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Montelukast (drug)

Firestone Institute for Respiratory Health · FDA-approved active Small molecule

Montelukast blocks cysteinyl leukotriene receptors (CysLT1) on airway and immune cells, preventing leukotriene-mediated inflammation and bronchoconstriction.

Montelukast blocks cysteinyl leukotriene receptors (CysLT1) on airway and immune cells, preventing leukotriene-mediated inflammation and bronchoconstriction. Used for Asthma (chronic maintenance and acute treatment), Allergic rhinitis, Exercise-induced bronchoconstriction.

At a glance

Generic nameMontelukast (drug)
SponsorFirestone Institute for Respiratory Health
Drug classCysteinyl leukotriene receptor antagonist (LTRA)
TargetCysLT1 receptor
ModalitySmall molecule
Therapeutic areaRespiratory / Immunology
PhaseFDA-approved

Mechanism of action

Leukotrienes are inflammatory mediators released by mast cells and eosinophils that bind to CysLT1 receptors, causing airway smooth muscle contraction, mucus secretion, and eosinophil recruitment. By antagonizing these receptors, montelukast reduces airway inflammation and improves airflow in asthma and allergic rhinitis. This mechanism is particularly effective in aspirin-exacerbated respiratory disease and exercise-induced asthma.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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