Tazemetostat

Epizyme is developing tazemetostat, an orally administered, first-in-class small molecule EZH2 inhibitor, for the treatment of multiple types of hematological malignancies and genetically defined solid tumors. We are currently conducting a comprehensive development program for tazemetostat designed to identify efficient and accelerated pathways to treat as many patients as may benefit. 

In early clinical development, tazemetostat has demonstrated clinical activity and a generally well-tolerated safety profile in both patients with hematological malignancies and genetically defined solid tumors.

We are investigating tazemetostat as a single-agent therapy in multiple clinical trial, including Phase 2 clinical trials in patients with relapsed or refractory non-Hodgkin lymphoma (NHL), adult patients with certain genetically defined solid tumors, including INI1-negative tumors and synovial sarcoma, and patients with mesothelioma characterized by BAP loss of function. We are also conducting a clinical trial of tazemetostat in pediatric patients with certain genetically defined solid tumors, including INI1-negative tumors and synovial sarcoma.

Tazemetostat is also being evaluated as a combination therapy in two clinical trials. One study is evaluating tazemetostat  in combination with R-CHOP, a chemotherapy regimen, as a first-line treatment for newly diagnosed elderly, high-risk patients with diffuse large B-cell lymphoma (DLBCL), the most common type of NHL. This front-line study isbeing conducted under our collaboration with the Lymphoma Study Association.

The second combination study is with an immuno-oncology medicine. The clinical trial is evaluating tazemetostat in combination with Tecentriq™ (atezolizumab), in patients with relapsed or refractory DLBCL. Tecentriq is an anti-PD-L1 cancer immunotherapy approved by FDA. This study is being conducted by Genentech, a member of the Roche Group, under Epizyme’s collaboration agreement with Roche.

Epizyme holds global development and commercialization rights to tazemetostat ex-Japan. Eisai owns development and commercialization rights to tazemetostat in Japan, and a right of first negotiation to rights in the rest of Asia.