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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:: 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

TargetsConditions

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

887932800000
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

887932800000
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

887932800000
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

887932800000
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
Health Status: healthy
Age Group: 21-40 years
Sex: M
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)
Health Status: unhealthy
Age Group: 29.8 years (range: 15.0–56.0 years)
Sex: M+F
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
Health Status: unhealthy
Age Group: 3 years
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)
Health Status: unhealthy
Age Group: 34 years (range: 18-54 years)
Sex: M+F
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
Health Status: unhealthy
Age Group: 37 years
Sex: F
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)
Health Status: unhealthy
Age Group: 39.1 years (range: 16.0–63.0 years)
Sex: M+F
Sources:
135 mg single, oral
Overdose
Dose: 135 mg
Route: oral
Route: single
Dose: 135 mg
Sources:
unhealthy, 5 years
Health Status: unhealthy
Age Group: 5 years
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)
Health Status: unhealthy
Age Group: 29.8 years (range: 15.0–56.0 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 34 years (range: 18-54 years)
Sex: M+F
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)
Health Status: unhealthy
Age Group: 34 years (range: 18-54 years)
Sex: M+F
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
Health Status: unhealthy
Age Group: 37 years
Sex: F
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
Health Status: unhealthy
Age Group: 37 years
Sex: F
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
Health Status: unhealthy
Age Group: 37 years
Sex: F
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
Pharmacology of leukotriene receptor antagonists
1998 Jun
Inhibition of 5-lipoxygenase diminishes neurally evoked tachykinergic contraction of guinea pig isolated airway.
1998 May
Montelukast added to inhaled beclomethasone in treatment of asthma. Montelukast/Beclomethasone Additivity Group.
1999 Dec
Pulmonary eosinophilia associated with montelukast.
1999 Jun
Characterization of the human cysteinyl leukotriene CysLT1 receptor.
1999 Jun 24
Oral montelukast, inhaled beclomethasone, and placebo for chronic asthma. A randomized, controlled trial. Montelukast/Beclomethasone Study Group.
1999 Mar 16
Effect of multiple doses of montelukast, a CysLT1 receptor antagonist, on digoxin pharmacokinetics in healthy volunteers.
1999 Sep
Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor.
1999 Sep
[A study on the heterogeneous apoptosis of lymphocytes, eosinophils, and neutrophils from peripheral blood of asthmatic patients].
2003 Oct
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
Differential effect of zileuton, a 5-lipoxygenase inhibitor, against nociceptive paradigms in mice and rats.
2005 Jul
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
Prevalence of alpha-1 antitrypsin deficiency in poorly controlled asthma--results from the ALA-ACRC low-dose theophylline trial.
2007 Oct
The recently identified P2Y-like receptor GPR17 is a sensor of brain damage and a new target for brain repair.
2008
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
Antileukotriene drugs in the treatment of asthma.
2010 Mar
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
2011 Dec 8
Association of the variants in AGT gene with modified drug response in Korean aspirin-intolerant asthma patients.
2011 Oct
Identification of old drugs as potential inhibitors of HIV-1 integrase - human LEDGF/p75 interaction via molecular docking.
2012 Dec
Systems pharmacological analysis of drugs inducing stevens-johnson syndrome and toxic epidermal necrolysis.
2015 May 18
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