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Jan 15, 2015
 |  BC Innovations  |  Product R&D

Epizyme's mantle piece

Epizyme's next first-in-class histone methyltransferase cancer compound

Epigenetic modulation notched another target last month when Epizyme Inc. announced a preclinical compound against PRMT5 - an arginine methyltransferase - that shows activity in mouse models of mantle cell lymphoma. The next step is to discover what other cancers involve the target, and the biotech is hoping its partner GlaxoSmithKline plc will help it mine that landscape.

The enzyme is one of over 20 histone methyltransferases (HMTs) known to drive abnormal gene regulation and tumor growth.

Epizyme has been pursuing HMT inhibitors for cancer since 2007. Its EPZ-5676, which targets the arginine methyltransferase DOT1L, is in Phase I testing for leukemia, and EPZ-6438, a lysine methyltransferase inhibitor, is in Phase I/II trials for lymphoma and non-Hodgkin's lymphoma (NHL). EPZ-5676 is partnered with Celgene Corp. and EPZ-6438 is partnered with Eisai Co. Ltd.

EVP and CSO Robert Copeland told BioCentury the company created the new inhibitor of PRMT5 with a combination of chemical library screening for new chemical scaffolds and optimization through 3D structure-guided medicinal chemistry.

He said his group's strategy is to focus on cancers that have an "addiction to the enzymatic activity of a particular HMT. The literature suggests that PRMT5 is implicated in a number of solid and hematological cancers including...

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