Drug intelligence / Profile preview

tazemetostat + lenalidomide

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

Overview

Tazemetostat + lenalidomide is a **combination regimen** under investigation for the treatment of relapsed/refractory follicular lymphoma and other B-cell lymphomas. **Tazemetostat** is a small molecule inhibitor of enhancer of zeste homolog 2 (**EZH2**), a histone lysine methyltransferase that regulates gene expression and cell differentiation; its inhibition leads to impaired proliferation and survival of cancer cells. **Lenalidomide** is an immunomodulatory agent that enhances immune-mediated destruction of tumor cells, inhibits angiogenesis, and has direct cytotoxic effects. The regimen is typically studied in combination with rituximab, but this entry details the combination of tazemetostat and lenalidomide specifically. Tazemetostat is developed by Epizyme and works as a targeted therapy for patients with either EZH2-mutant or wild-type disease[1][2][3][4][5][6][10]. Lenalidomide is developed and manufactured by Celgene; it is approved for several hematologic malignancies, including multiple myeloma and follicular lymphoma.

02

Targets

CRBN (Cereblon)EZH2 (Histone-lysine N-methyltransferase EZH2)IL-6 (Interleukin 6)TNFA (Tumor necrosis factor alpha (soluble))

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