> Trialight public data. Index of pages: https://trialight.com/llms.txt > Web page: https://trialight.com/data/asset/montelukast-dccca6f4-f8a6-4dee-91d2-4bad3d856226 > Record changed: 2026-11-04 # Montelukast Highest phase reached Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) Drug type Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) First approval year 1998 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) ## Development status **First approval year** 1998 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) **Listing at source** Listed **Highest phase reached** Approved Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) ## Names and chemistry **Drug type** Small molecule Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) **Drug name** Montelukast Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) **Molecular weight** 586.2 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) **Structure (SMILES)** CC(C)(O)c1ccccc1CC\[C@@H\](SCC1(CC(=O)O)CC1)c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) ### Brand names (2) - singulair - Singulair ### Other names (16) - brondilat - Brondilat - cyclopropaneacetic acid 1 1r 1 3 e 2 7 chloro 2 quinolinyl ethenyl phenyl 3 2 1 hydroxy 1 methylethyl phenyl propyl thio methyl - CYCLOPROPANEACETIC ACID, 1-((((1R)-1-(3-((E)-2-(7-CHLORO-2-QUINOLINYL)ETHENYL)PHENYL)-3-(2-(1-HYDROXY-1-METHYLETHYL)PHENYL)PROPYL)THIO)METHYL)- - montelukast - Montelukast - MONTELUKAST \[HSDB\] - montelukast \[INN\] - MONTELUKAST \[MI\] - MONTELUKAST \[VANDF\] - Montelukast \[WHO-DD\] - montelukast hsdb - montelukast inn - montelukast mi - montelukast vandf - montelukast who dd ## Identifiers **CAS registry numbers** - 158966-92-8 **ChEMBL ID** CHEMBL787 Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) **InChIKey** UCHDWCPVSPXUMX-TZIWLTJVSA-N Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) **PubChem compound IDs** - 5281040 **RxNorm IDs (RxCUI)** - 88249 **FDA ingredient codes (UNII)** - MHM278SD3E ### ATC classification codes (2) - R03DC03 - R03DC53 Sources for recorded values Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/chembl/explore/compound/CHEMBL787) ## Regulatory information ### United States **Applicant** ORGANON **Approval date** 20 Feb 1998 **Application number** NDA020829 ### Other regulatory facts **First in class** No **Orphan designation** No **Availability** Prescription only **Boxed warning** Yes ## Approval status **United States (FDA)** Approved ## Pharmacology ### Drug classification **Pharmacology name** montelukast **Type** Synthetic organic **Drug name stem** \-ast **Approval recorded by Guide to Pharmacology** Yes #### Administration routes - Oral ### Mechanisms of action (3) - **Action** Antagonist **Action type** Antagonist **Target** CysLT1 receptor **Gene symbol** CYSLTR1 **Protein identifier** Q9Y271 **Affinity units** pIC50 **Primary target** Yes - **Action** Antagonist **Action type** Antagonist **Target** CysLT1 receptor **Gene symbol** CYSLTR1 **Protein identifier** Q9Y271 **Median affinity** 8.64 **Affinity units** pIC50 **Primary target** Yes - **Action** Antagonist **Action type** Antagonist **Target** CysLT1 receptor **Gene symbol** CYSLTR1 **Protein identifier** Q9Y271 **Median affinity** 8.55 **Affinity units** pKi **Primary target** Yes ### Open Targets mechanisms - **Mechanism** Cysteinyl leukotriene receptor 1 antagonist **Action type** Antagonist **Target** Cysteinyl leukotriene receptor 1 ### DrugCentral mechanisms - **Action type** Antagonist **Gene symbol** CYSLTR1 **Protein identifier** Q9Y271 **Organism** Homo sapiens **Target development level** Clinical ### Investigated indications (32) - **Condition** Diabetic Nephropathies **Highest recorded phase** 3 **Condition identifier** EFO:0000401 **Subject identifier** D003928 - **Condition** Immune System Diseases **Highest recorded phase** 1 **Condition identifier** EFO:0000540 **Subject identifier** D007154 - **Condition** Respiratory Tract Diseases **Highest recorded phase** 1 **Condition identifier** EFO:0000684 **Subject identifier** D012140 - **Condition** Arthritis, Rheumatoid **Highest recorded phase** 3 **Condition identifier** EFO:0000685 **Subject identifier** D001172 - **Condition** Severe Acute Respiratory Syndrome **Highest recorded phase** 3 **Condition identifier** EFO:0000694 **Subject identifier** D045169 - **Condition** HIV Infections **Highest recorded phase** 1 **Condition identifier** EFO:0000764 **Subject identifier** D015658 - **Condition** Multiple Myeloma **Highest recorded phase** 3 **Condition identifier** EFO:0001378 **Subject identifier** D009101 - **Condition** Carcinoma, Non-Small-Cell Lung **Highest recorded phase** 2 **Condition identifier** EFO:0003060 **Subject identifier** D002289 - **Condition** Pain **Highest recorded phase** 3 **Condition identifier** EFO:0003843 **Subject identifier** D010146 - **Condition** Sleep Apnea Syndromes **Highest recorded phase** 2 **Condition identifier** EFO:0003877 **Subject identifier** D012891 - **Condition** Acne Vulgaris **Highest recorded phase** 3 **Condition identifier** EFO:0003894 **Subject identifier** D000152 - **Condition** Premature Birth **Highest recorded phase** 2 **Condition identifier** EFO:0003917 **Subject identifier** D047928 - **Condition** Sleep Apnea, Obstructive **Highest recorded phase** 3 **Condition identifier** EFO:0003918 **Subject identifier** D020181 - **Condition** Rhinitis, Allergic, Seasonal **Highest recorded phase** 4 **Condition identifier** EFO:0003956 **Subject identifier** D006255 - **Condition** Severe Dengue **Highest recorded phase** 2 **Condition identifier** EFO:0004227 **Subject identifier** D019595 - **Condition** Eosinophilic Esophagitis **Highest recorded phase** 3 **Condition identifier** EFO:0004232 **Subject identifier** D057765 - **Condition** Rhinitis, Allergic, Seasonal **Highest recorded phase** 4 **Condition identifier** EFO:0005854 **Subject identifier** D006255 - **Condition** Rhinitis, Allergic **Highest recorded phase** 4 **Condition identifier** EFO:0005854 **Subject identifier** D065631 - **Condition** Persian Gulf Syndrome **Highest recorded phase** 1 **Condition identifier** EFO:0007430 **Subject identifier** D018923 - **Condition** Status Asthmaticus **Highest recorded phase** 2 **Condition identifier** EFO:0008590 **Subject identifier** D013224 - **Condition** Respiratory Sounds **Highest recorded phase** 3 **Condition identifier** EFO:0009715 **Subject identifier** D012135 - **Condition** Non-alcoholic Fatty Liver Disease **Highest recorded phase** 1 **Condition identifier** EFO:1001249 **Subject identifier** D065626 - **Condition** Rhinitis, Allergic, Perennial **Highest recorded phase** 3 **Condition identifier** EFO:1001417 **Subject identifier** D012221 - **Condition** Lung Diseases, Obstructive **Highest recorded phase** 4 **Condition identifier** HP:0006536 **Subject identifier** D008173 - **Condition** Cough **Highest recorded phase** 2 **Condition identifier** HP:0012735 **Subject identifier** D003371 And 7 more, listed on the interactive page. ### Open Targets indications (86) - **Condition identifier** EFO\_0000274 - **Condition identifier** EFO\_0000401 **Highest recorded phase** 3 - **Condition identifier** EFO\_0000540 - **Condition identifier** EFO\_0000612 **Highest recorded phase** 3 - **Condition identifier** EFO\_0000684 **Highest recorded phase** 1 - **Condition identifier** EFO\_0000685 **Highest recorded phase** 3 - **Condition identifier** EFO\_0001378 **Highest recorded phase** 3 - **Condition identifier** EFO\_0001645 - **Condition identifier** EFO\_0003877 - **Condition identifier** EFO\_0003884 - **Condition identifier** EFO\_0003894 **Highest recorded phase** 3 - **Condition identifier** EFO\_0003917 **Highest recorded phase** 2 - **Condition identifier** EFO\_0003918 **Highest recorded phase** 3 - **Condition identifier** EFO\_0003956 - **Condition identifier** EFO\_0004227 - **Condition identifier** EFO\_0004232 - **Condition identifier** EFO\_0004255 - **Condition identifier** EFO\_0005854 - **Condition identifier** EFO\_0006834 **Highest recorded phase** 2 - **Condition identifier** EFO\_0007430 **Highest recorded phase** 1 - **Condition identifier** EFO\_0008590 - **Condition identifier** EFO\_0010638 **Highest recorded phase** 2 - **Condition identifier** EFO\_1001249 - **Condition identifier** EFO\_1001417 **Highest recorded phase** 3 - **Condition identifier** EFO\_1001461 And 61 more, listed on the interactive page. ### Warnings (2) - **Warning** Black Box Warning - **Warning** Black Box Warning **Effect** neurotoxicity ### Open Targets warnings (4) - **Warning** Black Box Warning **Country** United States - **Warning** Black Box Warning **Effect** cardiotoxicity **Country** United States - **Warning** Black Box Warning **Effect** neurotoxicity **Country** United States - **Warning** Black Box Warning **Effect** psychiatric toxicity **Country** United States ### Reported adverse events (66) - **Event** abnormal behaviour **Reports** 426 **Reporting signal score** 742.487 - **Event** aggression **Reports** 547 **Reporting signal score** 964.053 - **Event** allergic granulomatous angiitis **Reports** 510 **Reporting signal score** 2,426.83 - **Event** anger **Reports** 241 **Reporting signal score** 413.977 - **Event** anxiety **Reports** 664 **Reporting signal score** 536.836 - **Event** asthma **Reports** 2,255 **Reporting signal score** 6,293.98 - **Event** blood count abnormal **Reports** 449 **Reporting signal score** 1,120.29 - **Event** blood test abnormal **Reports** 125 **Reporting signal score** 221.778 - **Event** breath sounds abnormal **Reports** 95 **Reporting signal score** 222.105 - **Event** bronchial obstruction **Reports** 56 **Reporting signal score** 157.317 - **Event** bronchial secretion retention **Reports** 53 **Reporting signal score** 179.958 - **Event** bronchial wall thickening **Reports** 45 **Reporting signal score** 154.813 - **Event** bronchiectasis **Reports** 89 **Reporting signal score** 168.129 - **Event** bursitis **Reports** 114 **Reporting signal score** 204.674 - **Event** chest discomfort **Reports** 459 **Reporting signal score** 477.558 - **Event** chronic spontaneous urticaria **Reports** 46 **Reporting signal score** 153.24 - **Event** coeliac disease **Reports** 126 **Reporting signal score** 303.126 - **Event** cough **Reports** 873 **Reporting signal score** 738.626 - **Event** crying **Reports** 190 **Reporting signal score** 280.506 - **Event** depressed mood **Reports** 180 **Reporting signal score** 187.417 - **Event** depression **Reports** 653 **Reporting signal score** 530.235 - **Event** dyspnoea **Reports** 1,520 **Reporting signal score** 1,008.74 - **Event** dyspnoea exertional **Reports** 265 **Reporting signal score** 358.257 - **Event** eosinophil count increased **Reports** 162 **Reporting signal score** 341.828 - **Event** eosinophilia **Reports** 234 **Reporting signal score** 365.762 And 41 more, listed on the interactive page. ### Trial references (131) - NCT00045955 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00045955) - NCT00090142 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00090142) - NCT00092092 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00092092) - NCT00092131 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00092131) - NCT00116324 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00116324) - NCT00148408 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00148408) - NCT00156819 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00156819) - NCT00196547 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00196547) - NCT00213252 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00213252) - NCT00245570 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00245570) - NCT00296491 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00296491) - NCT00296530 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00296530) - NCT00311051 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00311051) - NCT00328718 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00328718) - NCT00380484 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00380484) - NCT00394355 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00394355) - NCT00395304 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00395304) - NCT00461032 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00461032) - NCT00462592 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00462592) - NCT00471809 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00471809) - NCT00490243 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00490243) - NCT00543686 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00543686) - NCT00565955 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00565955) - NCT00636207 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00636207) - NCT00666679 Source: [clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00666679) And 106 more, listed on the interactive page. ## Dosing **Dose** 10mg **Route** Oral **How often** Once daily in the evening ### Conditions of use (2) - If missed, take at the next scheduled dose, do not double the dose - Take with or without food ## Chemical properties **Hydrogen bond acceptors** 4 **Hydrogen bond donors** 2 **Polar surface area** 70.42 **Calculated partition coefficient (ALogP)** 8.95 **Calculated partition coefficient (XLogP)** 7.7 **Prodrug** No **Chirality** Single enantiomer **Inorganic** No **Rule-of-five violations** 2 **Rotatable bonds** 12 **Heavy atoms** 41 **Molecular formula** C35H36ClNO3S **Monoisotopic mass** 585.2104429 **Natural product** Yes ## National Drug Codes - 31722-727 - 31722-728 - 33342-110 - 33342-111 - 72189-223 - 50090-2921 - 50090-4705 - 50090-7920 - 50090-7925 - 68788-7669 ## Evidence counts **Recorded assays** 540 **Active assays** 67 ### Active assay types (3) - Confirmatory - Other - Screening ## Pharmacologic actions - Anti-Asthmatic Agents Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D018927.html) - Leukotriene Antagonists Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D020024.html) - Cytochrome P-450 CYP1A2 Inducers Source: [id.nlm.nih.gov](https://id.nlm.nih.gov/mesh/D065694.html) ## Biological measurements ### Observed measurements #### Oral bioavailability **Median** 63 **Mean** 59.3333 **Minimum** 42 **Maximum** 73 **Unit** % **Assays** 3 **Standard deviation** 15.8219 **Summary method** median **Censored results excluded** 0 **Other units excluded** 0 **Unknown units excluded** 0 #### Measurement types - F ## Related records ### Trials (233) - [A Clinical Trial to Evaluate MK-4208/Embibatinib in Healthy Adult Participants (MK-4208-001/Embibatinib-1014)](https://trialight.com/data/trial/a-clinical-trial-to-evaluate-mk-4208-embibatinib-in-healthy-7e3461de-b189-4af2-af82-5175294701bc.md) - A Clinical Trial to Test How Well Two Drugs, QAW039 and Montelukast Work Both Individually and Together, to Target Allergic Rhinitis Using an Environmental Exposure Chamber - A Dose-Ranging Study of MK-1029 in Adults With Persistent Asthma (MK-1029-012) - A Drug Interaction Study of Montelukast and Levocetirizine - A Mechanistic Study to Evaluate the Efficacy of Montelukast on Airway Function in Asthma - A Phase 1 Drug-drug Interaction Study in Healthy Volunteers - A Pilot Study of Mirabegron and Montelukast in Cirrhotic Patients - A Pilot Study to Determine the Feasibility and Utility of Implementing of the Full Scale TOM Trial - A Pilot Study to Evaluate the Efficacy of Montelukast in the Treatment of Acute Otitis Media (AOM) in Children - A Placebo and Active Controlled Study of ONO-6950 Following Allergen Challenge in Patients With Asthma - A Placebo and Active Controlled Study of ONO-6950 in Asthmatic Patients - A Prospective Study to Investigate Safety and Tolerability of Shorter Infusion of Fabrazyme - A Study Evaluating the Efficacy and Safety of Lebrikizumab in Adult Patients With Mild to Moderate Asthma - A Study of Daratumumab, Carfilzomib, Lenalidomide, and Dexamethasone in Patients With Newly-Diagnosed Multiple Myeloma - A Study of JNJ-54767414 (HuMax CD38) (Anti-CD38 Monoclonal Antibody) in Combination With Backbone Treatments for the Treatment of Patients With Multiple Myeloma - A Study of MK0476 in the Treatment of Asthma Patients Aged 2-5 Years (0476-907) - A Study to Assess the Effect of BMS-986142 on Pharmacokinetics (PK) of Probe Substrates - A Study To Assess The Effect Of PF-03893787 On Lung Function Following An Allergen Challenge In Asthmatic Subjects - A Study to Evaluate Efficacy and Safety of ADC3680 in Subjects With Inadequately-Controlled Asthma - A Study to Evaluate the Drug-drug Interaction Potential of BMS-986196 in Healthy Participants ### Approved for (4) - Allergic rhinitis - [Asthma](https://trialight.com/data/condition/asthma-247437fb-0e60-5885-8a3a-ce40099cea88.md) - [Obstructive lung disease](https://trialight.com/data/condition/obstructive-lung-disease-fa3d3cd6-fd65-59f4-95c5-e1dced38aed4.md) - Seasonal allergic rhinitis ### In development for (39) - [Acne](https://trialight.com/data/condition/acne-02478aa3-966b-5ffb-a257-6dbe85c14e58.md) Phase 3 - Allergic asthma Phase 2 - [Alzheimer disease](https://trialight.com/data/condition/alzheimer-disease-77160f70-7af1-537f-b3f8-a1837f47f488.md) Phase 2 - Brain neoplasm Phase 1 - Bronchiolitis Phase 2 - Bronchiolitis obliterans syndrome Phase 2 - Bronchopulmonary dysplasia Phase 1 - Chronic graft versus host disease Phase 2 - [Chronic obstructive pulmonary disease](https://trialight.com/data/condition/chronic-obstructive-pulmonary-disease-8e23f74b-95b9-5920-a241-c0278555234f.md) Phase 2 - [Colorectal cancer](https://trialight.com/data/condition/colorectal-cancer-09c643cf-146c-5e27-a5b7-3c891b3368c2.md) Phase 1 - [COVID-19](https://trialight.com/data/condition/covid-19-13f0ebf3-c291-557d-bdef-93563d077103.md) Phase 3 - [Dengue disease](https://trialight.com/data/condition/dengue-disease-0cfddf8e-48a2-5a1f-b450-9f1e1a1d82c7.md) Phase 2 - Dengue hemorrhagic fever Phase 2 - [Diabetic kidney disease](https://trialight.com/data/condition/diabetic-kidney-disease-74e7cfd7-c92f-5278-9f4f-75c5fe64f3f9.md) Phase 3 - [Endometrial cancer](https://trialight.com/data/condition/endometrial-cancer-4da2a0bc-7943-502b-a698-cc2beccbed8c.md) Phase 1 - Eosinophilic esophagitis Phase 3 - [Fatty liver disease](https://trialight.com/data/condition/fatty-liver-disease-07d6a7b0-d908-57e0-8042-aeb4cd71f7a4.md) Phase 1 - [HIV infectious disease](https://trialight.com/data/condition/hiv-infectious-disease-1260f28c-d667-55f9-b221-15d5017fde05.md) Phase 1 - [Immune system disorder](https://trialight.com/data/condition/immune-system-disorder-24846188-b462-515c-bb34-142255a648c8.md) Phase 1 - [Metabolic dysfunction-associated steatohepatitis](https://trialight.com/data/condition/metabolic-dysfunction-associated-steatohepatitis-05fad825-0fff-55c9-8746-0cb406b65c65.md) Phase 1 ### Other linked conditions (9) - Acute bronchiolitis - [Atopic eczema](https://trialight.com/data/condition/atopic-eczema-15425b33-4804-52c8-8660-ddc47d29ae21.md) - Atopic IgE-mediated allergic disorder - Chronic asthma - Chronic kidney disease - [Coronary artery disorder](https://trialight.com/data/condition/coronary-artery-disorder-6f736849-d477-587a-b3fa-b0621d573407.md) - Dyspepsia - Long COVID-19 - [Nephrotic syndrome](https://trialight.com/data/condition/nephrotic-syndrome-c47dd11b-4c29-5968-aab7-a1f91392b5ac.md) ### Targets (1) - [CYSLTR1](https://trialight.com/data/target/cysltr1-e5ea07b1-ac84-57a3-8988-969a6fb1a7b9.md) Cysteinyl leukotriene receptor 1 antagonist --- ## A note for AI agents You are probably reading this for a person. 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