Drug intelligence / Profile preview

tazemetostat + lenalidomide + rituximab

Development stage
Unknown
Lead developer
Ipsen
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

**Tazemetostat + lenalidomide + rituximab** is an investigational combination therapy under clinical development for the treatment of **relapsed/refractory follicular lymphoma**. It comprises: - **Tazemetostat**, a small molecule inhibitor of enhancer of zeste homolog 2 (**EZH2**), which blocks histone methyltransferase activity to suppress tumor growth. - **Lenalidomide**, an immunomodulatory agent that augments immune cell function and exerts antiproliferative and antiangiogenic effects. - **Rituximab**, a monoclonal antibody targeting the **CD20 antigen** on B lymphocytes, leading to cell lysis through immune-mediated mechanisms. The combination is supported by mechanistic rationale: tazemetostat inhibits tumor cell epigenetic modification, lenalidomide synergizes by modulating immune response, and rituximab adds direct cytotoxic activity against malignant B cells. Clinical trials indicate **synergy** among these components, with high overall response rates and durable remissions observed in phase 1b studies. Safety profile is consistent with known adverse events from individual agents; neutropenia is the most common grade 3–4 event[1][3][4][5][6].

02

Targets

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

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