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Epizyme Enrolls First Patient In Phase 1/2 Clinical Trial Of EPZ-6438, An Inhibitor Of EZH2

CAMBRIDGE, Mass., June 13, 2013 /PRNewswire/ --  Epizyme, Inc., (NASDAQ: EPZM) a clinical stage biopharmaceutical company creating innovative personalized therapeutics for patients with genetically defined cancers, announced today that the first patient has been enrolled in a Phase 1/2 clinical trial of EPZ-6438 (E7438). The trial is designed to assess the safety, tolerability and pharmacokinetics of EPZ-6438 (E7438), an orally available, small molecule inhibitor for non-Hodgkin lymphoma patients who have a cancer-causing (oncogenic) point mutation in EZH2.

Epizyme is developing EPZ-6438 (E7438) in partnership with Eisai Co., Ltd. In April 2011, the two companies announced a worldwide partnership to discover, develop and commercialize therapeutics targeting EZH2, with Epizyme retaining an opt-in right to co-develop, co-commercialize and share profits with Eisai on licensed products in the United States. As a result of the first patient enrollment in this trial, Epizyme earned a $6 million milestone payment from Eisai.

About EZH2 Cancers

EZH2 is a histone methyltransferase (HMT) that can become oncogenic and cause non-Hodgkin lymphoma and solid tumors. Two types of non-Hodgkin lymphoma, diffuse large B-cell lymphoma of germinal-center origin, or DLBCL, and follicular lymphoma, or FL, are mainly associated with oncogenic EZH2 mutations. Currently, there are no therapies approved specifically for the treatment of non-Hodgkin lymphoma associated with an EZH2 point mutation.

About Epizyme, Inc.

Epizyme is a clinical stage biopharmaceutical company creating personalized therapeutics for patients with genetically defined cancers. Epizyme has built a proprietary product platform that the company uses to create small molecule inhibitors of a 96-member class of enzymes known as histone methyltransferases, or HMTs. HMTs are part of the system of gene regulation, referred to as epigenetics, that controls gene expression. Genetic alterations can result in changes to the activity of HMTs, making them oncogenic (cancer-causing).

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