GSK, Epizyme enter partnership to discover, develop, and market epigenetic therapeutics

Epizyme today announced a worldwide strategic alliance with GlaxoSmithKline (GSK) to discover, develop, and market novel small molecule therapeutics targeting histone methyltransferases (HMTs), an important class of epigenetic enzymes, for the treatment of cancer and other diseases.

“Epizyme's mission is to develop personalized therapeutics for genetically-defined patients based on our understanding of the driving role played by many HMTs in human disease. We are excited to be working with GSK. This collaboration validates our unique discovery platform and the targeted approach we bring to HMT therapeutics.”

This alliance leverages Epizyme's unique HMT discovery platform, including its proprietary chemical library, expertise, and intellectual property, to discover and develop HMT therapeutics against the set of targets to be included in the collaboration. Under the terms of the agreement, Epizyme will receive an upfront payment of $20 million, as well as research funding. Epizyme is eligible to receive more than $630 million in total milestone payments if medicines are commercialized for all targets in the collaboration. Additionally, Epizyme is eligible to receive up to double-digit royalties on net sales of products resulting from the alliance. For each target in the collaboration, Epizyme will be primarily responsible for research up to development candidate selection, and GSK will be solely responsible for development and commercialization.

Epigenetic enzymes are an important class of proteins that regulate whether genes are turned off or on. The HMT family of epigenetic enzymes contains as many as 96 members, many of which have been associated genetically with cancer and other diseases. Targeting specific HMTs with potent and selective small molecule therapeutics offers the possibility of controlling pathways of gene expression that contribute to diseases.

Robert Gould, Ph.D., CEO and President of Epizyme, said: "Epizyme's mission is to develop personalized therapeutics for genetically-defined patients based on our understanding of the driving role played by many HMTs in human disease. We are excited to be working with GSK. This collaboration validates our unique discovery platform and the targeted approach we bring to HMT therapeutics."