Drug/Small Molecule:
montelukast

PharmGKB contains no dosing guidelines for this drug/small molecule. To report known genotype-based dosing guidelines, or if you are interested in developing guidelines, click here.

PharmGKB contains no drug labels with pharmacogenomic information for this drug/small molecule. To report a drug label with PGx, click here.

PharmGKB contains no Clinical Variants that meet the highest level of criteria.

To see more Clinical Variants with lower levels of criteria, click the button at the bottom of the page.

Disclaimer: The PharmGKB's clinical annotations reflect expert consensus based on clinical evidence and peer-reviewed literature available at the time they are written and are intended only to assist clinicians in decision-making and to identify questions for further research. New evidence may have emerged since the time an annotation was submitted to the PharmGKB. The annotations are limited in scope and are not applicable to interventions or diseases that are not specifically identified.

The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?

The table below contains information about pharmacogenomic variants on PharmGKB. Please follow the link in the "Variant" column for more information about a particular variant. Each link in the "Variant" column leads to the corresponding PharmGKB Variant Page. The Variant Page contains summary data, including PharmGKB manually curated information about variant-drug pairs based on individual PubMed publications. The PMIDs for these PubMed publications can be found on the Variant Page.

The tags in the first column of the table indicate what type of information can be found on the corresponding Variant Page.

Links in the "Gene" column lead to PharmGKB Gene Pages.

Gene ? Variant?
(138)
Alternate Names / Tag SNPs ? Drugs ? Alleles ?
(+ chr strand)
Function ? Amino Acid?
Translation
VIP No Clinical Annotations available No Variant Annotations available
chr10:45869552
No VIP available CA VA
rs119774 16026833C>T, 16086833C>T, 48400C>T, 49-14840C>T, MRP1, rs119774
C > T
Intronic
No VIP available CA VA
rs12422149 20189372G>A, 26546G>A, 503G>A, 74883577G>A, 869G>A, 935G>A, Arg168Gln, Arg290Gln, Arg312Gln, SLCO2B1:Arg312Gln, SLCO2B1:G935A
G > A
Missense
Arg168Gln
No VIP available CA VA
rs2115819 246472A>G, 3546154A>G, 36461A>G, 432-6550A>G, 45901089A>G, rs2115819
A > G
Intronic
No VIP available No Clinical Annotations available VA
rs2306168 1025C>T, 1391C>T, 1457C>T, 20213377C>T, 50551C>T, 74907582C>T, SLCO2B1:C1457T, SLCO2B1:Ser486Phe, Ser342Phe, Ser464Phe, Ser486Phe
C > T
Missense
Ser342Phe
No VIP available CA VA
rs2660845 -1400C>T, 58581859G>A, 96438553G>A, LTA4H, rs2660845
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs2712807 -546G>A, 20167676G>A, 4850G>A, 74861881G>A
G > A
5' Flanking
No VIP available No Clinical Annotations available VA
rs35199625 169G>A, 20186165G>A, 23339G>A, 535G>A, 601G>A, 74880370G>A, Val179Met, Val201Met, Val57Met
G > A
Missense
Val57Met
No VIP available CA VA
rs730012 -444A>C, 179220638A>C, 24031911A>C, 4653A>C, LTC4S, LTC4S: A-444C, LTC4S:-444C, rs730012
A > C
5' Flanking
Alleles, Functions, and Amino Acid Translations are all sourced from dbSNP 138
2D structure from PubChem
provided by PubChem

Overview

Generic Names
Trade Names
  • Montair
  • Singulair
  • Singular
Brand Mixture Names

PharmGKB Accession Id:
PA450546

Description

Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. It is usually administered orally. Montelukast blocks the action of leukotriene D4 on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene, and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific locus of operation, it does not interact with other allergy medications such as theophylline. Montelukast is marketed in United States and many other countries by Merck & Co. with the brand name Singulair®. It is available as oral tablets, chewable tablets, and oral granules. In India and other countries, it is also marketed under the brand name Montair R , produced by Indian company Cipla.

Source: Drug Bank

Indication

For the treatment of asthma

Source: Drug Bank

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Montelukast selectively antagonizes leukotriene D 4 (LTD 4) at the cysteinyl leukotriene receptor, CysLT 1, in the human airway. Montelukast inhibits the actions of LTD 4 at the CysLT 1 receptor, preventing airway edema, smooth muscle contraction, and enhanced secretion of thick, viscous mucus.

Source: Drug Bank

Pharmacology

Montelukast, like zafirlukast, is a leukotriene receptor antagonist used as an alternative to anti-inflammatory medications in the management and chronic treatment of asthma and exercise-induced bronchospasm (EIB). Unlike zafirlukast, montelukast does not inhibit CYP2C9 or CYP3A4 and is, therefore, not expected to affect the hepatic clearance of drugs metabolized by these enzymes.

Source: Drug Bank

Food Interaction

Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

99% (to plasma proteins)

Source: Drug Bank

Absorption

Rapidly absorbed following oral administration (bioavailability is 64%)

Source: Drug Bank

Half-Life

2.7-5.5 hours

Source: Drug Bank

Toxicity

Side effects include headache, abdominal or stomach pain, cough, dental pain, dizziness, fever, heartburn, skin rash, stuffy nose, weakness or unusual tiredness.

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

Source: Drug Bank

Volume of Distribution

  • 8 to 11 L

Source: Drug Bank

Chemical Properties

Chemical Formula

C35H36ClNO3S

Source: Drug Bank

Isomeric SMILES

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

Source: OpenEye

Canonical SMILES

OC(=O)CC1(CC1)CS[C@H](CCC1=CC=CC=C1C(O)(C)C)C1=CC=CC(\C=C\C2=NC3=C(C=CC(Cl)=C3)C=C2)=C1

Source: Drug Bank

Average Molecular Weight

586.183

Source: Drug Bank

Monoisotopic Molecular Weight

585.21044242

Source: Drug Bank

PharmGKB Curated Pathways

Pathways created internally by PharmGKB based primarily on literature evidence.

External Pathways

Links to non-PharmGKB pathways.

PharmGKB contains no links to external pathways for this drug. To report a pathway, click here.

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ALOX5 (source: Drug Bank)
CYSLTR1 (source: Drug Bank)

Drug Interactions

Drug Description
montelukast Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Montelukast. Consider alternate therapy or monitor for changes in Montelukast therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)
montelukast Tolbutamide, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Montelukast. Consider alternate therapy or monitor for changes in Montelukast therapeutic and adverse effects if Tolbutamide is initiated, discontinued or dose changed. (source: Drug Bank)

Curated Information ?

EvidenceDisease
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Asthma

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to montelukast: 16

No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Effects of polymorphisms of the SLCO2B1 transporter gene on the pharmacokinetics of montelukast in humans. Journal of clinical pharmacology. 2013. Kim Kyoung-Ah, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Tailored second line therapy in asthmatic children with the arginine-16 genotype. Clinical science (London, England : 1979). 2012. Lipworth Brian J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Integrative systems biology approaches in asthma pharmacogenomics. Pharmacogenomics. 2012. Dahlin Amber, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Gemfibrozil markedly increases the plasma concentrations of montelukast: a previously unrecognized role for CYP2C8 in the metabolism of montelukast. Clinical pharmacology and therapeutics. 2010. Karonen T, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Genetics and pharmacogenetics of the leukotriene pathway. The Journal of allergy and clinical immunology. 2009. Tantisira Kelan G, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Leukotriene pathway genetics and pharmacogenetics in allergy. Allergy. 2009. Duroudier N P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
5-lipoxygenase pharmacogenetics in asthma: overlap with Cys-leukotriene receptor antagonist loci. Pharmacogenetics and genomics. 2009. Tantisira Kelan G, et al. PubMed
No Dosing Guideline available No Drug Label available CA VA No VIP available No VIP available
Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenetics and genomics. 2009. Mougey Edward B, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Asthma pharmacogenetic study using finite mixture models to handle drug-response heterogeneity. Pharmacogenomics. 2009. York Timothy P, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Pharmacogenetics of asthma. Current opinion in pulmonary medicine. 2009. Lima John J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation. Analytical and bioanalytical chemistry. 2008. Zanger Ulrich M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Association of IL-13 polymorphisms with leukotriene receptor antagonist drug responsiveness in Korean children with exercise-induced bronchoconstriction. Pharmacogenetics and genomics. 2008. Kang Mi-Jin, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
CysLTR1 promoter polymorphism and requirement for leukotriene receptor antagonist in aspirin-intolerant asthma patients. Pharmacogenomics. 2007. Kim Seung-Hyun, et al. PubMed
Influence of leukotriene pathway polymorphisms on response to montelukast in asthma. American journal of respiratory and critical care medicine. 2006. Lima John J, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Telithromycin, but not montelukast, increases the plasma concentrations and effects of the cytochrome P450 3A4 and 2C8 substrate repaglinide. Clinical pharmacology and therapeutics. 2006. Kajosaari Lauri I, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0006-0275-82
DrugBank:
DB00471
ChEBI:
6992
KEGG Compound:
C07482
PubChem Compound:
5281040
PubChem Substance:
46505585
9685
Drugs Product Database (DPD):
2243602
ChemSpider:
4444507
Therapeutic Targets Database:
DAP000309
FDA Drug Label at DailyMed:
8c166755-7711-4df9-d689-8836a1a70885

Clinical Trials

These are trials that mention montelukast and are related to either pharmacogenetics or pharmacogenomics.

Common Searches

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.