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Vorapaxar

CHEMBL493982 Phase 4 ได้รับการอนุมัติ Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
492.6 g/mol
LogP
5.3
Phase
4

Vorapaxar is a first-in-class protease-activated receptor 1 (PAR-1) antagonist that irreversibly blocks thrombin-mediated platelet activation at the PAR-1 receptor on platelet surfaces, reducing platelet aggregation without affecting other coagulation pathways. It is approved for reduction of thrombotic cardiovascular events in patients with established myocardial infarction or peripheral arterial disease, used as adjunctive antiplatelet therapy. Its novel mechanism complements ADP-receptor antagonists by targeting thrombin-mediated platelet activation.

น้ำหนักโมเลกุล

492.6000 g/mol

LogP

5.30

TPSA

77.50 Ų

Lipinski RO5

ผ่าน

ด้านการรักษา

HIV/AIDS

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

                    
CCOC(=O)N[C@@H]1CC[C@@H]2[C@@H](C1)C[C@H]1C(=O)O[C@H](C)[C@H]1[C@H]2/C=C/c1ccc(-c2cccc(F)c2)cn1

                

                

                
                

                    
InChI

                    
InChI=1S/C29H33FN2O4/c1-3-35-29(34)32-23-10-11-24-20(14-23)15-26-27(17(2)36-28(26)33)25(24)12-9-22-8-7-19(16-31-22)18-5-4-6-21(30)13-18/h4-9,12-13,16-17,20,23-27H,3,10-11,14-15H2,1-2H3,(H,32,34)/b12-9+/t17-,20+,23-,24-,25+,26-,27+/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C29H33FN2O4

                    

                    
                    

                        
HBD / HBA

                        
1 / 6

                    

                    
                    

                        
พันธะที่หมุนได้

                        
6

                    

                    
                    
                    

                        
อะตอมหนัก

                        
36

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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

                

                    
                    

                        
                        

                            
Vorapaxar is a first-in-class protease-activated receptor 1 (PAR-1) antagonist that irreversibly blocks thrombin-mediated platelet activation at the PAR-1 receptor on platelet surfaces, reducing platelet aggregation without affecting other coagulation pathways. It is approved for reduction of thrombotic cardiovascular events in patients with established myocardial infarction or peripheral arterial disease, used as adjunctive antiplatelet therapy. Its novel mechanism complements ADP-receptor antagonists by targeting thrombin-mediated platelet activation.

                        

                    

                    

                    

                    
                    

                        
                        

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

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Vorapaxar 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

    
    
        
        
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                ChEMBL — European Bioinformatics Institute (EBI).
                CHEMBL493982.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 10077130.
                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.