Epizyme, Celgene announce strategic partnership

Agreement to focus on developing HMT inhibitors

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CAMBRIDGE, Mass.--A new strategic partnership was announced today betweenEpizyme and Celgene International Sàrl, a subsidiary of Celgene Corporation, todiscover, develop and commercialize personalized therapeutics for patients withgenetically defined cancers. The therapeutics will seek to treat cancer byinhibiting histone methyltransferases (HMTs).
Per the terms of the agreement, Celgene will receive anexclusive option to license ex-U.S. rights to Epizyme's available HMT inhibitorprograms during an initial three-year period. In addition, Celgene also gainsthe right to extend its option period for a year with additional funding. As aresult of the strategic partnership, Epizyme will receive an upfront payment of$90 million, which includes an equity investment. For each HMT inhibitor thatCelgene licenses through the partnership, Epizyme stands to receive more than$160 million in milestone payments, as well as up to double-digit royalties onex-U.S. sales. The two companies will be working together to develop the HMTinhibitors and will both contribute funding for global development of theprograms.
"Our Celgene partnership is a transformational step inEpizyme's growth and is made possible by Celgene's vision and commitment topatients," Robert Gould, Ph.D., CEO and president of Epizyme, said in a pressrelease. "Through this collaboration, Epizyme gains access to Celgene's leadingdrug development resources, enabling us to substantially increase the breadthand depth of our efforts while retaining US rights to our pipeline ofpersonalized therapeutics."
HMTs are a class of epigenetic enzymes, with 96 memberstotal, many of which have been associated with cancer and other seriousdiseases. Targeting HMTs represents a new approach to affect pathways ofdisease-causing gene expression. Adding small chemical units such as methylgroups at specific locations on a histone can alter the structure of thechromatin and signal cells to run transcription on or off for certain genes,Epizyme notes on its site. "The selective addition of methyl groups to specificsites on the histones is controlled by the action of a unique class of enzymesknown as the histone methyltransferases (HMTs). Once the methyl group has beendeposited on the histone site, the affected genes continue to be regulated(turned on or off) until this chemical unit is removed by other enzymes, knownas histone demethylases," it adds, meaning that HMTs could provide long-lastingmodification of gene expression.
The partnership will make use of Epizyme's HMT inhibitorplatform, including its DOT1L HMT inhibitor program, which is in preclinicaldevelopment targeted at treating mixed lineage leukemia. Celgene licensed theex-U.S. rights to the program at the partnership's signing.
"Celgene is a leader in epigenetic therapies for cancerthrough our existing drugs, and continues to focus on delivering new drugs withhigh therapeutic impact in this area," Thomas Daniel, M.D., president ofResearch for Celgene, said in a press release regarding the agreement. "Epizyme'splatform, scientific leadership in histone methyltransferases and leadingposition on promising HMT targets offers an exciting complementary approach.Our collaboration with Epizyme is a key element of our strategy to develop newand innovative therapeutic paradigms."

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