Drug intelligence / Profile preview

tazemetostat + venetoclax

Development stage
Discontinued
Lead developer
Ipsen
Modality
Small Molecules
Administration
Oral
01

Overview

Tazemetostat + venetoclax is an **investigational combination therapy** of two small molecule drugs: tazemetostat, an inhibitor of enhancer of zeste homolog 2 (EZH2), and venetoclax, a BCL2 inhibitor. This combination is being evaluated for use in patients with relapsed or refractory non-Hodgkin lymphoma, especially follicular lymphoma (FL) and diffuse large B-cell lymphoma (DLBCL). Tazemetostat blocks methyltransferase activity of EZH2, disrupting histone methylation and leading to reactivation of tumor suppressor genes. Venetoclax binds and inhibits BCL2, restoring the apoptotic process in malignant lymphocytes. Preclinical and early clinical studies show synergistic effects, particularly in tumors harboring both EZH2 and BCL2 alterations, leading to enhanced apoptosis and potential for improved efficacy compared with monotherapy. The regimen is oral, chemotherapy-free, and intended for individuals who have failed previous treatments[1][3][4][5][6][7][8][9][10].

02

Targets

BCL2L1 (B-cell lymphoma-extra large protein)EZH1EZH2 (Histone-lysine N-methyltransferase EZH2)MCL1 (Myeloid cell leukemia sequence 1)BCL-2 (BCL-2 family)

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