Overview
Montelukast was first approved for clinical use by the US FDA in 1998 as Merck's brand name Singulair. The medication is a member of the leukotriene receptor antagonist (LTRA) category of drugs. Although capable of demonstrating effectiveness, the use of such LTRAs like montelukast is typically in addition to or complementary with the use of inhaled corticosteroids or other agents in asthma step therapy. Regardless, in 2008-2009, there were FDA-led investigations into the possibility of montelukast to elicit neuropsychiatric effects like agitation, hallucinations, suicidal behaviour, and others in individuals who used the medication. And although these kinds of effects are currently included in the official prescribing information for montelukast, the drug still sees extensive use worldwide via millions of prescriptions annually and has since become available as a generic and as a brand name product.
Indication
Montelukast is indicated for: (a) the prophylaxis and chronic treatment of asthma in adults and pediatric patients who are 12 months of age and older, although other regional health authorities specifically note this indication for adults and adolescents who are 15 years and older and also include indications for preventing day and night-time symptoms, and the treatment of acetylsalicylic acid-sensitive asthma; (b) the prevention of exercise-induced bronchoconstriction (EIB) in patients who are 6 years of age and older, although other regional health authorities specifically note this indication for adults and adolescents who are 15 years and older; and (c) the relief of symptoms of seasonal allergic rhinitis in patients 2 years of age and older and perennial allergic rhinitis in patients 6 months of age and older, although other regional health authorities specifically note the relief of seasonal allergic rhinitis symptoms for adults and adolescents who are 15 years and older. Furthermore, some formulations like chewable montelukast tablets may also be specifically indicated by particular regulatory bodies for the prophylaxis and chronic treatment of asthma, including the prevention of day and night-time symptoms, the treatment of acetylsalicylic acid based asthma, and the prevention of exercise-induced bronchoconstriction in adult and pediatric patients aged 2 and older, between the ages 2 and 5, or between the ages of 6 and 14 years. Moreover, when employed for such indications montelukast is considered effective as monotherapy or when combined with other medications indicated for the maintenance treatment of chronic asthma. For instance, montelukast and inhaled corticosteroids can be used concomitantly to demonstrate additive effects to control asthma or to decrease the necessary inhaled corticosteroid dose while still maintaining clinical stability. Additionally, in patients who continue to experience asthma symptoms, montelukast can also be combined with an 'as required' short-acting beta-agonist, an inhaled corticosteroid, or inhaled corticosteroid paired with a long-acting beta-agonist.
Associated Conditions
- Asthma
- Exercise-Induced Bronchospasm
- Perennial Allergic Rhinitis (PAR)
- Seasonal Allergic Rhinitis
Research Report
Montelukast (DB00471): A Comprehensive Pharmacological, Clinical, and Regulatory Monograph
I. Executive Summary
Montelukast is a selective and orally active cysteinyl leukotriene receptor antagonist (CysLT1), developed by Merck & Co. and first marketed under the brand name Singulair. As a small molecule drug, it represents a targeted therapeutic approach to inflammatory airway diseases by blocking the pro-inflammatory cascade mediated by leukotrienes. Its established clinical utility lies in the prophylaxis and chronic treatment of asthma, the prevention of exercise-induced bronchoconstriction (EIB), and the symptomatic relief of both seasonal and perennial allergic rhinitis. In the therapeutic hierarchy, Montelukast is generally positioned as an alternative or adjunctive therapy. For asthma management, it is considered less effective than inhaled corticosteroids (ICS), which remain the first-line standard of care, but serves as a valuable option for patients with adherence issues to inhalers, specific asthma phenotypes such as aspirin-exacerbated respiratory disease, or those with a significant fear of steroids. In allergic rhinitis, its efficacy is comparable to second-generation antihistamines but inferior to intranasal corticosteroids.
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/08/03 | Not Applicable | Not yet recruiting | |||
2025/08/03 | Not Applicable | Not yet recruiting | |||
2025/03/20 | Early Phase 1 | Not yet recruiting | |||
2024/12/24 | Phase 2 | Recruiting | Phramongkutklao College of Medicine and Hospital | ||
2024/04/10 | Phase 2 | Recruiting | |||
2024/04/02 | Phase 3 | Not yet recruiting | |||
2023/11/02 | Phase 2 | Recruiting | Mostafa Bahaa | ||
2023/08/31 | Phase 4 | Completed | |||
2023/08/15 | Phase 1 | Recruiting | |||
2023/07/25 | Not Applicable | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| DIRECT RX | 72189-223 | ORAL | 5 mg in 1 1 | 5/21/2021 | |
| AvKARE | 42291-623 | ORAL | 5 mg in 1 1 | 1/3/2023 | |
| Dispensing Solutions Inc. | 68258-3032 | ORAL | 5 mg in 1 1 | 3/1/2010 | |
| Bryant Ranch Prepack | 71335-1979 | ORAL | 10 mg in 1 1 | 6/21/2021 | |
| Torrent Pharmaceuticals Limited | 13668-080 | ORAL | 5 mg in 1 1 | 6/28/2022 | |
| Pharmasource Meds, LLC | 82982-040 | ORAL | 10 mg in 1 1 | 3/29/2023 | |
| Preferred Pharmaceuticals, Inc. | 68788-8099 | ORAL | 10 mg in 1 1 | 8/13/2025 | |
| Torrent Pharmaceuticals Limited | 13668-081 | ORAL | 10 mg in 1 1 | 6/28/2022 | |
| A-S Medication Solutions | 50090-2921 | ORAL | 4 mg in 1 1 | 6/18/2021 | |
| Sandoz Inc | 0781-5555 | ORAL | 5 mg in 1 1 | 3/31/2021 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
| No EMA approvals found for this drug. | |||
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| MONTELAIR TABLET 10MG | SIN14788P | TABLET | 10mg | 5/26/2015 | |
| MONAST 4 MONTELUKAST SODIUM PAEDIATRIC CHEWABLE TABLET 4MG | SIN14954P | TABLET, CHEWABLE | 4.000 mg | 2/19/2016 | |
| ACTAMONE F.C. TABLET 10 MG | SIN15017P | TABLET, FILM COATED | 10.00 mg | 5/25/2016 | |
| Lukakline Chewable Tablet 4mg | SIN14330P | TABLET, CHEWABLE | 4 mg | 3/21/2013 | |
| Lukakline Tablet 10 mg | SIN14154P | TABLET, FILM COATED | 10 mg | 6/7/2012 | |
| MONTELUKAST-TEVA FC TABLET 10 MG | SIN16431P | TABLET, FILM COATED | 10 mg | 2/25/2022 | |
| REGULAIR CHEWABLE TABLET 5mg | SIN14977P | TABLET, CHEWABLE | 5mg | 4/5/2016 | |
| KLAIRMONT FILM-COATED TABLET 10MG | SIN15796P | TABLET, FILM COATED | 10mg | 9/4/2019 | |
| MONTELUKAST SANDOZ FILM COATED TABLET 10MG | SIN14385P | TABLET, FILM COATED | 10mg | 7/23/2013 | |
| M-KAST 10 FILM-COATED TABLETS 10MG | SIN16389P | TABLET, FILM COATED | 10mg | 11/25/2021 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| MONTELUKAST CH montelukast (as sodium) 4mg chewable tablet blister pack | 193242 | Medicine | A | 1/7/2013 | |
| MONTELUKAST TR 10 montelukast (as sodium) 10 mg uncoated tablet blister pack | 189245 | Medicine | A | 8/1/2012 | |
| MONTELUKAST TR 4 montelukast (as sodium) 4 mg chewable tablet blister pack | 189241 | Medicine | A | 8/1/2012 | |
| APX-MONTELUKAST montelukast 10 mg (as sodium) film-coated tablet blister pack | 184834 | Medicine | A | 5/17/2012 | |
| MONTELUKAST-GA montelukast (as sodium) 5 mg chewable tablet blister pack | 189216 | Medicine | A | 8/1/2012 | |
| MONTELUKAST CH montelukast (as sodium) 4mg chewable tablet bottle | 193243 | Medicine | A | 1/7/2013 | |
| APO-MONTELUKAST montelukast 4 mg (as sodium) chewable tablet bottle | 179111 | Medicine | A | 11/15/2011 | |
| SINGULAIR Montelukast (as sodium) 10 mg tablet blister pack | 61846 | Medicine | A | 5/11/1998 | |
| APO-MONTELUKAST montelukast 10mg (as sodium) tablet bottle | 170246 | Medicine | A | 8/9/2011 | |
| MONTELUKAST LUPIN montelukast 5 mg (as sodium) chewable tablet blister pack | 323022 | Medicine | A | 11/25/2019 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| APO-MONTELUKAST SODIUM CHEWABLE | 02517345 | Tablet (Chewable) - Oral | 5 MG | N/A | |
| APO-MONTELUKAST SODIUM | 02517329 | Tablet - Oral | 10 MG | N/A | |
| APO-MONTELUKAST SODIUM CHEWABLE | 02517337 | Tablet (Chewable) - Oral | 4 MG | N/A |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| SINGULAIR 10 MG COMPRIMIDOS RECUBIERTOS CON PELICULA | Organon Polska Sp. Z O.O. | 7957IP1 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized |
| SINGULAIR 10 MG COMPRIMIDOS RECUBIERTOS CON PELICULA | Organon Polska Sp. Z O.O. | 7957IP | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized |
| MONTELUKAST COMBIX 10 mg COMPRIMIDOS RECUBIERTOS CON PELICULA EFG | Laboratorios Combix S.L.U. | 75786 | COMPRIMIDO RECUBIERTO CON PELÍCULA | Medicamento Sujeto A Prescripción Médica | Commercialized |
| SINGULAIR 5 MG COMPRIMIDOS MASTICABLES | Organon Polska Sp. Z O.O. | 7956 | COMPRIMIDO MASTICABLE | Medicamento Sujeto A Prescripción Médica | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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