News Release

Constellation Pharmaceuticals Advances CPI-0209 into Clinical Trials, Expanding its EZH2 Franchise

September 24, 2019 at 7:00 AM EDT
Potential best-in-class EZH2 inhibitor focused on targeted patient segments was identified using Constellation’s epigenetics platform

CAMBRIDGE, Mass., Sept. 24, 2019 (GLOBE NEWSWIRE) -- Constellation Pharmaceuticals, Inc. (Nasdaq: CNST), a clinical-stage biopharmaceutical company using its expertise in epigenetics to discover and develop novel therapeutics, today announced that the Company has dosed the first patient in a Phase 1/2 clinical trial of CPI-0209.

CPI-0209 is a second-generation EZH2 inhibitor that has been designed to achieve comprehensive target coverage through extended on-target residence time and enhanced potency compared with first-generation EZH2 inhibitors. These features lead to faster onset of action than first-generation EZH2 inhibitors as well as robust anti-tumor activity in models of multiple cancer types. 

“We recognized that a best-in-class molecule with enhanced potency and residence time may help to access the full potential of EZH2 inhibition in cancer,” said Dr. Patrick Trojer, Chief Scientific Officer. “We believe that CPI-0209 can deliver on this need, and we are eager to learn more about CPI-0209 in the clinic. We have seen impressive pre-clinical activity of CPI-0209 and are excited to take the first steps toward bringing CPI-0209 to patients.”

Constellation has utilized its epigenetics platform, including expertise in translational science, to identify novel, targeted patient contexts that may be responsive to inhibition by next-generation EZH2 inhibitors. For instance, in xenografts derived from bladder cell lines harboring ARID1A mutations, once-daily treatment with CPI-0209 achieved regression at well-tolerated doses – activity that was superior to that from the chemotherapeutic agent cisplatin, a standard of care in bladder cancer. At the American Association for Cancer Research Bladder Cancer meeting on May 19, 2019, Constellation presented a poster with supporting data from these studies. 

The Phase 1 dose escalation phase of the clinical trial will study CPI-0209 monotherapy in advanced, relapsed solid tumor patients. After determining the recommended Phase 2 dose (RP2D) for the monotherapy, we will pursue expansion arms in selected tumor indications as well as combination therapy development, employing a biomarker strategy that includes assessment of ARID1A.

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 implications of preclinical data and the development status of, and development plans and timelines for, the Company’s product candidates. 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; whether preliminary or interim results from preclinical studies or a clinical trial will be predictive of the final results of a clinical trial; advance the development of its product candidates under the timelines it anticipates, or at all, in current and future clinical trials; obtain, maintain or protect intellectual property rights related to its product candidates; 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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Source: Constellation Pharmaceuticals