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Montelukast

CHEMBL787 Phase 4 Approved Small molecule
Half-Life
2.7-5.5 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
586.2 g/mol
LogP
7.7
Phase
4

This medication blocks leukotriene receptors, reducing airway inflammation and constriction in the lungs and relieving allergy symptoms in the nose and skin. It is taken once daily by mouth to prevent asthma attacks and treat allergic rhinitis and hives.

Molecular Weight

586.1800 g/mol

LogP

7.70

TPSA

95.70 Ų

Lipinski RO5

Fail

Therapeutic Areas

Asthma Atopic Dermatitis Breast Cancer Chronic Obstructive Pulmonary Disease Chronic Pain Colorectal Cancer Gastroesophageal Reflux Disease Generalized Anxiety Disorder Hepatitis C Multiple Sclerosis Non-Small Cell Lung Cancer Obesity Oncology Ovarian Cancer Pain Management Respiratory Disease Rheumatoid Arthritis Type 2 Diabetes

Drug Classes

R — R - Respiratory System

Mechanism of Action

Selective leukotriene D4 receptor antagonist.

Pharmacokinetics (PK)

Half-Life 2.7-5.5 hours

Pharmacodynamics (PD)

Mechanism

Selective leukotriene D4 receptor antagonist.

2D Structure

SVG PNG

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SMILES

                    
CC(C)(O)c1ccccc1CC[C@@H](SCC1(CC(=O)O)CC1)c1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1

                

                

                
                

                    
InChI

                    
InChI=1S/C35H36ClNO3S/c1-34(2,40)30-9-4-3-7-25(30)13-17-32(41-23-35(18-19-35)22-33(38)39)27-8-5-6-24(20-27)10-15-29-16-12-26-11-14-28(36)21-31(26)37-29/h3-12,14-16,20-21,32,40H,13,17-19,22-23H2,1-2H3,(H,38,39)/b15-10+/t32-/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C35H36ClNO3S

                    

                    
                    

                        
HBD / HBA

                        
2 / 5

                    

                    
                    

                        
Rotatable Bonds

                        
12

                    

                    
                    
                    

                        
Heavy Atoms

                        
41

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            PTGS2 (Cyclooxygenase-2)
                            Antagonist
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            PPARG (Peroxisome Proliferator-Activated Receptor Gamma)
                            Other
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Minor


                            
                                Montelukast + Phenytoin
                            
                        

                        
                        
Phenytoin, a potent CYP inducer, can increase the metabolism of montelukast, potentially reducing its plasma levels and therapeutic efficacy.

                        
                    
                    
                    
                        

                            

  
  Minor


                            
                                Montelukast + Fluconazole
                            
                        

                        
                        
Fluconazole inhibits CYP2C8-mediated metabolism of montelukast, modestly increasing montelukast plasma concentrations; the clinical impact is generally minor given montelukast's wide therapeutic index.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Frequently Asked Questions

                

                    
                    

                        
                        

                            
This medication blocks leukotriene receptors, reducing airway inflammation and constriction in the lungs and relieving allergy symptoms in the nose and skin. It is taken once daily by mouth to prevent asthma attacks and treat allergic rhinitis and hives.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Selective leukotriene D4 receptor antagonist.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Montelukast: Half-life: 2.7-5.5 hours.

                        

                    

                    

                    

                        
                        

                            
Yes, Montelukast is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.

                        

                    

                

            

            

            
            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Albuterol
                            Small molecule
                        
                        
                        
                            Cetirizine
                            Small molecule
                        
                        
                        
                            Diphenhydramine
                            Small molecule
                        
                        
                        
                            Loratadine
                            Small molecule
                        
                        
                    

                

                

                
                
                
            

            

            
            
{# References & Data Sources section for drug detail pages.
   Renders standard pharmacological database links plus the drug's data_sources field. #}


    
References & Data Sources

    
    
        
        
  • 
            
            
                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL787.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 5281040.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.




        


        
        
    


    



    
Medical Disclaimer

    

        This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.
    

    

        Data sources:
        ChEMBL,
        PubChem,
        DailyMed.