Identification

Name
Zafirlukast
Accession Number
DB00549  (APRD00377)
Type
Small Molecule
Groups
Approved, Investigational
Description

Zafirlukast 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
  • Cyclopentyl 3-(2-methoxy-4-((O-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate
  • ICI-204,219
External IDs
ICI 204,219
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AccolateTablet, film coated10 mg/1OralPar Pharmaceutical2015-01-09Not applicableUs
AccolateTablet, film coated20 mg/1OralAstra Zeneca Lp1996-10-01Not applicableUs
AccolateTablet, film coated10 mg/1OralAstra Zeneca Lp1996-10-01Not applicableUs
AccolateTablet, film coated20 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
AccolateTablet, film coated20 mg/1OralPar Pharmaceutical2015-01-09Not applicableUs
AccolateTablet, coated10 mg/1OralPar Pharmaceutical2015-11-01Not applicableUs
AccolateTablet, coated20 mg/1OralPar Pharmaceutical2015-11-01Not applicableUs
Accolate Tab 20 mgTablet20 mgOralAstra Zeneca1997-11-17Not applicableCanada
ZafirlukastTablet, coated20 mg/1OralAvera Mc Kennan Hospital2016-06-06Not applicableUs
ZafirlukastTablet, coated20 mg/1OralPar Pharmaceutical2015-12-16Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ZafirlukastTablet, film coated10 mg/1OralDr Reddy's Laboratories2010-11-18Not applicableUs55111 0625 01 nlmimage10 b53f5afa
ZafirlukastTablet, film coated20 mg/1OralCarilion Materials Management2010-11-18Not applicableUs
ZafirlukastTablet, film coated20 mg/1OralDr Reddy's Laboratories2010-11-18Not applicableUs55111 0626 60 nlmimage10 233f11c8
ZafirlukastTablet, film coated20 mg/1OralAv Pak2017-09-15Not applicableUs
ZafirlukastTablet, film coated20 mg/1OralAmerincan Health Packaging2013-06-07Not applicableUs
International/Other Brands
Accolate
Categories
UNII
XZ629S5L50
CAS number
107753-78-6
Weight
Average: 575.675
Monoisotopic: 575.209006493
Chemical Formula
C31H33N3O6S
InChI Key
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

Pharmacology

Indication

For the prophylaxis and chronic treatment of asthma.

Structured Indications
Pharmacodynamics

Zafirlukast 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 action

Zafirlukast 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.

TargetActionsOrganism
ACysteinyl leukotriene receptor 1
antagonist
Human
Absorption

Rapidly absorbed following oral administration, reduced following a high-fat or high-protein meal.

Volume of distribution
  • 70 L
Protein binding

99%

Metabolism

Hepatic

Route of elimination

The most common metabolic products are hydroxylated metabolites which are excreted in the feces.

Half life

10 hours

Clearance
  • apparent oral CL=20 L/h
  • 11.4 L/h [7-11 yrs]
  • 9.2 L/h [5-6 yrs]
Toxicity

Side effects include rash and upset stomach.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not 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, Investigational
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, Investigational
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, Investigational
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
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
AtorvastatinThe risk or severity of adverse effects can be increased when Zafirlukast is combined with Atorvastatin.Approved
AzelastineThe metabolism of Azelastine can be decreased when combined with Zafirlukast.Approved
BexaroteneThe metabolism of Bexarotene can be decreased when combined with Zafirlukast.Approved, Investigational
BoceprevirThe metabolism of Zafirlukast can be decreased when combined with Boceprevir.Approved, Withdrawn
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
BrivaracetamThe metabolism of Brivaracetam can be decreased when combined with Zafirlukast.Approved, Investigational
BromocriptineThe risk or severity of adverse effects can be increased when Bromocriptine 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
CabergolineThe risk or severity of adverse effects can be increased when Cabergoline is 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
Candesartan cilexetilThe 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
CerivastatinThe serum concentration of Cerivastatin can be increased when it is combined with Zafirlukast.Withdrawn
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, Investigational
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 Clopidogrel can be decreased when combined with Zafirlukast.Approved, Nutraceutical
ClorindioneThe serum concentration of Clorindione can be increased when it is combined with Zafirlukast.Experimental
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
CrisaboroleThe metabolism of Zafirlukast can be decreased when combined with Crisaborole.Approved
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
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
DihydroergocornineThe risk or severity of adverse effects can be increased when Dihydroergocornine is combined with Zafirlukast.Approved
DihydroergocristineThe risk or severity of adverse effects can be increased when Dihydroergocristine is combined with Zafirlukast.Experimental
DihydroergocryptineThe risk or severity of adverse effects can be increased when Dihydroergocryptine is combined with Zafirlukast.Experimental
DihydroergotamineThe metabolism of Zafirlukast can be decreased when combined with Dihydroergotamine.Approved
DiltiazemThe metabolism of Zafirlukast can be decreased when combined with Diltiazem.Approved
DiphenadioneThe serum concentration of Diphenadione can be increased when it is combined with Zafirlukast.Experimental
DiphenhydramineThe metabolism of Diphenhydramine can be decreased when combined with Zafirlukast.Approved
DoconexentThe metabolism of Doconexent can be decreased when combined with Zafirlukast.Approved, Investigational
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
DosulepinThe metabolism of Zafirlukast can be decreased when combined with Dosulepin.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 metabolism of Zafirlukast can be decreased when combined with Efavirenz.Approved, Investigational
EletriptanThe metabolism of Eletriptan can be decreased when combined with Zafirlukast.Approved, Investigational
EnasidenibThe metabolism of Enasidenib can be decreased when combined with Zafirlukast.Approved
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
ErgonovineThe risk or severity of adverse effects can be increased when Ergonovine is combined with Zafirlukast.Approved
ErgotamineThe risk or severity of adverse effects can be increased when Ergotamine is combined with Zafirlukast.Approved
ErythromycinThe serum concentration of Zafirlukast can be decreased when it is combined with Erythromycin.Approved, Vet 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 metabolism of Etravirine can be decreased when combined with Zafirlukast.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
HistamineThe metabolism of Histamine can be decreased when combined with Zafirlukast.Approved, Investigational
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, Investigational
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
LisurideThe risk or severity of adverse effects can be increased when Lisuride is combined with Zafirlukast.Approved, Investigational
LobeglitazoneThe metabolism of Zafirlukast can be decreased when combined with Lobeglitazone.Approved, Investigational
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, Investigational
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
Lysergic Acid DiethylamideThe risk or severity of adverse effects can be increased when Lysergic Acid Diethylamide is combined with Zafirlukast.Illicit, Investigational, Withdrawn
ManidipineThe metabolism of Zafirlukast can be decreased when combined with Manidipine.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
MetergolineThe risk or severity of adverse effects can be increased when Metergoline is combined with Zafirlukast.Experimental
MethadoneThe metabolism of Methadone can be decreased when combined with Zafirlukast.Approved
MethoxyfluraneThe metabolism of Methoxyflurane can be decreased when combined with Zafirlukast.Approved, Investigational, Vet Approved
MethylergometrineThe risk or severity of adverse effects can be increased when Methylergometrine is combined with Zafirlukast.Approved
MethysergideThe risk or severity of adverse effects can be increased when Methysergide is combined with Zafirlukast.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
MevastatinThe serum concentration of Mevastatin can be increased when it is combined with Zafirlukast.Experimental
MidostaurinThe metabolism of Zafirlukast can be decreased when combined with Midostaurin.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
MontelukastThe metabolism of Montelukast can be decreased when combined with Zafirlukast.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
NicergolineThe risk or severity of adverse effects can be increased when Nicergoline is combined with Zafirlukast.Approved, Investigational
NiclosamideThe metabolism of Niclosamide can be decreased when combined with Zafirlukast.Approved, Investigational, 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 Omeprazole can be decreased when combined with Zafirlukast.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
PergolideThe risk or severity of adverse effects can be increased when Pergolide is combined with Zafirlukast.Approved, Investigational, Vet Approved, Withdrawn
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, Investigational
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, Investigational
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 Quinine can be decreased when combined with Zafirlukast.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
RupatadineThe metabolism of Rupatadine 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
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
SimvastatinThe serum concentration of Simvastatin can be increased when it is combined with Zafirlukast.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.Investigational, 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, Withdrawn
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
TergurideThe risk or severity of adverse effects can be increased when Terguride is combined with Zafirlukast.Experimental
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, Withdrawn
TicagrelorThe metabolism of Zafirlukast can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Zafirlukast can be decreased when combined with Ticlopidine.Approved
TioclomarolThe serum concentration of Tioclomarol can be increased when it is combined with Zafirlukast.Experimental
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
TopiroxostatThe metabolism of Zafirlukast can be decreased when combined with Topiroxostat.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 Trimethoprim can be decreased when combined with Zafirlukast.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.Investigational, Withdrawn
UbidecarenoneThe serum concentration of Ubidecarenone can be increased when it is combined with Zafirlukast.Approved, Experimental
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, Investigational
ZaltoprofenThe metabolism of Zaltoprofen can be decreased when combined with Zafirlukast.Approved, Investigational
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 References
Not Available
External Links
Human Metabolome Database
HMDB14689
KEGG Drug
D00411
KEGG Compound
C07206
PubChem Compound
5717
PubChem Substance
46506874
ChemSpider
5515
BindingDB
50009073
ChEBI
10100
ChEMBL
CHEMBL603
Therapeutic Targets Database
DAP000091
PharmGKB
PA451949
IUPHAR
3322
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Zafirlukast
ATC Codes
R03DC01 — Zafirlukast
AHFS Codes
  • 48:10.24 — Leukotriene Modifiers
FDA label
Download (233 KB)
MSDS
Download (57.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedTreatmentHealthy Volunteers1
2RecruitingTreatmentCancer, Breast1

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)
US5612367No1994-03-182014-03-18Us
US4859692No1993-09-262010-09-26Us
CA2056066No2002-04-022011-11-22Canada
CA1340567No1999-06-012016-06-01Canada

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)139 °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 FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-0003191000-ba3996913abfda3b22c4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0a4r-0259300000-1440474b4cb47824c9f2
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0002-0001191000-58bcdb71b459847fc794
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0ap0-0149300000-896e679131032968db95

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Benzenesulfonamides
Direct Parent
Benzenesulfonamides
Alternative Parents
3-alkylindoles / N-alkylindoles / Benzenesulfonyl compounds / Benzoic acids and derivatives / Phenoxy compounds / Benzoyl derivatives / Anisoles / Methoxybenzenes / Toluenes / Alkyl aryl ethers
show 12 more
Substituents
Benzenesulfonamide / N-alkylindole / 3-alkylindole / Benzoic acid or derivatives / Benzenesulfonyl group / Indole / Indole or derivatives / Phenoxy compound / Anisole / Benzoyl
show 28 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
carbamate ester, sulfonamide, indoles (CHEBI:10100)

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, e...
Gene Name
CYSLTR1
Uniprot ID
Q9Y271
Uniprot Name
Cysteinyl leukotriene receptor 1
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

Details
1. Cytochrome P450 2C9
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
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
Substrate
Inhibitor
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 un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
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 gas...
Gene Name
PTGS1
Uniprot ID
P23219
Uniprot Name
Prostaglandin G/H synthase 1
Molecular Weight
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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 un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
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 im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
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...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
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 ...
Gene Name
CYP2E1
Uniprot ID
P05181
Uniprot Name
Cytochrome P450 2E1
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 fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
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]

Drug created on June 13, 2005 07:24 / Updated on November 13, 2017 21:49