Epizyme Achieves $4 Million Pre-Clinical Milestone Payment in Eisai Strategic Partnership

Epizyme, Inc., a company leading the discovery and development of personalized therapeutics for genetically-defined cancer patients, today announced the achievement of a pre-clinical milestone in its alliance with Eisai Co., Ltd., triggering a $4 million milestone payment. Epizyme and Eisai entered a worldwide strategic alliance in March 2011 to discover, develop and commercialize therapeutics targeting EZH2, an epigenetic enzyme, for the treatment of lymphoma and other cancers in genetically-defined patients. Under the terms of the agreement, Epizyme may earn more than $200M in research, development and sales milestones and up to double-digit royalties. Additionally, Eisai will fund 100 percent of R&D through human proof-of-concept, at which point Epizyme has the right to opt into a profit share and co-commercialization arrangement for the United States.

Robert Copeland, Ph.D., EVP and CSO of Epizyme, said: “EZH2 is a very promising oncogenic target with strong validation in genetically-defined cancers, including subtypes of lymphoma and solid tumors with high unmet therapeutic needs. It has been less than a year since we began our partnership with Eisai. The significant progress we have made in this time affirms Epizyme’s ability to discover and pursue small molecule histone methyltransferase inhibitors as personalized therapeutics for genetically-defined cancer patients.”

The HMT class of epigenetic enzymes contains 96 members, many of which have strong genetic associations with cancer and other serious diseases. Targeting HMTs with potent and selective small molecule inhibitors offers an innovative therapeutic approach to controlling pathways of disease-causing gene expression.

About Epizyme

Epizyme is leading the discovery and development of small molecule histone methyltransferase (HMT) inhibitors, a new class of personalized therapeutics for the treatment of genetically-defined cancer patients based on breakthroughs in the field of epigenetics. Genetic alterations in the HMTs are strongly associated with the underlying causes of multiple human diseases, including cancer. Epizyme’s patient-driven approach represents the future of personalized therapeutics by creating better medicines for the right patients more quickly and at lower cost than traditional approaches. www.epizyme.com