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Sitaxentan

CHEMBL282724 Phase 4 ได้รับการอนุมัติ Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
454.9 g/mol
LogP
3.7
Phase
4

Sitaxentan is a selective endothelin-A (ETA) receptor antagonist developed for the treatment of pulmonary arterial hypertension (PAH), where it reduces pulmonary vascular resistance by blocking endothelin-1-mediated vasoconstriction. Unlike dual endothelin receptor antagonists, its selectivity for ETA preserves the vasodilatory and clearance functions of the ETB receptor while blocking the vasoconstrictive ETA pathway. It was withdrawn from the market due to severe hepatotoxicity, including fatal cases.

น้ำหนักโมเลกุล

454.9000 g/mol

LogP

3.70

TPSA

144.00 Ų

Lipinski RO5

ผ่าน

ด้านการรักษา

Asthma Chronic Kidney Disease Hypertension Heart Failure

กลไกการออกฤทธิ์

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

Pharmacokinetics (PK)

Pharmacodynamics (PD)

กลไก

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

โครงสร้าง 2 มิติ

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
Cc1cc2c(cc1CC(=O)c1sccc1S(=O)(=O)Nc1onc(C)c1Cl)OCO2

                

                

                
                

                    
InChI

                    
InChI=1S/C18H15ClN2O6S2/c1-9-5-13-14(26-8-25-13)7-11(9)6-12(22)17-15(3-4-28-17)29(23,24)21-18-16(19)10(2)20-27-18/h3-5,7,21H,6,8H2,1-2H3

                

                

                

                    
                    

                        
Molecular Formula

                        
C18H15ClN2O6S2

                    

                    
                    

                        
HBD / HBA

                        
1 / 9

                    

                    
                    

                        
พันธะที่หมุนได้

                        
6

                    

                    
                    
                    

                        
อะตอมหนัก

                        
29

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
คำถามที่พบบ่อย

                

                    
                    

                        
                        

                            
Sitaxentan is a selective endothelin-A (ETA) receptor antagonist developed for the treatment of pulmonary arterial hypertension (PAH), where it reduces pulmonary vascular resistance by blocking endothelin-1-mediated vasoconstriction. Unlike dual endothelin receptor antagonists, its selectivity for ETA preserves the vasodilatory and clearance functions of the ETB receptor while blocking the vasoconstrictive ETA pathway. It was withdrawn from the market due to severe hepatotoxicity, including fatal cases.

                        

                    

                    

                    

                    
                    

                        
                        

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

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Sitaxentan 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).
                CHEMBL282724.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 216235.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
ข้อจำกัดความรับผิดชอบทางการแพทย์

    

        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.