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, coated10 mg/1OralPar Pharmaceutical2015-11-01Not applicableUs
AccolateTablet, film coated10 mg/1OralAstra Zeneca Lp1996-10-012017-04-28Us
AccolateTablet, film coated10 mg/1OralPar Pharmaceutical2015-01-09Not applicableUs
AccolateTablet, film coated20 mg/1OralPhysicians Total Care, Inc.1996-09-262011-09-30Us
AccolateTablet, coated20 mg/1OralPar Pharmaceutical2015-11-01Not applicableUs
AccolateTablet, film coated20 mg/1OralState of Florida DOH Central Pharmacy2009-07-01Not applicableUs
AccolateTablet, film coated20 mg/1OralAstra Zeneca Lp1996-10-012017-09-29Us
AccolateTablet, film coated20 mg/1OralPar Pharmaceutical2015-01-09Not applicableUs49884 01120180907 15195 uthax8
Accolate Tab 20 mgTablet20 mgOralAstra Zeneca1997-11-17Not applicableCanada
ZafirlukastTablet, coated10 mg/1OralPar Pharmaceutical2010-11-19Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ZafirlukastTablet, film coated20 mg/1OralAmerincan Health Packaging2013-05-22Not applicableUs
ZafirlukastTablet, film coated10 mg/1OralDr Reddy's Laboratories2010-11-18Not applicableUs55111 0625 01 nlmimage10 b53f5afa
ZafirlukastTablet, film coated20 mg/1OralCarilion Materials Management2010-11-18Not applicableUs68151 197720180907 15195 16eodxo
ZafirlukastTablet, film coated20 mg/1OralAvPAK2017-09-15Not applicableUs
ZafirlukastTablet, film coated20 mg/1OralDr Reddy's Laboratories2010-11-18Not applicableUs55111 0626 60 nlmimage10 233f11c8
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.

Associated Conditions
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
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Zafirlukast.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Zafirlukast.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of Zafirlukast can be decreased when it is combined with 3-isobutyl-1-methyl-7H-xanthine.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Zafirlukast.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Zafirlukast.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Zafirlukast.
6-O-benzylguanineThe serum concentration of Zafirlukast can be decreased when it is combined with 6-O-benzylguanine.
7-DeazaguanineThe serum concentration of Zafirlukast can be decreased when it is combined with 7-Deazaguanine.
7,9-DimethylguanineThe serum concentration of Zafirlukast can be decreased when it is combined with 7,9-Dimethylguanine.
8-azaguanineThe serum concentration of Zafirlukast can be decreased when it is combined with 8-azaguanine.
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
HMDB0014689
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
  • AstraZeneca Inc.
  • Cardinal Health
  • IPR Pharmaceuticals Inc.
  • Murfreesboro Pharmaceutical Nursing Supply
  • Physicians Total Care Inc.
  • Resource Optimization and Innovation LLC
  • Zeneca Pharma Inc.
Dosage forms
FormRouteStrength
Tablet, coatedOral10 mg/1
Tablet, coatedOral20 mg/1
TabletOral20 mg
Tablet, film coatedOral10 mg/1
Tablet, film 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)
US5612367No1997-03-182014-03-18Us
US4859692No1989-08-222010-09-26Us
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]
  4. Zafirlukast FDA label [File]
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]
  3. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
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
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
Curator comments
Data is limited to in vitro studies.
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]
  2. Shader RI, Granda BW, von Moltke LL, Giancarlo GM, Greenblatt DJ: Inhibition of human cytochrome P450 isoforms in vitro by zafirlukast. Biopharm Drug Dispos. 1999 Nov;20(8):385-8. [PubMed:10870095]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Data supporting this enzyme inhibition is limited to one in vitro study.
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. Shader RI, Granda BW, von Moltke LL, Giancarlo GM, Greenblatt DJ: Inhibition of human cytochrome P450 isoforms in vitro by zafirlukast. Biopharm Drug Dispos. 1999 Nov;20(8):385-8. [PubMed:10870095]
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]
  2. Shader RI, Granda BW, von Moltke LL, Giancarlo GM, Greenblatt DJ: Inhibition of human cytochrome P450 isoforms in vitro by zafirlukast. Biopharm Drug Dispos. 1999 Nov;20(8):385-8. [PubMed:10870095]

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 21, 2018 10:03