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Tenofovir Alafenamide

CHEMBL2107825 Phase 4 Zugelassen Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
476.5 g/mol
LogP
1.9
Phase
4

Tenofovir alafenamide (TAF) is a prodrug of tenofovir, a nucleotide reverse transcriptase inhibitor (NRTI) that, after intracellular activation to tenofovir diphosphate, competitively inhibits HIV and HBV reverse transcriptase and terminates DNA chain elongation. Compared to tenofovir disoproxil fumarate, TAF delivers higher intracellular concentrations of active metabolite in lymphocytes at substantially lower plasma tenofovir exposures, resulting in reduced renal and bone toxicity. It is a cornerstone of modern combination antiretroviral therapy regimens.

Molekularmasse

476,5000 g/mol

LogP

1,90

TPSA

143,00 Ų

Lipinski-Regel der Fünf

Bestanden

Therapeutische Bereiche

Rheumatoid Arthritis Osteoporosis Generalized Anxiety Disorder Multiple Sclerosis Non-Alcoholic Fatty Liver Disease Obesity Lymphoma Hypertension HIV/AIDS Hepatitis C Tuberculosis Heart Failure Cardiovascular Disease Leukemia

Wirkmechanismus

Administered as an inactive precursor that is metabolically converted to its active form in the body. This prodrug design improves bioavailability, absorption, or targeted delivery compared to the active compound.

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Mechanismus

Administered as an inactive precursor that is metabolically converted to its active form in the body. This prodrug design improves bioavailability, absorption, or targeted delivery compared to the active compound.

2D-Struktur

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
CC(C)OC(=O)[C@H](C)N[P@](=O)(CO[C@H](C)Cn1cnc2c(N)ncnc21)Oc1ccccc1

                

                

                
                

                    
InChI

                    
InChI=1S/C21H29N6O5P/c1-14(2)31-21(28)16(4)26-33(29,32-17-8-6-5-7-9-17)13-30-15(3)10-27-12-25-18-19(22)23-11-24-20(18)27/h5-9,11-12,14-16H,10,13H2,1-4H3,(H,26,29)(H2,22,23,24)/t15-,16+,33+/m1/s1

                

                

                

                    
                    

                        
Molecular Formula

                        
C21H29N6O5P

                    

                    
                    

                        
HBD / HBA

                        
2 / 10

                    

                    
                    

                        
Rotierbare Bindungen

                        
12

                    

                    
                    
                    

                        
Schwere Atome

                        
33

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
Häufig gestellte Fragen

                

                    
                    

                        
                        

                            
Tenofovir alafenamide (TAF) is a prodrug of tenofovir, a nucleotide reverse transcriptase inhibitor (NRTI) that, after intracellular activation to tenofovir diphosphate, competitively inhibits HIV and HBV reverse transcriptase and terminates DNA chain elongation. Compared to tenofovir disoproxil fumarate, TAF delivers higher intracellular concentrations of active metabolite in lymphocytes at substantially lower plasma tenofovir exposures, resulting in reduced renal and bone toxicity. It is a cornerstone of modern combination antiretroviral therapy regimens.

                        

                    

                    

                    

                    
                    

                        
                        

                            
Administered as an inactive precursor that is metabolically converted to its active form in the body. This prodrug design improves bioavailability, absorption, or targeted delivery compared to the active compound.

                        

                    

                    

                    

                    

                        
                        

                            
Yes, Tenofovir Alafenamide 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).
                CHEMBL2107825.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 9574768.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
Medizinischer Haftungsausschluss

    

        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.