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Apixaban

CHEMBL231779 Phase 4 Одобрено Small molecule
Half-Life
12 hours
Bioavailability
—
Protein Binding
—
Molecular Weight
459.5 g/mol
LogP
2.2
Phase
4

Apixaban is a direct Factor Xa inhibitor that blocks a pivotal enzyme in the clotting cascade, the point where the intrinsic and extrinsic pathways converge to generate thrombin. Halting Factor Xa slows clot formation and lowers the risk of stroke in atrial fibrillation while treating and preventing deep vein thrombosis and pulmonary embolism. Unlike older anticoagulants, it is taken by mouth and acts directly on its target without requiring routine blood-level monitoring. A small molecule (C25H25N5O4) with a half-life of about 12 hours, it is typically dosed twice daily to maintain a steady effect. Its predictable, targeted action on a single clotting factor distinguishes it from agents that broadly disrupt the coagulation system. Apixaban is an approved oral anticoagulant among the direct Factor Xa inhibitors.

A Factor Xa inhibitor that blocks a critical step in the clotting cascade to prevent blood clots from forming, reducing the risk of stroke in atrial fibrillation and treating or preventing deep vein thrombosis and pulmonary embolism. It is taken by mouth and does not require routine blood monitoring.

Молекулярная масса

459,4970 g/mol

LogP

2,20

TPSA

111,00 Ų

Правило пяти Липинского

Соответствует

Терапевтические области

Ovarian Cancer Pancreatic Cancer Bladder Cancer Thyroid Cancer Cardiovascular Disease Non-Small Cell Lung Cancer Migraine Inflammatory Bowel Disease Systemic Lupus Erythematosus Chronic Kidney Disease Stroke Deep Vein Thrombosis / Pulmonary Embolism Obesity Lymphoma Type 2 Diabetes Hypertension Breast Cancer Heart Failure Atrial Fibrillation Prostate Cancer Colorectal Cancer Leukemia

Классы препаратов

B — B - Blood and Blood Forming Organs

Механизм действия

Direct Factor Xa inhibitor.

Pharmacokinetics (PK)

Half-Life 12 hours

Pharmacodynamics (PD)

Механизм

Direct Factor Xa inhibitor.

2D Структура

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
SMILES

                    
COc1ccc(-n2nc(C(N)=O)c3c2C(=O)N(c2ccc(N4CCCCC4=O)cc2)CC3)cc1

                

                

                
                

                    
InChI

                    
InChI=1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)

                

                

                

                    
                    

                        
Molecular Formula

                        
C25H25N5O4

                    

                    
                    

                        
HBD / HBA

                        
1 / 5

                    

                    
                    

                        
Вращаемые Связи

                        
5

                    

                    
                    
                    

                        
Тяжёлые Атомы

                        
34

                    

                    
                

            


            
            

                
                

                    
                    

                        

                            F10 (Factor Xa)
                            Inhibitor
                        

                        
                        Primary Target
                        
                    

                    
                    

                        

                            CYP3A4 (Cytochrome P450 3A4)
                            Substrate
                        

                        
                    

                    
                

                
            


            
            

                
                

                    
                    
                        

                            

  
  Major


                            
                                Apixaban + Fluconazole
                            
                        

                        
                        
Fluconazole increases apixaban plasma concentrations significantly through dual CYP3A4 and P-gp inhibition, raising bleeding risk.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Apixaban + Ibuprofen
                            
                        

                        
                        
NSAIDs combined with apixaban significantly elevate the risk of GI and other bleeding through additive effects on hemostasis and gastric mucosal injury.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Apixaban + Clopidogrel
                            
                        

                        
                        
Triple antithrombotic therapy (apixaban + clopidogrel ± aspirin) carries the highest bleeding risk of any oral antithrombotic combination.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Apixaban + Naproxen
                            
                        

                        
                        
Naproxen with apixaban significantly increases GI bleeding risk through additive effects on hemostasis and direct gastric mucosal damage.

                        
                    
                    
                    
                        

                            

  
  Major


                            
                                Apixaban + Cyclosporine
                            
                        

                        
                        
Cyclosporine significantly increases apixaban exposure through inhibition of CYP3A4 and P-glycoprotein, elevating bleeding risk.

                        
                    
                    
                    
                        

                            

  
  Moderate


                            
                                Apixaban + Aspirin
                            
                        

                        
                        
Combining apixaban with aspirin increases major bleeding risk beyond that of either agent alone through additive antithrombotic and gastric mucosal effects.

                        
                    
                    
                

                
            


            
            

                
                


    
    
        
    
    
    
No side effects recorded

    
    
Side effect data is not yet available for this drug.

    



                
            


            
            
            

                
Часто задаваемые вопросы

                

                    
                    

                        
                        

                            
A Factor Xa inhibitor that blocks a critical step in the clotting cascade to prevent blood clots from forming, reducing the risk of stroke in atrial fibrillation and treating or preventing deep vein thrombosis and pulmonary embolism. It is taken by mouth and does not require routine blood monitoring.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Direct Factor Xa inhibitor.

                        

                    

                    

                    
                    

                        
                        

                            
Key pharmacokinetic parameters for Apixaban: Half-life: 12 hours.

                        

                    

                    

                    

                        
                        

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

                        

                    

                

            

            

            
            
            

                
                
                    ADME Journey →
                
                
                
            

            

            
            
            

                
Related Drugs


                
                

                    
Same Drug Class

                    

                        
                        
                            Warfarin
                            Small molecule
                        
                        
                        
                            Clopidogrel
                            Small molecule
                        
                        
                        
                            Rivaroxaban
                            Small molecule
                        
                        
                        
                            Dabigatran
                            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).
                CHEMBL231779.
                Open-access bioactivity database.
            
        
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  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 10182969.
                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.