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

Hepatic

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

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

US20040186300
General ReferencesNot Available
External Links
ATC CodesR03DC01
AHFS Codes
  • 48:10.24
PDB EntriesNot Available
FDA labelDownload (233 KB)
MSDSDownload (57.6 KB)
Interactions
Drug Interactions
Drug
AcenocoumarolThe serum concentration of Acenocoumarol can be increased when it is combined with Zafirlukast.
AminophyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Aminophylline.
AmodiaquineThe serum concentration of Amodiaquine can be increased when it is combined with Zafirlukast.
AripiprazoleThe serum concentration of Aripiprazole can be increased when it is combined with Zafirlukast.
BosentanThe serum concentration of Bosentan can be increased when it is combined with Zafirlukast.
CarvedilolThe serum concentration of Carvedilol can be increased when it is combined with Zafirlukast.
CeritinibThe serum concentration of Zafirlukast can be increased when it is combined with Ceritinib.
DabrafenibThe serum concentration of Zafirlukast can be decreased when it is combined with Dabrafenib.
DicoumarolThe serum concentration of Dicoumarol can be increased when it is combined with Zafirlukast.
DronabinolThe serum concentration of Dronabinol can be increased when it is combined with Zafirlukast.
ErythromycinThe serum concentration of Zafirlukast can be decreased when it is combined with Erythromycin.
FloxuridineThe metabolism of Zafirlukast can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Zafirlukast can be decreased when combined with Fluconazole.
LoxapineThe risk or severity of adverse effects can be increased when Zafirlukast is combined with Loxapine.
LumacaftorThe serum concentration of Zafirlukast can be decreased when it is combined with Lumacaftor.
MifepristoneThe serum concentration of Zafirlukast can be increased when it is combined with Mifepristone.
PhenytoinThe metabolism of Zafirlukast can be increased when combined with Phenytoin.
SecobarbitalThe metabolism of Zafirlukast can be increased when combined with Secobarbital.
SildenafilThe metabolism of Sildenafil can be decreased when combined with Zafirlukast.
SulfisoxazoleThe metabolism of Zafirlukast can be decreased when combined with Sulfisoxazole.
TheophyllineThe serum concentration of Zafirlukast can be decreased when it is combined with Theophylline.
TizanidineThe serum concentration of Tizanidine can be increased when it is combined with Zafirlukast.
WarfarinThe serum concentration of Warfarin can be increased when it is combined with Zafirlukast.
Food Interactions
  • Take on empty stomach: 1 hour before or 2 hours after meals.

Targets

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

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Walsky RL, Gaman EA, Obach RS: Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78. [PubMed:15601807 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Prostaglandin-endoperoxide synthase activity
Specific Function:
Converts arachidonate to prostaglandin H2 (PGH2), a committed step in prostanoid synthesis. Involved in the constitutive production of prostanoids in particular in the stomach and platelets. In gastric epithelial cells, it is a key step in the generation of prostaglandins, such as prostaglandin E2 (PGE2), which plays an important role in cytoprotection. In platelets, it is involved in the gener...
Gene Name:
PTGS1
Uniprot ID:
P23219
Molecular Weight:
68685.82 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrateinhibitor
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Zhou SF, Zhou ZW, Yang LP, Cai JP: Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675. Epub 2009 Sep 1. [PubMed:19515014 ]
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Steroid hydroxylase activity
Specific Function:
Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
Gene Name:
CYP2E1
Uniprot ID:
P05181
Molecular Weight:
56848.42 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
Antagonist
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Sun YL, Kathawala RJ, Singh S, Zheng K, Talele TT, Jiang WQ, Chen ZS: Zafirlukast antagonizes ATP-binding cassette subfamily G member 2-mediated multidrug resistance. Anticancer Drugs. 2012 Sep;23(8):865-73. doi: 10.1097/CAD.0b013e328354a196. [PubMed:22614107 ]
Comments
comments powered by Disqus
Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:11