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Tazemetostat

CHEMBL3414621 Phase 4 Đã phê duyệt 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.

Khối lượng phân tử

572,7000 g/mol

LogP

4,20

TPSA

83,10 Ų

Lipinski RO5

Đạt

Lĩnh vực điều trị

Bladder Cancer Melanoma Lymphoma Breast Cancer Prostate Cancer Leukemia

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Cấu trúc 2D

SVG PNG

Cite this structure


                        

                            
                            
                        

                    

                


                
                

                    

                    

                        
Embed this structure

                        

                        

                            
                            
                        

                    

                

                

                
                

                    
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

                    

                    
                    

                        
Liên kết có thể quay

                        
9

                    

                    
                    
                    

                        
Nguyên tử nặng

                        
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.

    



                
            


            
            
            

                
Câu hỏi thường gặp

                

                    
                    

                        
                        

                            
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.




        


        
        
    


    



    
Tuyên bố miễn trách y tế

    

        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.