Epizyme, Inc., a company leading the discovery and development of personalized therapeutics for genetically-defined cancer patients, 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 $200 million in research, development and sales milestones and up to double-digit royalties.  Additionally, Eisai will fund 100 per cent 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, PhD, 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 tumours 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.