Epizyme (EPZM) Commences Dosing in Tazemetostat Phase 2 as Mesothelioma Treatment

August 11, 2016 6:31 AM EDT

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Epizyme, Inc. (Nasdaq: EPZM) announced that the first patient has been dosed in the Company’s global phase 2 study evaluating tazemetostat, a first-in-class EZH2 inhibitor, for the treatment of adults with mesothelioma characterized by BAP1 loss-of-function.

“Mesothelioma remains a cancer that is very difficult to treat and has an extremely poor prognosis,” said Marjorie Zauderer, M.D., medical oncologist at Memorial Sloan Kettering Cancer Center. “The overwhelming majority of patients are refractory to or relapse following first-line treatment with chemotherapy leaving them with no approved treatment options. The preclinical data demonstrating that EZH2 inhibition may play a role in the treatment of mesothelioma is promising, and I look forward to exploring the potential for tazemetostat as a targeted agent for patients with this devastating disease.”

Mesothelioma affects nearly 12,000 people each year in major markets, of which 40 to 60% have tumors characterized by BAP1 loss-of-function. The median overall survival for all patients with mesothelioma generally ranges from eight to 14 months from the time of diagnosis. The most commonly used first-line treatment consists of cisplatin or carboplatin combined with pemetrexed, which is the only drug approved (2004) for the treatment of mesothelioma1.

“Patient dosing in this phase 2 study marks another milestone for Epizyme and the expansion of our clinical development program into a new cancer indication for which there is a significant medical need,” said Peter Ho, M.D., Ph.D., Executive Vice President and Chief Medical Officer, Epizyme. “With this study, Epizyme now has four registration-supporting monotherapy trials underway with tazemetostat, and plans for two combination trials to be initiated later this year.”

Phase 2 Study Design

The international, open-label, phase 2 study will evaluate tazemetostat as a monotherapy in a total of 67 patients at multiple sites in the United States, United Kingdom and France. Tazemetostat is orally administered at a dose of 800 mg twice-daily. The safety and pharmacokinetic profile of tazemetostat will first be evaluated in 12 patients with relapsed or refractory mesothelioma regardless of BAP1 status. Subsequently, a total of 55 patients with relapsed or refractory mesothelioma characterized by BAP1 loss-of-function will be treated using a two-stage study design. The primary endpoint of the study is disease control rate (complete response, partial response or stable disease) at 12 weeks. Secondary endpoints include overall response rate, progression-free survival, duration of response and overall survival.

EZH2 Inhibition in Mesothelioma

Tazemetostat is a first-in-class small molecule inhibitor of EZH2 created by Epizyme using its proprietary drug development platform. Aberrant EZH2 activity results in misregulation of genes that control cell proliferation and has been associated with a diverse set of human cancers. Preclinical findings from published reports suggest that mesothelioma, and particularly mesothelioma characterized by BAP1 loss of function, may be sensitive to EZH2 inhibition2. Mesothelioma characterized by BAP1 loss of function accounts for 40 to 60 percent of the approximately 12,000 new mesothelioma cases each year in major markets3-6.

About the Tazemetostat Clinical Trial Program

Tazemetostat, a first-in-class EZH2 inhibitor, is currently being studied in ongoing phase 2 programs in non-Hodgkin lymphoma (NHL), certain genetically defined solid tumors, including INI1-negative and SMARCA4-negative tumors and synovial sarcoma, and mesothelioma.

The company plans to initiate additional clinical trials of tazemetostat in 2016, including a combination with R-CHOP in collaboration with the Lymphoma Study Association and a combination with Tecentriq™ (atezolizumab) in collaboration with Genentech, a member of the Roche Group, both in patients with diffuse large B-cell lymphoma.

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