Epizyme announces strategic alliance with GSK to develop epigenetic therapeutics

Under the terms of the agreement, Epizyme will receive an upfront payment of $20 million, as well as research funding, and will also may be eligible to receive more than $630 million in total milestone payments

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CAMBRIDGE, Mass.—Epizyme has announced a global strategic alliance with GlaxoSmithKline (GSK) to discover, develop and market novel small-molecule therapeutics targeting histone methyltransferases (HMTs), which Epizyme calls "an important class of epigenetic enzymes," for the treatment of cancer and other diseases. The total potential value of the deal is more than $650 million.

GSK would pay $20 million upfront, plus research funding, along with a potential $630 million in developmental milestones. The alliance would leverage Epizyme's HMT discovery platform—including its proprietary chemical library, expertise, and intellectual property—against a set of drug targets for cancer and other diseases. In addition, 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 candidate selection, and GSK will be solely responsible for development and commercialization.  Neither company is being specific about the disease targets, but Epizyme noted in fall 2009, after a couple years of focusing only on cancer applications, that it saw broader opportunities for also pursuing therapies against inflammatory diseases, metabolic disorders and neurodegenerative conditions.

Epigenetic enzymes are a 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 reportedly offers the possibility of controlling pathways of gene expression that contribute to diseases without altering the genes themselves.

"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," says Dr. Robert Gould, president and CEO of Epizyme. "This collaboration validates our unique discovery platform and the targeted approach we bring to HMT therapeutics."

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