Epizyme Presents Preclinical Research Providing Deeper Understanding of Multiple Cancer Targets

First example of a peptide-bound structure for CARM1 provides insights for pathway targeting
First-in-class PRMT6 inhibitor demonstrates potency and selectivity –

Philadelphia, PA — Epizyme, Inc. (NASDAQ: EPZM), a clinical stage biopharmaceutical company creating novel epigenetic therapies for cancer patients, today announced the presentation of data on two epigenetic targets in its pioneering therapeutic pipeline. These data were presented this week at the American Association for Cancer Research (AACR) Annual Meeting in Philadelphia, Penn. Epizyme’s AACR 2015 posters will be posted at http://www.epizyme.com/media-center/publications/ after each one is presented at the meeting.

Epizyme presented a poster illustrating the first examples of structures of histone-derived peptides bound to CARM1 (also known as PRMT4), a histone methyltransferase implicated in a variety of solid tumors and hematologic malignancies. Additionally, Epizyme presented a second poster with data revealing a kinetic mechanism of CARM1 and its preference for methylating sites on peptide substrates.

Increased CARM1 expression has been observed in a number of cancers, making it a potential target for drug discovery efforts. CARM1 is known to methylate a number of histone and non-histone substrates. However, until now, no crystal structures of CARM1 with substrate peptides bound have been published, despite success in obtaining peptide complexes for other PRMTs. The insights generated from this research will be applied to the development of compounds that have the potential to specifically inhibit the activity of CARM1.

“At Epizyme, we are interested in understanding all aspects of the targets we are investigating, including function, mechanism and dynamics,” said Robert A. Copeland, Ph.D., President of Research and Chief Scientific Officer, Epizyme. “By applying this approach to CARM1, we have unlocked new information that brings us closer to understanding the best way to pursue CARM1 as a therapeutic target.”

On Wednesday, April 22, Epizyme will present data on the identification of an aryl pyrazole as the first small molecule PRMT6 inhibitor, created from the Company’s proprietary product platform. PRMT6 is a histone methyltransferase that is overexpressed in a variety of solid tumors, suggesting potential clinical utility for a small molecule inhibitor.

The compound detailed in the presentation demonstrates selectivity for PRMT6 over other PRMT family members and is suitable for use in in vitro and in vivo target validation research. These data will be presented in the session on Histone Deacetylase Inhibitors, Methyltransferase Inhibitors, and Other Targets.

“This new information on PRMT6 provides additional evidence of the productivity of Epizyme’s proprietary platform and opens the door for further exploration of several potentially interesting compounds for cancer therapy,” said Dr. Copeland

About Epizyme, Inc.

Epizyme, Inc. is a clinical stage biopharmaceutical company creating novel epigenetic therapeutics for cancer patients. Epizyme has built a proprietary product platform that the company uses to create small molecule inhibitors of a 96-member class of enzymes known as histone methyltransferases, or HMTs. HMTs are part of the system of gene regulation, referred to as epigenetics, that controls gene expression. Genetic alterations can result in changes to the activity of HMTs, making them oncogenic (cancer-causing). By focusing on the genetic drivers of cancers, Epizyme’s targeted science seeks to match the right medicines with the right patients.

Cautionary Note on Forward-Looking Statements

Any statements in this press release about future expectations, plans and prospects for Epizyme, Inc. and other statements containing the words “anticipate,” “believe,” “estimate,” “expect,” “intend,” “may,” “plan,” “predict,” “project,” “target,” “potential,” “will,” “would,” “could,” “should,” “continue,” and similar expressions, constitute forward-looking statements within the meaning of The Private Securities Litigation Reform Act of 1995. Actual results may differ materially from those indicated by such forward-looking statements as a result of various important factors, including: uncertainties inherent in the initiation of future clinical studies or expansion of ongoing clinical studies, availability and timing of data from ongoing clinical studies, expectations for regulatory approvals, development progress of the Company’s companion diagnostics, availability of funding sufficient for the Company’s foreseeable and unforeseeable operating expenses and capital expenditure requirements, other matters that could affect the availability or commercial potential of the Company’s therapeutic candidates or companion diagnostics and other factors discussed in the “Risk Factors” section of the Company’s Quarterly Report on Form 10-K filed with the Securities and Exchange Commission in March 2015. In addition, the forward-looking statements included in this press release represent the Company’s views as of the date hereof. The Company anticipates that subsequent events and developments will cause the Company’s views to change. However, while the Company may elect to update these forward-looking statements at some point in the future, the Company specifically disclaims any obligation to do so. These forward-looking statements should not be relied upon as representing the Company’s views as of any date subsequent to the date hereof.

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