This Day On The Street
Continue to site right-arrow
This account is pending registration confirmation. Please click on the link within the confirmation email previously sent you to complete registration.
Need a new registration confirmation email? Click here
TheStreet Open House

Epizyme, Inc. Publishes Data Demonstrating EPZ-5676 As Potent, Selective Inhibitor Of DOT1L For Genetically Defined Acute Leukemias

CAMBRIDGE, Mass., June 26, 2013 /PRNewswire/ --  Epizyme, Inc., (NASDAQ: EPZM) a clinical stage biopharmaceutical company creating innovative personalized therapeutics for patients with genetically defined cancers, announced today the publication of data on the company's clinical candidate EPZ-5676, a potent and selective small-molecule inhibitor of DOT1L, a histone methyltransferase (HMT). DOT1L is implicated in acute leukemias in which the MLL gene is rearranged (MLL-r) . This research, published in the journal Blood, provides a detailed preclinical characterization of EPZ-5676, which Epizyme is developing for the treatment of MLL-r leukemia. The paper expands on data reported by the same authors in a poster at the December 2012 American Society of Hematology (ASH) annual meeting.  

Key results presented in this paper include:

- detailed characterization of the correlation between DOT1L inhibition, methylation of the DOT1L target (H3K79), reversal of leukemogenic gene expression and anti-proliferative effects specific to MLL-r leukemia

- sustained tumor growth inhibition in animal models of MLL-r leukemia, including durable effects after drug dosing is discontinued

- development of a quantitative PK/PD relationship

- development of an assay to assess methylation of H3K79 status in non-invasive, surrogate tissues such as bone marrow and peripheral blood mononuclear cells

"This paper provides a clear and comprehensive description of the preclinical characterization of EPZ-5676 that paved the way for this drug becoming the first HMT inhibitor to our knowledge to enter human clinical trials. The work is illustrative of the discovery efforts ongoing at Epizyme that are fueling the clinical development of multiple drugs against the HMT target class," said Robert A. Copeland, Ph.D., Executive Vice President and Chief Scientific Officer of Epizyme.

The paper titled, "Potent Inhibition of DOT1L as Treatment for MLL-Fusion Leukemia," was authored by Roy M. Pollock, Scott R. Daigle, Edward J. Olhava and colleagues at Epizyme, and is available online here.

About EPZ-5676

Epizyme initiated a Phase I study in September 2012 to evaluate the safety, pharmacokinetics and pharmacodynamics of escalating doses of EPZ-5676. An expansion cohort of patients with genetically defined MLL-r leukemia is anticipated in the second half of 2013. Epizyme retains all U.S. rights to EPZ-5676 and has granted Celgene an exclusive license to EPZ-5676 outside of the United States. In partnership with Abbott, Epizyme is developing a companion diagnostic for this program.

About Mixed Lineage Leukemia (MLL-r)

MLL-r leukemia is an aggressive subtype of two of the most common forms of acute leukemia, acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL), and is caused by a chromosomal translocation involving the MLL gene. Based on published research, the five-year overall survival rate for adult patients with the MLL-r subtype of AML ranges from approximately 5 to 24 percent. MLL-r also occurs in an infant/pediatric population, which has a similarly poor prognosis. At this time, there are no approved therapies specifically indicated for MLL-r leukemia.

1 of 2

Check Out Our Best Services for Investors

Action Alerts PLUS

Portfolio Manager Jim Cramer and Director of Research Jack Mohr reveal their investment tactics while giving advanced notice before every trade.

Product Features:
  • $2.5+ million portfolio
  • Large-cap and dividend focus
  • Intraday trade alerts from Cramer
Quant Ratings

Access the tool that DOMINATES the Russell 2000 and the S&P 500.

Product Features:
  • Buy, hold, or sell recommendations for over 4,300 stocks
  • Unlimited research reports on your favorite stocks
  • A custom stock screener
Stocks Under $10

David Peltier uncovers low dollar stocks with serious upside potential that are flying under Wall Street's radar.

Product Features:
  • Model portfolio
  • Stocks trading below $10
  • Intraday trade alerts
14-Days Free
Try it NOW
Only $9.95
Try it NOW
14-Days Free
Try it NOW

Check Out Our Best Services for Investors

Dividend Stock Advisor

David Peltier identifies the best of breed dividend stocks that will pay a reliable AND significant income stream.

Product Features:
  • Diversified model portfolio of dividend stocks
  • Updates with exact steps to take - BUY, HOLD, SELL
Trifecta Stocks

Every recommendation goes through 3 layers of intense scrutiny—quantitative, fundamental and technical analysis—to maximize profit potential and minimize risk.

Product Features:
  • Model Portfolio
  • Intra Day Trade alerts
  • Access to Quant Ratings
Options Profits

Our options trading pros provide over 100 monthly option trading ideas and strategies to help you become a well-seasoned trader.

Product Features:
  • Actionable options commentary and news
  • Real-time trading community
Try it NOW
Try it NOW
Try it NOW
To begin commenting right away, you can log in below using your Disqus, Facebook, Twitter, OpenID or Yahoo login credentials. Alternatively, you can post a comment as a "guest" just by entering an email address. Your use of the commenting tool is subject to multiple terms of service/use and privacy policies - see here for more details.
Submit an article to us!


DOW 17,712.66 +34.43 0.19%
S&P 500 2,061.02 +4.87 0.24%
NASDAQ 4,891.2190 +27.8570 0.57%

Partners Compare Online Brokers

Free Reports

Free Newsletters from TheStreet

My Subscriptions:

After the Bell

Before the Bell

Booyah! Newsletter

Midday Bell

TheStreet Top 10 Stories

Winners & Losers

Register for Newsletters
Top Rated Stocks Top Rated Funds Top Rated ETFs