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Details

Stereochemistry ABSOLUTE
Molecular Formula C35H36ClNO3S
Molecular Weight 586.1856
Optical Activity UNSPECIFIED
Defined Stereocenters 1 / 1
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of MONTELUKAST

SMILES

CC(C)(c1ccccc1CC[C@]([H])(c2cccc(/C(/[H])=C(\[H])/c3ccc4ccc(cc4n3)Cl)c2)SCC5(CC5)CC(=O)O)O

InChI

InChIKey=UCHDWCPVSPXUMX-TZIWLTJVSA-N
InChI=1S/C35H36ClNO3S/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39)/b15-10+/t32-/m1/s1

HIDE SMILES / InChI

Description
Curator's Comment:: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/mesh/67093875

Montelukast (SINGULAIR®) is a selective and orally active leukotriene D4 (LTD4) receptor antagonist that inhibits the cysteinyl leukotriene CysLT1 receptor. It is indicated for the prophylaxis and chronic treatment of asthma, for prevention of exercise-induced bronchoconstriction, and for the relief of symptoms of seasonal allergic rhinitis. LTD4 is a product of arachidonic acid metabolism and is released from various cells, including mast cells and eosinophils. This eicosanoid binds to CysLT1 receptor found in the human airway (including airway smooth muscle cells and airway macrophages) and on other pro-inflammatory cells (including eosinophils and certain myeloid stem cells). Cysteinyl leukotriene receptors (CysLTs) have been correlated with the pathophysiology of asthma and allergic rhinitis. In asthma, leukotriene-mediated effects include airway edema, smooth muscle contraction, and altered cellular activity associated with the inflammatory process. In allergic rhinitis, CysLTs are released from the nasal mucosa after allergen exposure during both earlyand late-phase reactions and are associated with symptoms of allergic rhinitis. Montelukast (SINGULAIR®) binds with high affinity and selectivity to the CysLT1 (in preference to other pharmacologically important airway receptors, such as the prostanoid, cholinergic, or beta-adrenergic receptor). It inhibits physiologic actions of LTD4 at the CysLT1 receptor without any agonist activity.

CNS Activity

Curator's Comment:: Neuropsychiatric events have been reported with SINGULAIR®.

Originator

Curator's Comment:: # Merck & Co., Inc.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SINGULAIR

Approved Use

Montelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older.

Launch Date

8.8793278E11
Preventing
SINGULAIR

Approved Use

Montelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older.

Launch Date

8.8793278E11
Primary
SINGULAIR

Approved Use

Montelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older.

Launch Date

8.8793278E11
Primary
SINGULAIR

Approved Use

Montelukast sodium tablets are a leukotriene receptor antagonist indicated for: •Prophylaxis and chronic treatment of asthma in patients 2 years of age and older (1.1). •Acute prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older (1.2). •Relief of symptoms of allergic rhinitis (AR): seasonal allergic rhinitis (SAR) in patients 2 years of age and older, and perennial allergic rhinitis (PAR) in patients 2 years of age and older (1.3). 1.1 Asthma Montelukast sodium is indicated for the prophylaxis and chronic treatment of asthma in adults and pediatric patients 2 years of age and older. 1.2 Exercise-Induced Bronchoconstriction (EIB) Montelukast sodium is indicated for prevention of exercise-induced bronchoconstriction (EIB) in patients 15 years of age and older. Pediatric use information for patients ages 6 to 14 years of age for acute prevention of exercise-induced bronchoconstriction (EIB) is approved for Merck Sharp & Dohme Corp’s montelukast tablet products. However, due to Merck Sharp & Dohme Corp’s marketing exclusivity rights, this drug product is not labeled with that pediatric information. 1.3 Allergic Rhinitis Montelukast sodium is indicated for the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 2 years of age and older.

Launch Date

8.8793278E11
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
541.5 ng/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MONTELUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
602.8 ng/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
MONTELUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
13.8 ng/mL
1 mg single, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
18.5 ng/mL
1 mg single, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
224 ng/mL
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
23.4 ng/mL
1 mg 1 times / day multiple, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
54.3 ng/mL
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
184 ng/mL
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
225 ng/mL
10 mg 1 times / day multiple, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
233 ng/mL
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
242 ng/mL
10 mg 1 times / day multiple, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
44.3 ng/mL
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
5.1 ng/mL
0.3 mg single, respiratory
dose: 0.3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
5.24 ng/mL
0.3 mg single, respiratory
dose: 0.3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
60 ng/mL
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
64.8 ng/mL
3 mg 1 times / day multiple, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
76 ng/mL
3 mg 1 times / day multiple, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
3540 ng × h/mL
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MONTELUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3978 ng × h/mL
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
MONTELUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
132 ng*h/mL
1 mg single, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1500 ng*h/mL
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
155 ng*h/mL
1 mg single, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1576 ng*h/mL
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1600 ng*h/mL
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1850 ng*h/mL
10 mg 1 times / day multiple, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
1880 ng*h/mL
10 mg 1 times / day multiple, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
214 ng*h/mL
1 mg 1 times / day multiple, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
357 ng*h/mL
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
403 ng*h/mL
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
491 ng*h/mL
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
526 ng*h/mL
3 mg 1 times / day multiple, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
576 ng*h/mL
3 mg 1 times / day multiple, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
5.3 h
10 mg single, oral
dose: 10 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
MONTELUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.6 h
10 mg 1 times / day steady-state, oral
dose: 10 mg
route of administration: Oral
experiment type: STEADY-STATE
co-administered:
MONTELUKAST plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5.7 h
1 mg single, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
5.7 h
10 mg single, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
8.2 h
1 mg 1 times / day multiple, respiratory
dose: 1 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
6.9 h
3 mg single, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: single
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
7.4 h
10 mg 1 times / day multiple, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
7.7 h
10 mg 1 times / day multiple, respiratory
dose: 10 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
7.6 h
3 mg 1 times / day multiple, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
8.1 h
3 mg 1 times / day multiple, respiratory
dose: 3 mg
route of administration: respiratory
experiment type: multiple
co-administered:
MONTELUKAST plasma
Homo sapiens
population: unhealthy
age:
sex:
food status:
Doses

Doses

DosePopulationAdverse events​
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
healthy, 21-40 years
n = 18
Health Status: healthy
Age Group: 21-40 years
Sex: M
Population Size: 18
Sources:
7 mg single, intravenous
Dose: 7 mg
Route: intravenous
Route: single
Dose: 7 mg
Sources:
unhealthy, 29.8 years (range: 15.0–56.0 years)
n = 50
Health Status: unhealthy
Condition: asthma
Age Group: 29.8 years (range: 15.0–56.0 years)
Sex: M+F
Population Size: 50
Sources:
Other AEs: Headache...
Other AEs:
Headache (2%)
Sources:
80 mg single, oral
Overdose
Dose: 80 mg
Route: oral
Route: single
Dose: 80 mg
Sources:
unhealthy, 3 years
n = 1
Health Status: unhealthy
Condition: asthma
Age Group: 3 years
Population Size: 1
Sources:
200 mg 3 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Sources:
unhealthy, 34 years (range: 18-54 years)
n = 28
Health Status: unhealthy
Condition: chronic asthma
Age Group: 34 years (range: 18-54 years)
Sex: M+F
Population Size: 28
Sources:
Other AEs: Bilirubin total increased, Alanine aminotransferase increase...
Other AEs:
Bilirubin total increased (mild, 1 patient)
Alanine aminotransferase increase (mild, 1 patient)
Sources:
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 37 years
n = 1
Health Status: unhealthy
Age Group: 37 years
Sex: F
Population Size: 1
Sources:
Disc. AE: Jaundice, Pruritus...
AEs leading to
discontinuation/dose reduction:
Jaundice (1 patient)
Pruritus (severe, 1 patient)
Nausea (1 patient)
Sources:
1000 ug single, respiratory
Dose: 1000 ug
Route: respiratory
Route: single
Dose: 1000 ug
Sources:
unhealthy, 39.1 years (range: 16.0–63.0 years)
n = 36
Health Status: unhealthy
Condition: chronic asthma
Age Group: 39.1 years (range: 16.0–63.0 years)
Sex: M+F
Population Size: 36
Sources:
135 mg single, oral
Overdose
Dose: 135 mg
Route: oral
Route: single
Dose: 135 mg
Sources:
unhealthy, 5 years
n = 1
Health Status: unhealthy
Condition: asthma
Age Group: 5 years
Population Size: 1
Sources:
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, >15 years
Other AEs: Psychiatric disorder NOS...
AEs

AEs

AESignificanceDosePopulation
Headache 2%
7 mg single, intravenous
Dose: 7 mg
Route: intravenous
Route: single
Dose: 7 mg
Sources:
unhealthy, 29.8 years (range: 15.0–56.0 years)
n = 50
Health Status: unhealthy
Condition: asthma
Age Group: 29.8 years (range: 15.0–56.0 years)
Sex: M+F
Population Size: 50
Sources:
Alanine aminotransferase increase mild, 1 patient
200 mg 3 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Sources:
unhealthy, 34 years (range: 18-54 years)
n = 28
Health Status: unhealthy
Condition: chronic asthma
Age Group: 34 years (range: 18-54 years)
Sex: M+F
Population Size: 28
Sources:
Bilirubin total increased mild, 1 patient
200 mg 3 times / day multiple, oral
Highest studied dose
Dose: 200 mg, 3 times / day
Route: oral
Route: multiple
Dose: 200 mg, 3 times / day
Sources:
unhealthy, 34 years (range: 18-54 years)
n = 28
Health Status: unhealthy
Condition: chronic asthma
Age Group: 34 years (range: 18-54 years)
Sex: M+F
Population Size: 28
Sources:
Jaundice 1 patient
Disc. AE
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 37 years
n = 1
Health Status: unhealthy
Age Group: 37 years
Sex: F
Population Size: 1
Sources:
Nausea 1 patient
Disc. AE
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 37 years
n = 1
Health Status: unhealthy
Age Group: 37 years
Sex: F
Population Size: 1
Sources:
Pruritus severe, 1 patient
Disc. AE
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, 37 years
n = 1
Health Status: unhealthy
Age Group: 37 years
Sex: F
Population Size: 1
Sources:
Psychiatric disorder NOS serious
10 mg 1 times / day steady, oral
Recommended
Dose: 10 mg, 1 times / day
Route: oral
Route: steady
Dose: 10 mg, 1 times / day
Sources:
unhealthy, >15 years
PubMed

PubMed

TitleDatePubMed
Leukotriene receptor antagonists: efficacy and safety in children with asthma.
2000 Aug
A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization.
2000 Dec 29
Recurrent panniculitis in a man with asthma receiving treatment with leukotriene-modifying agents.
2000 Jun
The role of LTRAs in the management of persistent asthma.
2000 Sep 15
The protective effects of leukotriene modifiers in aspirin-induced asthma.
2000 Sep 15
LTRA inhibition of exercise-induced bronchoconstriction.
2000 Sep 15
Dose selection and dosing interval determination for LTRA use in asthma.
2000 Sep 15
Clinical safety and tolerability of montelukast, a leukotriene receptor antagonist, in controlled clinical trials in patients aged > or = 6 years.
2001 Jan
Long-term asthma control with oral montelukast and inhaled beclomethasone for adults and children 6 years and older.
2001 Jun
Inverse agonist activity of selected ligands of the cysteinyl-leukotriene receptor 1.
2004 Apr
Montelukast-induced hepatitis.
2004 Apr 6
Role of leukotriene inhibitors in the postoperative management of nasal polyps.
2005
Prediction of genotoxicity of chemical compounds by statistical learning methods.
2005 Jun
Influence of leukotriene pathway polymorphisms on response to montelukast in asthma.
2006 Feb 15
Montelukast and zafirlukast do not affect the pharmacokinetics of the CYP2C8 substrate pioglitazone.
2006 Jul
Leukotriene D4 increases the excitability of capsaicin-sensitive nasal sensory nerves to electrical and chemical stimuli.
2008 Jul
Cysteinyl leucotriene receptor type 1 mediates contraction in human and guinea-pig oesophagus.
2008 Oct
Montelukast-associated Churg-Strauss vasculitis: another associated report.
2009 Apr
Discovery of novel tricyclic full agonists for the G-protein-coupled niacin receptor 109A with minimized flushing in rats.
2009 Apr 23
Functional expression, inhibition and induction of CYP enzymes in HepaRG cells.
2009 Jun
Leukotriene pathways and in vitro adenotonsillar cell proliferation in children with obstructive sleep apnea.
2009 May
Enhanced fracture repair by leukotriene antagonism is characterized by increased chondrocyte proliferation and early bone formation: a novel role of the cysteinyl LT-1 receptor.
2009 Oct
Association of the variants in AGT gene with modified drug response in Korean aspirin-intolerant asthma patients.
2011 Oct
Patents

Sample Use Guides

SINGULAIR® should be taken once daily in the evening. The following dose is recommended for adults and adolescents 15 years of age and older: one 10-mg tablet.
Route of Administration: Oral
In Vitro Use Guide
Montelukast is a potent and selective inhibitor of [3H]leukotriene D4 specific binding in guinea pig lung (Ki 0.18 +/- 0.03 nM), sheep lung (Ki 4 nM), and dimethylsulfoxide-differentiated U937 cell plasma membrane preparations (Ki 0.52 +/- 0.23 nM), but it was essentially inactive versus [3H]leukotriene C4 specific binding in dimethylsulfoxide-differentiated U937 cell membranes (IC50 10 microM) and [3H]leukotriene B4 specific binding in THP-1 cell membranes (IC50 40 microM). Montelukast also inhibited specific binding of [3H]leukotriene D4 to guinea pig lung in the presence of human serum albumin, human plasma, and squirrel monkey plasma with Ki values of 0.21 +/- 0.08, 0.19 +/- 0.02, and 0.26 +/- 0.02 nM, respectively.
Name Type Language
MONTELUKAST
HSDB   INN   MI   VANDF   WHO-DD  
INN  
Official Name English
MONTELUKAST [MI]
Common Name English
MONTELUKAST [INN]
Common Name English
MONTELUKAST [VANDF]
Common Name English
BRONDILAT
Brand Name English
(1-((((1R)-1-(3-((E)-2-(7-CHLOROQUINOLIN-2-YL)VINYL)PHENYL)-3-(2-(1-HYDROXY-1-METHYLETHYL)PHENYL)PROPYL)THIO)METHYL)CYCLOPROPYL)ACETIC ACID
Systematic Name English
MONTELUKAST [WHO-DD]
Common Name English
CYCLOPROPANEACETIC ACID, 1-((((1R)-1-(3-((E)-2-(7-CHLORO-2-QUINOLINYL)ETHENYL)PHENYL)-3-(2-(1-HYDROXY-1-METHYLETHYL)PHENYL)PROPYL)THIO)METHYL)-
Common Name English
MONTELUKAST [HSDB]
Common Name English
Classification Tree Code System Code
NDF-RT N0000000083
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
LIVERTOX 652
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
WHO-ATC R03DC03
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
WHO-VATC QR03DC03
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
WHO-ATC R03DC53
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
NDF-RT N0000175777
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
NCI_THESAURUS C29712
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
Code System Code Type Description
HSDB
7582
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
EVMPD
SUB09054MIG
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
CAS
158966-92-8
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
FDA UNII
MHM278SD3E
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
IUPHAR
3340
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
EPA CompTox
158966-92-8
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
ChEMBL
CHEMBL787
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
DRUG CENTRAL
1836
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
INN
7388
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
LACTMED
Montelukast
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
NCI_THESAURUS
C66189
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
MESH
C093875
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
MERCK INDEX
M7616
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY Merck Index
WIKIPEDIA
MONTELUKAST
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
PUBCHEM
5281040
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY
RXCUI
88249
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY RxNorm
DRUG BANK
DB00471
Created by admin on Sat Jun 26 02:38:02 UTC 2021 , Edited by admin on Sat Jun 26 02:38:02 UTC 2021
PRIMARY