Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C31H33N3O6S |
| Molecular Weight | 575.6775 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cc1ccccc1S(=O)(=O)N=C(c2ccc(Cc3cn(C)c4ccc(cc34)N=C(O)OC5CCCC5)c(c2)OC)O
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)
| Molecular Formula | C31H33N3O6S |
| Molecular Weight | 575.6775 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment:: Description was created based on several sources, including http://www.accessdata.fda.gov/drugsatfda_docs/label/2009/020547s027lbl.pdf
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.
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
| 1.1 nM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | ACCOLATE Approved UseACCOLATE is indicated for the prophylaxis and chronic treatment of asthma in adults and children 5 years of age and older. Launch Date8.436096E11 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
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
| Dose | Population | Adverse 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
Other AEs: Pharyngitis, Headache... Other AEs: Pharyngitis (24.7%) Sources: 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%) |
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: |
unhealthy, 37 n = 67 Health Status: unhealthy Condition: asthma, moderate Age Group: 37 Sex: M+F Population Size: 67 Sources: |
Other AEs: Headache, Gastritis... Other AEs: Headache (7%) Sources: Gastritis (1%) Pharyngitis (20%) Rhinitis (7%) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 12-76 n = 514 Health Status: unhealthy Condition: asthma, mild-to-moderate Age Group: 12-76 Sex: M+F Population Size: 514 Sources: |
| 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: |
unhealthy, 37 n = 67 Health Status: unhealthy Condition: asthma, moderate Age Group: 37 Sex: M+F Population Size: 67 Sources: |
| 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: |
unhealthy, 37 n = 67 Health Status: unhealthy Condition: asthma, moderate Age Group: 37 Sex: M+F Population Size: 67 Sources: |
| 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: |
unhealthy, 37 n = 67 Health Status: unhealthy Condition: asthma, moderate Age Group: 37 Sex: M+F Population Size: 67 Sources: |
| 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: |
unhealthy, 37 n = 67 Health Status: unhealthy Condition: asthma, moderate Age Group: 37 Sex: M+F Population Size: 67 Sources: |
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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 |
|
| Pharmacology of airway afferent nerve activity. | 2001 |
|
| Comparative efficacy of inhaled corticosteroids and antileukotriene drugs in asthma. | 2001 |
|
| The role of leukotriene receptor antagonists in the treatment of chronic asthma in childhood. | 2001 |
|
| Pathophysiology of the cysteinyl leukotrienes and effects of leukotriene receptor antagonists in asthma. | 2001 |
|
| [The relationship between eosinophils, activated T lymphocyte, leukotreine and the exercise-induced asthma]. | 2001 Jun |
|
| Efficacy of antileukotriene agents in asthma management. | 2001 Jun |
|
| Discovery of leukotrienes and development of antileukotriene agents. | 2001 Jun |
|
| The role of antileukotrienes in the treatment of asthma. | 2001 Jun |
|
| Safety of antileukotriene agents in asthma management. | 2001 Jun |
|
| Role of cysteinyl leukotrienes in nociceptive and inflammatory conditions in experimental animals. | 2001 Jun 29 |
|
| Role of Zafirlukast on skin prick test. | 2001 Mar-Apr |
|
| Use of changes in symptoms to predict changes in lung function in assessing the response to asthma therapy. | 2001 May |
|
| Synergistic antiallergic activity of combined histamine H1- and cysteinyl leukotriene1-receptor blockade in human bronchus. | 2001 May 11 |
|
| Severe liver injury associated with zafirlukast. | 2001 Nov 20 |
|
| The effect of low-dose inhaled fluticasone propionate on exhaled nitric oxide in asthmatic patients and comparison with oral zafirlukast. | 2001 Oct |
|
| Asthma treatment with inhaled corticosteroids versus antileukotrienes: what exhaled nitric oxide studies do and do not tell us. | 2001 Oct |
|
| Acute hepatocellular injury associated with zafirlukast. | 2001 Oct |
|
| Zafirlukast-related hepatitis: report of a further case. | 2001 Oct |
|
| [Leukotriene modifiers]. | 2001 Oct |
|
| Chronic asthma. | 2001 Oct 27 |
|
| Effects of zafirlukast upon clinical, physiologic, and inflammatory responses to natural cat allergen exposure. | 2001 Sep |
|
| Fulminant eosinophilic endomyocarditis in an asthmatic patient treated with pranlukast after corticosteroid withdrawal. | 2001 Sep |
|
| Leukotriene receptor antagonists in the treatment of asthma: an update. | 2002 |
|
| Loss of response to treatment with leukotriene receptor antagonists but not inhaled corticosteroids in patients over 50 years of age. | 2002 Apr |
|
| Where do leukotriene modifiers fit in asthma management? | 2002 Apr |
|
| [Zafirlukast (Accolate): a review of its pharmacological and clinical profile]. | 2002 Apr |
|
| Pharmacogenetics of asthma. | 2002 Apr 1 |
|
| Pharmacological differences among CysLT(1) receptor antagonists with respect to LTC(4) and LTD(4) in human lung parenchyma. | 2002 Apr 15 |
|
| [Reflections on antileukotrienes]. | 2002 Apr 15 |
|
| Vasculitis induced by zafirlukast therapy. | 2002 Aug |
|
| Chemoprevention by lipoxygenase and leukotriene pathway inhibitors of vinyl carbamate-induced lung tumors in mice. | 2002 Aug 1 |
|
| Participation of chemical mediators other than histamine in nasal allergy signs: a study using mice lacking histamine H(1) receptors. | 2002 Aug 9 |
|
| Economic impact of asthma therapy with fluticasone propionate, montelukast, or zafirlukast in a managed care population. | 2002 Feb |
|
| Receptor preferences of cysteinyl-leukotrienes in the guinea pig lung parenchyma. | 2002 Feb 1 |
|
| [Churg-Strauss syndrome after treatment with Singulair (montelukast)]. | 2002 Feb 20 |
|
| [Study on relationship between leukotrienes and exercise-induced asthma]. | 2002 Jan 10 |
|
| 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 Jul |
|
| Efficacy and safety of low-dose fluticasone propionate compared with zafirlukast in patients with persistent asthma. | 2002 Jul |
|
| Churg-Strauss syndrome in a case of asthma. | 2002 Jul |
|
| Antitussive effect of the leukotriene receptor antagonist zafirlukast in subjects with cough-variant asthma. | 2002 Jun |
|
| Pulmonary function changes and immunomodulation of cytokine expression by zafirlukast after sensitization and allergen challenge in brown Norway rats. | 2002 Jun |
|
| Novel phthalimide derivatives, designed as leukotriene D(4) receptor antagonists. | 2002 Jun 3 |
|
| [Zafirlukast in treatment of nasal polyps in patients with aspirin intolerant bronchial asthma--preliminary report]. | 2002 Mar |
|
| Leukotriene modifiers: novel therapeutic opportunities in asthma. | 2002 Mar |
|
| Prevalence of serious eosinophilia and incidence of Churg-Strauss syndrome in a cohort of asthma patients. | 2002 Mar |
|
| Inhaled fluticasone and zafirlukast in persistent asthma. | 2002 Mar |
|
| [Aspirin induced asthma, urinary leukotriene E4 and zafirlukast]. | 2002 Mar-Apr |
|
| Influence of zafirlukast and loratadine on exercise-induced bronchoconstriction. | 2002 May |
|
| Exercise-induced asthma: is there still a case for histamine? | 2002 May |
Sample Use Guides
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
| Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Jun 25 23:37:48 UTC 2021
by
admin
on
Fri Jun 25 23:37:48 UTC 2021
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| Record UNII |
XZ629S5L50
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| Record Status |
Validated (UNII)
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| Record Version |
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NDF-RT |
N0000175777
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NDF-RT |
N0000000083
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NCI_THESAURUS |
C29712
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LIVERTOX |
1043
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WHO-ATC |
R03DC01
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WHO-VATC |
QR03DC01
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107753-78-6
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M11576
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7244
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XZ629S5L50
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SUB00128MIG
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CHEMBL603
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C47785
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5717
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DB00549
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107753-78-6
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Zafirlukast
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ZAFIRLUKAST
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2855
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C062735
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114970
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N0000185504
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PRIMARY | Cytochrome P450 2C9 Inhibitors [MoA] |
| Related Record | Type | Details | ||
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BINDER->LIGAND |
BINDING
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TARGET -> INHIBITOR | |||
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METABOLIC ENZYME -> SUBSTRATE |
MAJOR
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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.
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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
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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| Route of Elimination | PHARMACOKINETIC |
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| Volume of Distribution | PHARMACOKINETIC |
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| Cmax | PHARMACOKINETIC |
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| Route of Elimination | PHARMACOKINETIC |
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| Volume of Distribution | PHARMACOKINETIC |
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| Biological Half-life | PHARMACOKINETIC |
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| Cmax | PHARMACOKINETIC |
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Populations PHARMACOKINETIC |
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| Tmax | PHARMACOKINETIC |
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| Onset of Action | PHARMACOKINETIC |
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