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Tazemetostat

CHEMBL3414621 Phase 4 承認済み Small molecule
Half-Life
—
Bioavailability
—
Protein Binding
—
Molecular Weight
572.7 g/mol
LogP
4.2
Phase
4

Tazemetostat is an oral inhibitor of EZH2, the catalytic subunit of the polycomb repressive complex 2 (PRC2), which trimethylates histone H3 at lysine 27 (H3K27me3) to silence tumor suppressor genes. It is approved for relapsed or refractory follicular lymphoma with EZH2 mutations and for epithelioid sarcoma, and is under investigation for other EZH2-driven malignancies including bladder and breast cancers. By restoring silenced tumor suppressor gene expression, it exerts antiproliferative and pro-apoptotic effects.

分子量

572.7000 g/mol

LogP

4.20

TPSA

83.10 Ų

リピンスキーの五則

適合

治療領域

Melanoma Bladder Cancer Lymphoma Breast Cancer Prostate Cancer Leukemia

Pharmacokinetics (PK)

Pharmacodynamics (PD)

2D構造

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
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SMILES

                    
CCN(c1cc(-c2ccc(CN3CCOCC3)cc2)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)C1CCOCC1

                

                

                
                

                    
InChI

                    
InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)

                

                

                

                    
                    

                        
Molecular Formula

                        
C34H44N4O4

                    

                    
                    

                        
HBD / HBA

                        
2 / 6

                    

                    
                    

                        
回転可能結合数

                        
9

                    

                    
                    
                    

                        
重原子数

                        
42

                    

                    
                

            


            
            

                
                


    
    
        
    
    
    
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.

    



                
            


            
            
            

                
よくある質問

                

                    
                    

                        
                        

                            
Tazemetostat is an oral inhibitor of EZH2, the catalytic subunit of the polycomb repressive complex 2 (PRC2), which trimethylates histone H3 at lysine 27 (H3K27me3) to silence tumor suppressor genes. It is approved for relapsed or refractory follicular lymphoma with EZH2 mutations and for epithelioid sarcoma, and is under investigation for other EZH2-driven malignancies including bladder and breast cancers. By restoring silenced tumor suppressor gene expression, it exerts antiproliferative and pro-apoptotic effects.

                        

                    

                    

                    

                    

                    

                    

                        
                        

                            
Yes, Tazemetostat 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).
                CHEMBL3414621.
                Open-access bioactivity database.
            
        
    • 
        
        
        
  • 
            
            
                PubChem — National Center for Biotechnology Information (NCBI).
                CID 66558664.
                Chemical information database.
            
        
    • 
        
        
        
        
    

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




        


        
        
    


    



    
医学的免責事項

    

        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.