Phase 1 development for epilepsy expected to
commence in 2017
Cerecor Inc. (NASDAQ: CERC), a clinical-stage biopharmaceutical
company developing treatments to make a difference in the lives of
patients with neurological and psychiatric disorders, today
announced that it has acquired exclusive, worldwide rights from Eli
Lilly and Company (“Lilly”) to develop and commercialize LY3130418
(now designated as CERC-611). CERC-611 is a potent and selective
Transmembrane AMPA Receptor Regulatory Proteins
(“TARP”)-γ8-dependent AMPA receptor antagonist. TARPs are a fairly
recently discovered family of proteins that have been found to
associate with and modulate the activity of AMPA receptors.
TARP-γ8-dependent AMPA receptors are localized primarily in the
hippocampus, a region of importance in complex partial seizures and
particularly relevant to seizure origination and/or propagation.
Research suggests that selectively targeting individual TARPs may
enable selective modulation of specific brain circuits without
globally affecting synaptic transmission which may lead to improved
efficacy, safety and tolerability. Cerecor expects to submit an
investigational new drug application (“IND”) to the United States
Food and Drug Administration (“FDA”) and, upon acceptance of the
IND by the FDA, commence Phase 1 development of CERC-611 in
2017.
CERC-611 was discovered and developed by Lilly for the treatment
of epilepsy, a neurological disorder affecting over 50 million
people worldwide. 150,000 new cases of epilepsy are diagnosed in
the United States annually, and 30%-40% of treated patients are
resistant to current pharmacotherapies, with only 8% of treated
patients being maintained seizure free. The disorder, if not
controlled, can lead to severe pathology and death. “There is a
significant unmet need for new mechanisms that provide a new
approach to treatment of epilepsy, with improved efficacy, safety,
tolerability and ease-of-use,” said Ron Marcus, M.D., Chief Medical
Officer and Head, Regulatory Affairs at Cerecor.
AMPA receptor antagonists are known anticonvulsant agents, and
their ability to down-modulate excitatory neurotransmission is key
to their antiepileptic therapeutic potential. However, since AMPA
receptor activity is so ubiquitous in the central nervous system
(“CNS”), a non-selective AMPA antagonist approach affects many
areas of the CNS, resulting in undesired effects, such as ataxia,
sedation, falls, and/or dizziness, which are shared by all known
general or broad-spectrum AMPA receptor antagonists. Typically, the
doses of these medications needed to obtain anti-convulsant
activity are close to, or overlap with, doses at which undesired
effects are observed. “Because of the predominant hippocampal
location of TARP-γ8-dependent AMPA receptors, we believe that the
efficacy and side effect profile of CERC-611 may represent an
improvement compared to current antiepileptics,” said Uli Hacksell,
Ph.D., Cerecor’s CEO, President and Chairman. “We are excited to
make CERC-611 a key addition to our pipeline and we expect to file
an IND and commence Phase 1 development in 2017."
Under the terms of the agreement, Cerecor will immediately
assume full development and commercialization responsibilities of
CERC-611. Lilly will receive an upfront licensing fee as well as
milestone and tiered royalty payments.
About CERC-611CERC-611 (formerly LY3130481) is a potent
and selective TARP-γ8-dependent AMPA receptor antagonist that we
believe is the first molecule to selectively target and
functionally block regionally-specific AMPA receptors after oral
dosing. This selectivity was engineered into CERC-611 using
structure-activity relationship information to achieve selective
blockade of the AMPA receptor regulator protein, or TARP-γ8 (high
density expression in hippocampus, a region of importance in
partial epilepsies), while sparing AMPA receptors thought to be
associated with TARP-γ2 (high density expression in cerebellum
regulating the ataxia and falling associated with broad spectrum
AMPA receptor antagonists). CERC-611 has been observed to have
positive preclinical activity in multiple models of epilepsy,
neuropathic pain, and depression.
About CerecorCerecor is a clinical-stage
biopharmaceutical company developing innovative drug candidates to
make a difference in the lives of patients with neurological and
psychiatric disorders. We are committed to the development of drugs
that improve lives by applying our extensive knowledge and
experience in central nervous system
disorders. Cerecor is currently pursuing the development
of two clinical Phase 2-stage product candidates: CERC-301 and
CERC-501.
CERC-301 is an oral, NR2B specific N-methyl-D-aspartate receptor
antagonist that is currently in a Phase 2 clinical trial as an
oral, rapidly acting adjunctive treatment for patients with severe
major depressive disorder (“MDD”) who are failing to achieve an
adequate response to their current antidepressant treatment. We
expect top-line data from this trial in November 2016. Cerecor
received fast track designation by the United States Food and Drug
Administration in 2013 for CERC-301 for the treatment of MDD. We
believe CERC-301 has the potential to be a first-in-class
medication that may significantly reduce depressive symptoms in a
matter of days.
CERC-501 is a potent and selective kappa opioid receptor
antagonist that is currently in a Phase 2 clinical trial for
smoking cessation that is expected to provide top-line data in
December 2016. In addition to Cerecor’s Phase 2 trial, three
externally-funded clinical trials are being conducted to evaluate
the use of CERC-501 in treating depressive symptoms, stress related
smoking relapse and cocaine addiction. One study is being conducted
under the auspices of the National Institute of Mental Health, the
second is a collaboration between Cerecor and Yale investigators
with funding from the National Institutes of Health and the third
is being conducted at Rockefeller University Hospital with funding
from a private foundation.
Cerecor has one preclinical stage asset, CERC-406, a brain
penetrant catechol-O-methyltransferase inhibitor with potential
procognitive activity.
For more information about the Company and its products, please
visit www.cerecor.com or contact Mariam E. Morris,
Chief Financial Officer, at (443) 304-8002.
Forward-Looking StatementsThis press release may include
forward-looking statements made pursuant to the Private Securities
Litigation Reform Act of 1995. Forward-looking statements are
statements that are not historical facts. Such forward-looking
statements are subject to significant risks and uncertainties that
are subject to change based on various factors (many of which are
beyond Cerecor’s control), which could cause actual results to
differ from the forward-looking statements. Such statements
include, without limitation, statements about the potential
efficacy, safety and tolerability of Cerecor’s product candidates
as well as their potential therapeutic benefits, the timing of the
expected IND submission and commencement of clinical development
for CERC-611, the timing of the availability of data from clinical
trials, and other statements with respect to Cerecor’s plans,
objectives, projections, expectations and intentions and other
statements identified by words such as “projects,” “may,” “will,”
“could,” “would,” “should,” “continue,” “seeks,” “aims,”
“predicts,” “believes,” “expects,” “anticipates,” “estimates,”
“intends,” “plans,” “potential” or similar expressions (including
their use in the negative), or by discussions of future matters
such as the development of product candidates or products,
potential benefits of product candidates, the expected timing of
data from clinical trials, technology enhancements and other
statements that are not historical. These statements are based upon
the current beliefs and expectations of Cerecor’s management but
are subject to significant risks and uncertainties, including those
detailed in Cerecor’s filings with the Securities and Exchange
Commission. Actual results may differ from those set forth in the
forward-looking statements. Except as required by applicable
law, Cerecor expressly disclaims any obligations or
undertaking to release publicly any updates or revisions to any
forward-looking statements contained herein to reflect any change
in Cerecor’s expectations with respect thereto or any change in
events, conditions or circumstances on which any statement is
based.
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version on businesswire.com: http://www.businesswire.com/news/home/20160926005275/en/
MacDougall Biomedical CommunicationsJoe Rayne,
781-235-3060ir@cerecor.com
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