Novel Opportunity For Treatment Of Genetically Defined Human B-Cell Lymphomas

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BlankNovel Opportunity For Treatment Of Genetically Defined Human B-Cell

Lymphomas

16 Nov 2010

Epizyme, Inc., a company leading the discovery and development of

first-in-class, targeted cancer therapeutics against epigenetic targets, has

announced the publication of breakthrough new research in the Proceedings of the

National Academy of Sciences (USA). The discovery, centered on the epigenetic

enzyme EZH2, illuminates a clear path for the translation of basic science into

targeted therapies for the safe and effective treatment of specific forms of

human lymphomas. EZH2 is a histone methyltransferase (HMT), a class of enzymes

that play an important role in regulating the activity of particular groups of

genes that are involved in serious diseases, including cancer.

The paper describes how the development of two non-Hodgkin lymphomas -

follicular lymphoma and germinal center B-cell like subtype of diffuse large

B-cell lymphoma - requires the combined activities of both the wild-type and

Tyr641 mutants of EZH2. This novel insight reinforces the development of

targeted therapeutics for these patients, as it repudiates the previous

supposition that the Tyr641 mutation resulted in a loss of EZH2 function.

Dr. A. Copeland, EVP of R & D and CSO, said, " We believe this is the first

example of a human disease that is reliant on the combined catalytic activity of

both normal and disease-associated mutant enzymes. By targeting HMTs with clear

genetic disease associations, such as EZH2, Epizyme takes a hypothesis-driven

approach to development of personalized therapeutics for specific patient

populations with high unmet needs. Our product platform enables the creation of

novel, potent and selective small molecule HMT inhibitors. "

" This paper is a novel, important and representative example of the rapidly

growing understanding of the oncogenic role played by HMTs in many cancers. It

highlights the promise of HMT inhibitors as novel therapeutics against these

targets, " said Professor T. Walsh, the Hamilton Kuhn Professor of

Biological Chemistry and Molecular Pharmacology (BCMP) at Harvard Medical School

and a member of Epizyme's Scientific Advisory Board.