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Singulair (montelukast)
Leukotriene receptor antagonist (LTRA) that blocks CysLT1 receptors, reducing bronchoconstriction, mucus production, and airway inflammation.
Montelukast (Singulair) is the most prescribed leukotriene receptor antagonist, developed by Merck and approved in 1998. Available generically. BLACK BOX WARNING (2020): risk of neuropsychiatric events — restricted to patients who cannot use alternative therapies.
At a glance
| Generic name | montelukast |
|---|---|
| Also known as | Singulair |
| Sponsor | Merck & Co. |
| Drug class | Leukotriene receptor antagonist (LTRA) |
| Target | Cytochrome P450 2C8, Adenosine receptor A3, Cysteinyl leukotriene receptor 2 |
| Modality | Small molecule |
| Therapeutic area | Neuroscience |
| Phase | FDA-approved |
| First approval | 1998-02-20 (United States) |
Mechanism of action
Montelukast blocks cysteinyl leukotrienes, inflammatory mediators released by mast cells and eosinophils that cause bronchoconstriction and airway inflammation. Unlike inhaled corticosteroids, it is taken as a convenient oral tablet. FDA added a black box warning in 2020 for neuropsychiatric events (agitation, depression, suicidal ideation), limiting its use to patients who cannot use alternative therapies.
Approved indications
- Allergic asthma
- Allergic rhinitis
- Asthma management
- Exercise-Induced Bronchospasm Prevention
- Non-allergic asthma
Common side effects
- Upper respiratory infection
- Fever
- Headache
- Pharyngitis
- Cough
- Abdominal pain
- Diarrhea
- Otitis media
- Influenza
- Rhinorrhea
- Sinusitis
- Otitis
Serious adverse events
- Neuropsychiatric events
Key clinical trials
- An Open-label, Randomised, Single Dose, Three-Way Crossover, Six Sequence, Pilot Study to Determine the Relative Bioavailability of Montelukast Sodium 5mg From Two Candidate Chewable Tablet Formulatio (Phase 1)
- Multi-Institutional Prospective Phase II Study of Montelukast for the Treatment of Bronchiolitis Obliterans Following Allogeneic or Autologous Stem Cell Transplantation in Children and Adults (Phase 2)
- Montelukast and Nasa ICS for Treatment of Mild Obstructive Sleep Apnea in Adults (Phase 3)
- A Phase 3 Randomized, Open-label, Multicenter Study of Isatuximab (SAR650984) in Combination With Lenalidomide and Dexamethasone Versus Lenalidomide and Dexamethasone in Patients With High-risk Smolde (Phase 3)
- A Multicenter, Double-Blind, Randomized, Placebo-Controlled, Parallel-Group Study Investigating the Clinical Effects of Montelukast in Patients With Perennial Allergic Rhinitis (Phase 3)
- Comparative Study of the Effect of Two Doses of Mometasone Furoate Dry Powder Inhaler 200 mcg and 400 mcg QD PM, Fluticasone Propionate 250 mcg BID, and Montelukast 10 mg QD PM, on Bone Mineral Densit (Phase 4)
- Montelukast in Chronic Asthma: Non-interventional Study With Montelukast 10 mg (N/A)
- Montelukast, on Pediatric Bronchial Asthma in Multicenter Comparative Double-Blind Clinical Study (Phase IV) With Ketotifen Fumarate (Phase 4)
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Singulair CI brief — competitive landscape report
- Singulair updates RSS · CI watch RSS
- Merck & Co. portfolio CI