Epizyme Granted Patent Covering Diagnosis and Treatment of Cancers Associated with EZH2 Mutation

Patent provides protection until 2033 and complements Epizyme's issued composition of matter claims for EZH2 inhibitors

Cambridge, MA — Epizyme, Inc., a clinical stage biopharmaceutical company creating innovative personalized therapeutics for patients with genetically defined cancers, announced today that the U.S. Patent and Trademark Office has granted U.S. Patent No. 8,691,507 with claims that cover the identification of patients carrying EZH2 oncogenic mutations as candidates for treatment with EZH2 inhibitors. EZH2 is a histone methyltransferase (HMT) that can become oncogenic due to genetic alterations and cause non-Hodgkin lymphoma and solid tumors. The patent, entitled “Inhibitors of Human EZH2 and Methods of Use Thereof,” expires in 2033.

“We believe the issued claims, which cover detecting the presence of an EZH2 mutation and treatment with an EZH2 inhibitor, are the first instance of patented diagnostic applications for EZH2 cancers,” said Zoran Zdraveski Ph.D, J.D., Chief Patent Counsel, Epizyme. “These diagnostic and treatment claims complement our issued composition of matter claims that expire in 2032. Our growing patent estate reflects the potential of our product platform to create personalized therapeutics for patients with genetically defined cancers.”

Epizyme’s small molecule inhibitor of EZH2, EPZ-6438 (E7438), is currently being developed in a Phase 1/2 clinical trial in patients with advanced solid tumors or relapsed or refractory B-cell lymphoma. In 2014, Epizyme plans to initiate two proof of concept studies with EPZ-6438 pending Phase 1 completion, one in non-Hodgkin lymphoma patients with EZH2 point mutations and one in synovial sarcoma patients. EPZ-6438 is being developed in collaboration with Eisai, Inc.

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

About EPZ-6438 Epizyme and it’s partner Eisai are developing EPZ-6438, a small molecule inhibitor of EZH2 created with our proprietary product platform, for the treatment of non-Hodgkin lymphoma patients who have an oncogenic (cancer-causing) point mutation in EZH2. In many human cancers, misregulated EZH2 enzyme activity results in misregulation of genes that control cell proliferation — without these control mechanisms, cancer cells are free to grow rapidly.

Epizyme granted Eisai a worldwide license to EPZ-6438 (Eisai refers to this therapeutic candidate as E7438), subject to Epizyme’s right to opt in for co-development, co-commercialization and profit share arrangement with Eisai in the United States. Epizyme is working with Roche and Eisai to develop a companion diagnostic to identify patients with non-wild type EZH2, where EZH2 contains point mutations.

In June 2013, Epizyme and its partner Eisai initiated a Phase 1/2 clinical trial of EPZ-6438 in patients with advanced solid tumors or with relapsed or refractory B-cell lymphoma. This program is currently in the dose escalation phase. The company believes EPZ-6438 is the second HMTi to enter human clinical development (following Epizyme’s DOT1L inhibitor, EPZ-5676).

About Epizyme, Inc. Epizyme, Inc. 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). By focusing on the genetic drivers of cancers, Epizyme’s targeted science seeks to match the right medicines with the right patients for a personalized approach to cancer treatment.

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