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Macitentan

CHEMBL2103873 Phase 4 Одобрено 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.

Молекулярная масса

588,3000 g/mol

LogP

3,70

TPSA

137,00 Ų

Правило пяти Липинского

Соответствует

Терапевтические области

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

Механизм действия

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

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Механизм

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

2D Структура

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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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

                    

                    
                    

                        
Вращаемые Связи

                        
11

                    

                    
                    
                    

                        
Тяжёлые Атомы

                        
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.

    



                
            


            
            
            

                
Часто задаваемые вопросы

                

                    
                    

                        
                        

                            
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.




        


        
        
    


    



    
Медицинский отказ от ответственности

    

        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.