonThe metabolism of Zileuton can be decreased when combined with Zafirlukast.Approved, Investigational, Withdrawn
ZiprasidoneThe metabolism of Zafirlukast can be decreased when combined with Ziprasidone.Approved
ZolpidemThe metabolism of Zolpidem can be decreased when combined with Zafirlukast.Approved
ZopicloneThe metabolism of Zopiclone can be decreased when combined with Zafirlukast.Approved
Food Interactions
  • Take on empty stomach: 1 hour before or 2 hours after meals.
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)
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
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

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 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on August 17, 2016 12:23