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tazemetostat + rituximab

Development stage: Unknown
Lead developer: Ipsen
Modality: Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration: Oral (tazemetostat), Intravenous (rituximab), Subcutaneous (rituximab)

Overview

**Tazemetostat + rituximab** is a combination regimen currently under investigation for the treatment of relapsed or refractory follicular lymphoma. - **Tazemetostat** is a first-in-class oral small molecule inhibitor of enhancer of zeste homolog 2 (EZH2), an epigenetic regulator implicated in cancer; its inhibition blocks methyltransferase activity on histone H3K27, suppressing tumor cell proliferation and survival[2][4][5]. - **Rituximab** is a monoclonal antibody targeting CD20 on B lymphocytes, mediating cell death via antibody-dependent cellular cytotoxicity and direct cytotoxicity[5]. Combination therapy is designed to leverage the cell killing and immune modulation of rituximab alongside the epigenetic antitumor effect of tazemetostat. The regimen is being studied in phase 1b/3 trials in patients with relapsed or refractory follicular lymphoma, especially in cases with mutant or wild-type EZH2. The combination has shown favorable safety and promising efficacy (objective response rate ~95% in early trials)[2][3][5].

Brand names: Tazverik (tazemetostat)Rituxan (rituximab)
Other names: tazemetostat + rituximab

Targets

EZH2 (Histone-lysine N-methyltransferase EZH2)CD20 (B-lymphocyte antigen CD20)

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