U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C31H33N3O6S
Molecular Weight 575.675
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ZAFIRLUKAST

SMILES

COC1=CC(=CC=C1CC2=CN(C)C3=C2C=C(NC(=O)OC4CCCC4)C=C3)C(=O)NS(=O)(=O)C5=CC=CC=C5C

InChI

InChIKey=YEEZWCHGZNKEEK-UHFFFAOYSA-N
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)

HIDE SMILES / InChI
Molecular Formula C31H33N3O6S
Molecular Weight 575.675
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020547s027lbl.pdf

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. Zafirlukast is 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. 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. Zafirlukast is marketed by Astra Zeneca with the brand names Accolate, Accoleit, and Vanticon. It was the first LTRA to be marketed in the USA and is now approved in over 60 countries, including the UK, Japan, Taiwan, Italy, Spain, Canada, Brazil, China and Turkey.

CNS Activity

CNS Non-penetrant
1040
Curator's Comment: Studies in rats using radiolabeled Zafirlukast indicate minimal distribution across the blood-brain barrier.

Originator

Approval Year

1996
224
Targets

Targets

Primary TargetPharmacologyConditionPotency
Antagonist
2849
 1.1 nM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8583
ACCOLATE

Approved Use

ACCOLATE is indicated for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older.

Launch Date

1996
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
352.7 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/11888331
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ZAFIRLUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1090.41 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/11888331
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ZAFIRLUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
2.3 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/11888331
20 mg single, oral
dose: 20 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
ZAFIRLUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Other AEs: Pharyngitis, Headache...
Other AEs:
Pharyngitis (24.7%)
Headache (13.8%)
Myalgia (3.7%)
Sinusitis (3.5%)
Flu syndrome (3.3%)
Cough increased (3.1%)
Rash (3.1%)
Rhinitis (3.1%)
Accidental injury (3.1%)
Nausea (3.1%)
Back pain (2.9%)
Hypertonia (2.9%)
Diarrhea (2.7%)
Exacerbation of asthma (2.7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
20 mg 2 times / day multiple, oral
Highest studied dose
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
unhealthy, 37
Health Status: unhealthy
Age Group: 37
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
Other AEs: Headache, Gastritis...
Other AEs:
Headache (7%)
Gastritis (1%)
Pharyngitis (20%)
Rhinitis (7%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
AEs

AEs

AESignificanceDosePopulation
Headache 13.8%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Diarrhea 2.7%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Exacerbation of asthma 2.7%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Back pain 2.9%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Hypertonia 2.9%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Pharyngitis 24.7%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Accidental injury 3.1%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Cough increased 3.1%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Nausea 3.1%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Rash 3.1%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Rhinitis 3.1%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Flu syndrome 3.3%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Sinusitis 3.5%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Myalgia 3.7%
20 mg 2 times / day multiple, oral
Recommended
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
unhealthy, 12-76
Health Status: unhealthy
Age Group: 12-76
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/9377612/
Gastritis 1%
20 mg 2 times / day multiple, oral
Highest studied dose
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
unhealthy, 37
Health Status: unhealthy
Age Group: 37
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
Pharyngitis 20%
20 mg 2 times / day multiple, oral
Highest studied dose
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
unhealthy, 37
Health Status: unhealthy
Age Group: 37
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
Headache 7%
20 mg 2 times / day multiple, oral
Highest studied dose
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
unhealthy, 37
Health Status: unhealthy
Age Group: 37
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
Rhinitis 7%
20 mg 2 times / day multiple, oral
Highest studied dose
Dose: 20 mg, 2 times / day
Route: oral
Route: multiple
Dose: 20 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
unhealthy, 37
Health Status: unhealthy
Age Group: 37
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/8087328/
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:10100
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:10100
ChemicalBook
CB8703479
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB8703479
eMolecules
1989568
https://www.emolecules.com/cgi-bin/more?vid=1989568
MolPort
MolPort-003-850-873
https://www.molport.com/shop/molecule-link/MolPort-003-850-873
Selleck Chemicals
Zafirlukast(Accolate)
http://www.selleckchem.com/products/Zafirlukast(Accolate).html
ZINC
ZINC000000896717
http://zinc15.docking.org/substances/ZINC000000896717
PubMed

PubMed

TitleDatePubMed
Participation of chemical mediators other than histamine in nasal allergy signs: a study using mice lacking histamine H(1) receptors.
2002-08-09
Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice.
2002-08-01
Vasculitis induced by zafirlukast therapy.
2002-08
[Aspirin induced asthma, urinary leukotriene E4 and zafirlukast].
2002-07-03
Effects of adding either a leukotriene receptor antagonist or low-dose theophylline to a low or medium dose of inhaled corticosteroid in patients with persistent asthma.
2002-07
Efficacy and safety of low-dose fluticasone propionate compared with zafirlukast in patients with persistent asthma.
2002-07
Churg-Strauss syndrome in a case of asthma.
2002-07
Novel phthalimide derivatives, designed as leukotriene D(4) receptor antagonists.
2002-06-03
5-Lipoxygenase polymorphism and in-vivo response to leukotriene receptor antagonists.
2002-06
Antitussive effect of the leukotriene receptor antagonist zafirlukast in subjects with cough-variant asthma.
2002-06
Pulmonary function changes and immunomodulation of cytokine expression by zafirlukast after sensitization and allergen challenge in brown Norway rats.
2002-06
[New horizons in the treatment of atopic dermatitis].
2002-05-04
Comparison of second controller medications in addition to inhaled corticosteroid in patients with moderate asthma.
2002-05
Influence of zafirlukast and loratadine on exercise-induced bronchoconstriction.
2002-05
Exercise-induced asthma: is there still a case for histamine?
2002-05
Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma.
2002-04-15
[Reflections on antileukotrienes].
2002-04-15
Pharmacogenetics of asthma.
2002-04-01
Loss of response to treatment with leukotriene receptor antagonists but not inhaled corticosteroids in patients over 50 years of age.
2002-04
Where do leukotriene modifiers fit in asthma management?
2002-04
[Zafirlukast (Accolate): a review of its pharmacological and clinical profile].
2002-04
An open study to evaluate the safety and efficacy of zafirlukast ("Accolate") in patients with mild to moderate asthma in Ibadan, Nigeria.
2002-03-12
[Zafirlukast in treatment of nasal polyps in patients with aspirin intolerant bronchial asthma--preliminary report].
2002-03
Leukotriene modifiers: novel therapeutic opportunities in asthma.
2002-03
Prevalence of serious eosinophilia and incidence of Churg-Strauss syndrome in a cohort of asthma patients.
2002-03
Treatment of canine atopic dermatitis with zafirlukast, a leukotriene-receptor antagonist: a single-blinded, placebo-controlled study.
2002-03
Inhaled fluticasone and zafirlukast in persistent asthma.
2002-03
[Churg-Strauss syndrome after treatment with Singulair (montelukast)].
2002-02-20
Receptor preferences of cysteinyl-leukotrienes in the guinea pig lung parenchyma.
2002-02-01
Economic impact of asthma therapy with fluticasone propionate, montelukast, or zafirlukast in a managed care population.
2002-02
Pharmacoeconomic studies of asthma controller drugs: marketing gimmick or icing on the cake?
2002-02
[Study on relationship between leukotrienes and exercise-induced asthma].
2002-01-10
Leukotriene receptor antagonists in the treatment of asthma: an update.
2002
Pharmacokinetic profile of zafirlukast.
2002
Severe liver injury associated with zafirlukast.
2001-11-20
Molecular cloning and functional characterization of murine cysteinyl-leukotriene 1 (CysLT(1)) receptors.
2001-11-01
Chronic asthma.
2001-10-27
Severe liver injury.
2001-10-02
The effect of low-dose inhaled fluticasone propionate on exhaled nitric oxide in asthmatic patients and comparison with oral zafirlukast.
2001-10
Asthma treatment with inhaled corticosteroids versus antileukotrienes: what exhaled nitric oxide studies do and do not tell us.
2001-10
Acute hepatocellular injury associated with zafirlukast.
2001-10
Zafirlukast-related hepatitis: report of a further case.
2001-10
[Leukotriene modifiers].
2001-10
Leukotriene receptor antagonists in the treatment of allergic rhinitis.
2001-10
Effects of zafirlukast upon clinical, physiologic, and inflammatory responses to natural cat allergen exposure.
2001-09
[The relationship between eosinophils, activated T lymphocyte, leukotreine and the exercise-induced asthma].
2001-06
Comparison of the bronchodilating effect of salmeterol and zafirlukast in combination with that of their use as single treatments in asthma and chronic obstructive pulmonary disease.
2001
Addition of anti-leukotriene agents to inhaled corticosteroids for chronic asthma.
2001
Pharmacology of airway afferent nerve activity.
2001
Cost-efficacy analysis of fluticasone propionate versus zafirlukast in patients with persistent asthma.
2001
Patents

Patents

20010009918
5
JP2007513165A
55
JP2009149679A
1
JP2011528275A
456

Sample Use Guides

In Vivo Use Guide
Should be taken at least 1 hour before or 2 hours after meals. Adults and Children 12 years of age and older The recommended dose of ACCOLATE in adults and children 12 years and older is 20 mg twice daily. Pediatric Patients 5 through 11 years of age The recommended dose of ACCOLATE in children 5 through 11 years of age is 10 mg twice daily.
Route of Administration: Oral
In Vitro Use Guide
Zafirlukast significantly inhibited 10 uM LTD4-evoked 35SO4 output in a concentration-dependent fashion, with maximal inhibition of 78% at 10 uM zafirlukast, and IC50 value of 0.6 uM.
Substance Class Chemical
Created
by admin
on Wed Apr 02 09:29:27 GMT 2025
Edited
by admin
on Wed Apr 02 09:29:27 GMT 2025
Record UNII
XZ629S5L50
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
ZAFIRLUKAST
INN   JAN   MART.   MI   ORANGE BOOK   USAN   VANDF   WHO-DD  
USAN   INN  
Official Name English
ACCOLATE
Preferred Name English
ZAFIRLUKAST [MART.]
Common Name English
Cyclopentyl 3-[2-methoxy-4-[(O-tolylsulfonyl)carbamoyl]benzyl]-1-methylindole-5-carbamate
Common Name English
ZAFIRLUKAST [USAN]
Common Name English
ICI-204,219
Common Name English
ICI 204,219
Code English
ICI-204219
Code English
Zafirlukast [WHO-DD]
Common Name English
ZAFIRLUKAST [MI]
Common Name English
ZAFIRLUKAST [VANDF]
Common Name English
ZAFIRLUKAST [ORANGE BOOK]
Common Name English
zafirlukast [INN]
Common Name English
ZAFIRLUKAST [JAN]
Common Name English
CARBAMIC ACID, (3-((2-METHOXY-4-(((2-METHYLPHENYL)SULFONYL)AMINO)CARBONYL)PHENYL)METHYL)-1-METHYL-1H-INDOL-5-YL)-, CYCLOPENTYL ESTER
Common Name English
Classification Tree Code System Code
NDF-RT N0000175777
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
NDF-RT N0000000083
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
NCI_THESAURUS C29712
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
LIVERTOX NBK547915
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
WHO-ATC R03DC01
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
WHO-VATC QR03DC01
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
Code System Code Type Description
SMS_ID
100000091929
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
CAS
107753-78-6
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
USAN
GG-93
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
MERCK INDEX
m11576
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY Merck Index
INN
7244
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
FDA UNII
XZ629S5L50
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
EVMPD
SUB00128MIG
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
ChEMBL
CHEMBL603
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
NCI_THESAURUS
C47785
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
PUBCHEM
5717
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
IUPHAR
3322
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
DRUG BANK
DB00549
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
EPA CompTox
DTXSID5023746
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
LACTMED
Zafirlukast
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
WIKIPEDIA
ZAFIRLUKAST
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
DRUG CENTRAL
2855
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
MESH
C062735
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
RXCUI
114970
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY RxNorm
DAILYMED
XZ629S5L50
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
CHEBI
10100
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY
NDF-RT
N0000185504
Created by admin on Wed Apr 02 09:29:27 GMT 2025 , Edited by admin on Wed Apr 02 09:29:27 GMT 2025
PRIMARY Cytochrome P450 2C9 Inhibitors [MoA]
Related Record Type Details
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
CYSTEINYL LEUKOTRIENE RECEPTOR 1
TARGET -> INHIBITOR
CYTOCHROME P450 2C9
METABOLIC ENZYME -> SUBSTRATE
MAJOR
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INHIBITOR
in vitro studies utilizing human liver microsomes show that zafirlukast inhibits the cytochrome P450 CYP3A4 and CYP2C9 isoenzymes at concentrations close to the clinically achieved total plasma concentrations.
CYTOCHROME P450 2C9
METABOLIC ENZYME -> INHIBITOR
in vitro studies utilizing human liver microsomes show that zafirlukast inhibits the cytochrome P450 CYP3A4 and CYP2C9 isoenzymes at concentrations close to the clinically achieved total plasma concentrations
Related Record Type Details
Structure of 4-((5-(((CYCLOPENTYLOXY)CARBONYL)AMINO)-1-METHYL-1H-INDOL-3-YL)METHYL)-3-METHOXYBENZOIC ACID
IMPURITY -> PARENT
Structure of ZAFIRLUKAST P-TOLYL ISOMER
IMPURITY -> PARENT
Related Record Type Details
Structure of ZAFIRLUKAST
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Route of Elimination PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Cmax PHARMACOKINETIC Populations
PHARMACOKINETIC
Route of Elimination PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Cmax PHARMACOKINETIC Populations
PHARMACOKINETIC
Tmax PHARMACOKINETIC
Onset of Action PHARMACOKINETIC
NIH
NCATS
PRIVACY NOTICE
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966