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Macitentan

CHEMBL2103873 Phase 4 Approuvé Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
588.3 g/mol
LogP
3.7
Phase
4

An endothelin receptor antagonist used to treat pulmonary arterial hypertension (PAH) by blocking the action of endothelin, a substance that causes blood vessels in the lungs to narrow. It helps improve exercise capacity and slow disease progression.

Masse moléculaire

588,3000 g/mol

LogP

3,70

TPSA

137,00 Ų

Règle des 5 de Lipinski

Conforme

Aires thérapeutiques

Cardiovascular Disease Respiratory Disease Chronic Obstructive Pulmonary Disease Alzheimer's Disease Parkinson's Disease Infectious Disease Gastroesophageal Reflux Disease Inflammatory Bowel Disease Chronic Kidney Disease Non-Alcoholic Fatty Liver Disease Deep Vein Thrombosis / Pulmonary Embolism Hypertension Heart Failure

Mécanisme d'action

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mécanisme

Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

Structure 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
CCCNS(=O)(=O)Nc1ncnc(OCCOc2ncc(Br)cn2)c1-c1ccc(Br)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C19H20Br2N6O4S/c1-2-7-26-32(28,29)27-17-16(13-3-5-14(20)6-4-13)18(25-12-24-17)30-8-9-31-19-22-10-15(21)11-23-19/h3-6,10-12,26H,2,7-9H2,1H3,(H,24,25,27)

                

                

                

                    
                    

                        
Molecular Formula

                        
C19H20Br2N6O4S

                    

                    
                    

                        
HBD / HBA

                        
2 / 10

                    

                    
                    

                        
Liaisons Rotatives

                        
11

                    

                    
                    
                    

                        
Atomes Lourds

                        
32

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
No targets recorded

    
    
Target interaction data is not yet available for this drug.

    



                
            


            
            

                
                


    
    
        
    
    
    
No interactions recorded

    
    
Drug interaction data is not yet available for this compound.

    



                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Foire aux questions

                

                    
                    

                        
                        

                            
An endothelin receptor antagonist used to treat pulmonary arterial hypertension (PAH) by blocking the action of endothelin, a substance that causes blood vessels in the lungs to narrow. It helps improve exercise capacity and slow disease progression.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Competitively binds to its target receptor without activating it, blocking the natural ligand from binding and preventing receptor-mediated signaling.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Macitentan is an approved drug. It has reached clinical phase 4. It is classified as a 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).
                CHEMBL2103873.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 16004692.
                Chemical information database.
            
        
    • 
        
        
        
        
    

    
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-04.




        


        
        
    


    



    
Avertissement médical

    

        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.