Constellation Pharmaceuticals Presentation Highlights Enhanced EZH2 Target Engagement, Leading to Second-Generation EZH2 Inhi...
12 Juin 2019 - 3:00PM
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.
Contact
Ronald AldridgeSenior Director, Investor
RelationsConstellation Pharmaceuticals+1
617-714-0539ron.aldridge@constellationpharma.com
Lauren ArnoldMedia RelationsMacDougall Biomedical
Communications+1 781-235-3060larnold@macbiocom.com
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