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
SMILES
COC1=C(CC2=CN(C)C3=C2C=C(NC(=O)OC4CCCC4)C=C3)C=CC(=C1)C(=O)NS(=O)(=O)C5=C(C)C=CC=C5
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 | 575.675 |
| 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 |
|---|---|---|
| Zafirlukast in clinical practice: results of the Accolate Clinical Experience and Pharmacoepidemiology Trial (ACCEPT) in patients with asthma. | 1999 Jun |
|
| [Zafirlukast therapy of patients with mild-to-moderate bronchial asthma]. | 1999 Jun 13 |
|
| Characterization of the human cysteinyl leukotriene CysLT1 receptor. | 1999 Jun 24 |
|
| Discovery of CP-199,330 and CP-199,331: two potent and orally efficacious cysteinyl LT1 receptor antagonists devoid of liver toxicity. | 1999 Sep 20 |
|
| Lung function improvement in smokers suffering from COPD with zafirlukast, a CysLT(1)-receptor antagonist. | 2000 |
|
| Efficacy and duration of action of the antileukotriene zafirlukast on cold air-induced bronchoconstriction. | 2000 Apr |
|
| Efficacy and safety of Zafirlukast ('Accolate') in the management of patients with mild-to-moderate asthma. | 2000 Apr-Jun |
|
| Effects of adding a leukotriene antagonist or a long-acting beta(2)-agonist in asthmatic patients with the glycine-16 beta(2)-adrenoceptor genotype. | 2000 Aug 1 |
|
| Montelukast in the prophylaxis of migraine: a potential role for leukotriene modifiers. | 2000 Feb |
|
| Acute effects of antileukotrienes on sinonasal polyposis and sinusitis. | 2000 Jan |
|
| Effect of leukotriene receptor antagonist therapy on the risk of asthma exacerbations in patients with mild to moderate asthma: an integrated analysis of zafirlukast trials. | 2000 Jun |
|
| Characterization of the human cysteinyl leukotriene 2 receptor. | 2000 Sep 29 |
|
| 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 |
|
| 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 |
|
| Allergy and angiitis: two aspects of Churg-Strauss syndrome. | 2001 Feb |
|
| Asthma outcome changes associated with use of the leukotriene-receptor antagonist zafirlukast. | 2001 Feb |
|
| Fluticasone propionate compared with zafirlukast in controlling persistent asthma: a randomized double-blind, placebo-controlled trial. | 2001 Jul |
|
| Comparison of inhaled salmeterol and oral zafirlukast in asthmatic patients using concomitant inhaled corticosteroids. | 2001 Jul 5 |
|
| 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 |
|
| Efficacy of zafirlukast in the treatment of patients with bronchial asthma. | 2001 Mar |
|
| Use of changes in symptoms to predict changes in lung function in assessing the response to asthma therapy. | 2001 May |
|
| 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 |
|
| Acute hepatocellular injury associated with zafirlukast. | 2001 Oct |
|
| Severe liver injury. | 2001 Oct 2 |
|
| An open study to evaluate the safety and efficacy of zafirlukast ("Accolate") in patients with mild to moderate asthma in Ibadan, Nigeria. | 2001 Oct-Dec |
|
| 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 |
|
| 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 |
|
| [Reflections on antileukotrienes]. | 2002 Apr 15 |
|
| 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 |
|
| Churg-Strauss syndrome in a case of asthma. | 2002 Jul |
|
| 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 |
|
| Prevalence of serious eosinophilia and incidence of Churg-Strauss syndrome in a cohort of asthma patients. | 2002 Mar |
|
| Treatment of canine atopic dermatitis with zafirlukast, a leukotriene-receptor antagonist: a single-blinded, placebo-controlled study. | 2002 Mar |
|
| [Aspirin induced asthma, urinary leukotriene E4 and zafirlukast]. | 2002 Mar-Apr |
|
| Comparison of second controller medications in addition to inhaled corticosteroid in patients with moderate asthma. | 2002 May |
|
| 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
Thu Jul 06 23:04:26 UTC 2023
by
admin
on
Thu Jul 06 23:04:26 UTC 2023
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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 |
NBK547915
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WHO-ATC |
R03DC01
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WHO-VATC |
QR03DC01
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100000091929
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107753-78-6
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GG-93
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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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DTXSID5023746
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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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XZ629S5L50
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10100
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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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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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Populations 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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