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Constellation Pharmaceuticals Presentation Highlights Enhanced EZH2 Target Engagement, Leading to Second-Generation EZH2 Inhibitor CPI-0209

1075 Days ago

CAMBRIDGE, Mass., June 12, 2019 (GLOBE NEWSWIRE) -- Constellation Pharmaceuticals, Inc. (Nasdaq: CNST) today announced that Dr. Jacob Stuckey, Senior Scientist at Constellation Pharmaceuticals, gave an oral presentation titled Methods for Kinetic Assessment of High Affinity EZH2 Inhibitors: Identification of a 2nd Generation EZH2i with Improved Biological Activity and Extremely Long Residence Time at the Oxford Global Drug Discovery Summit in Berlin earlier today.

Dr. Stuckey described detailed studies conducted by Constellation Pharmaceuticals to characterize molecules from the Company’s second-generation EZH2 inhibitor program. As outlined in Dr. Stuckey’s presentation, potent EZH2 inhibitors present a number of unique challenges for measurement of biochemical potency and residence time. To meet these challenges, the Company developed customized biochemical and binding assays to evaluate these parameters. A key structural modification was identified that bestows prolonged residence time on multiple known EZH2-inhibitor scaffolds. Optimized second-generation EZH2 inhibitors display sub-pM potencies that translate into enhanced cell killing of EZH2-inhibitor-sensitive preclinical models both in vitro and in vivo.

The culmination of the Company’s second-generation EZH2 inhibitor program was the identification of CPI-0209, which reversibly binds to the PRC2 complex with sub-pM binding affinity and a residence time of >3 months. Constellation expects to file an Investigational New Drug (IND) application for CPI-0209 in June 2019.

About Constellation Pharmaceuticals

Constellation Pharmaceuticals is a clinical-stage biopharmaceutical company developing novel therapeutics that selectively modulate gene expression to address serious unmet medical needs in patients with cancer. The Company has a deep understanding of how epigenetic and chromatin modifications in cancer cells and in the tumor and immune microenvironment play a fundamental role in driving disease progression and drug resistance. Constellation is driving development of the EZH2 inhibitors CPI-1205 and CPI-0209 for the treatment of metastatic castration-resistant prostate cancer and other cancers as well as the BET inhibitor CPI-0610 for the treatment of myelofibrosis. The Company is also applying its broad research and development capabilities to explore other novel targets that directly and indirectly impact gene expression to fuel a sustainable pipeline of innovative small-molecule product candidates.

Forward-Looking Statements

This press release contains “forward-looking statements” within the meaning of the Private Securities Litigation Reform Act of 1995 that involve substantial risks and uncertainties, including statements regarding the Company’s plans and timelines for regulatory filings and the development status of the Company’s product candidates and their potential impact on disease modification. All statements, other than statements of historical facts, contained in this press release, including statements regarding the Company’s strategy, future operations, future financial position, prospects, plans and objectives of management, are forward-looking statements. The words “anticipate,” “believe,” “continue,” “could,” “estimate,” “expect,” “intend,” “may,” “plan,” “potential,” “predict,” “project,” “should,” “target,” “will,” “would” and similar expressions are intended to identify forward-looking statements, although not all forward-looking statements contain these identifying words. Any forward-looking statements are based on management’s current expectations of future events and are subject to a number of risks and uncertainties that could cause actual results to differ materially and adversely from those set forth in, or implied by, such forward-looking statements. These risks and uncertainties include, but are not limited to, risks associated with Constellation’s ability to: obtain and maintain necessary approvals from the FDA and other regulatory authorities; continue to advance its product candidates in clinical trials; advance the development of its product candidates under the timelines it anticipates, or at all; manage expenses; and raise the substantial additional capital needed to achieve its business objectives. For a discussion of other risks and uncertainties, any of which could cause the Company’s actual results to differ from those contained in the forward-looking statements, see the “Risk Factors” section, as well as discussions of potential risks, uncertainties, and other important factors, in the Company’s most recent filings with the Securities and Exchange Commission. In addition, the forward-looking statements included in this press release represent the Company’s views as of the date hereof and should not be relied upon as representing the Company’s views as of any date subsequent to 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. CPI-1205, CPI-0610, CPI-0209, and other product candidates are investigational in nature and have not yet been approved by the FDA or other regulatory authorities.


Ronald Aldridge
Senior Director, Investor Relations
Constellation Pharmaceuticals
+1 617-714-0539

Lauren Arnold
Media Relations
MacDougall Biomedical Communications
+1 781-235-3060

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