GENEVA--(Marketwire - Dec 20, 2012) - Addex Therapeutics /
Addex Scientists Discover and Characterize the First Potent and Selective
Small
Molecule Negative Allosteric Modulator Targeting mGlu7 receptor
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The issuer is solely responsible for the content of this announcement.
This is a significant breakthrough in the validation of this GPCR target
for the
potential treatment of major neurological indications such as PTSD and OCD
(ADXN: SIX), a leading company
pioneering allosteric modulation-based drug discovery and development,
announced
today the publication of new scientific findings in the Journal of
Pharmacology
and Experimental Therapeutics, describing the discovery and
characterization of
ADX71743, a novel, potent and selective negative allosteric modulator
(NAM) of
the metabotropic glutamate receptor 7 (mGlu7). (Kalinichev et al, 2012,
JPET
fast forward online publication December 21, 2012).
"The discovery and characterization of ADX71743 offers an important and
much
needed new approach to understanding the role of mGlu7 in the
underlying
pathophysiology of psychiatric and neurologic disorders" said Professor
Peter
Flor, one of the scientists who identified the mGlu7 receptor and a
pioneer in
the field of mGlu7 pharmacology.
mGlu7 is one of the most expressed receptors within the family of eight
mGlu
receptors, and is thought to play a central role in multiple CNS functions,
such
as emotional and stress reactivity, learning, memory and attention.
mGlu7 is
considered a promising novel target for potential treatment of a
variety of
disorders, including post-traumatic stress disorder (PTSD), obsessive
compulsive
disorder (OCD), anxiety, depression, drug abuse and schizophrenia.
Understanding
the role of the mGlu7 receptor has been hampered by the lack of
selective,
bioavailable and brain-penetrant pharmacological agents. This
publication
describes the full characterization of ADX71743, a novel potent and
selective
mGlu7 NAM, in both in vitro and in vivo studies. The compound was
active in
rodent models of anxiety and of OCD. Novel chemical series of mGlu7
NAMs are
currently being optimized to identify one or several compounds that Addex
plans
to advance into development.
Commenting on the data, Dr Robert Lütjens, Vice-President of
Biology and co-author of the publication explained that "the
identification of mGlu7 NAM
combined with our success in identifying mGlu7 positive allosteric
modulators
(PAM) provides us with a powerful advantage in elucidating the
importance of
mGlu7 in disease processes and the development of potential new
differentiated
therapeutics."
"This is yet another validation and demonstrates the power of our
innovative
allosteric modulator drug discovery platform to identify novel small
molecule
allosteric modulators of a receptor that was difficult to address
using
conventional small molecule approaches," commented Graham Dixon, CSO at
Addex.
Addex recently announced being awarded a grant of CHF700,000 from the
Swiss
Commission for Technology and Innovation (CTI) to develop allosteric
modulator
therapeutics for neurodegenerative and psychiatric diseases including
further
characterization of allosteric modulators against mGlu4 and mGlu7.
Addex Therapeutics (www.addextherapeutics.com) discovers and
develops an
emerging class of small molecule drugs, called allosteric modulators, which
have
the potential to be more specific and confer significant therapeutic
advantages
over conventional "orthosteric" small molecule or biological drugs. The
Company
uses its proprietary discovery platform to address receptors and other
proteins
that are recognized as attractive targets for modulation of important
diseases
with unmet medical needs. The Company's two lead products are being
investigated
in Phase 2 clinical testing: dipraglurant (ADX48621, an mGlu5
negative
allosteric modulator or NAM) is being developed by Addex to treat
Parkinson's
disease levodopa-induced dyskinesia (PD-LID); and ADX71149 (mGlu2
positive
allosteric modulator or PAM) is being developed in collaboration with
Janssen
Pharmaceuticals Inc. to treat schizophrenia and anxiety seen in
patients
suffering from major depressive disorder. Addex also is advancing
several
preclinical programs including: GABA-BR PAM for spasticity in MS, OAB and
other
disorders; mGlu4 PAM for Parkinson's, MS, anxiety and other
diseases. In
addition, Addex is applying its proprietary discovery platform to
identify
highly selective and potent allosteric modulators of a number of both
GPCR and
non-GPCR targets that are implicated in diseases of significant unmet
medical
need.
Disclaimer: The foregoing release may contain forward-looking statements
that
can be identified by terminology such as "not approvable",
"continue",
"believes", "believe", "will", "remained open to exploring", "would",
"could",
or similar expressions, or by express or implied discussions regarding
Addex
Therapeutics, formerly known as, Addex Pharmaceuticals, its
business, the
potential approval of its products by regulatory authorities, or
regarding
potential future revenues from such products. Such forward-looking
statements
reflect the current views of Addex Therapeutics regarding future events,
future
economic performance or prospects, and, by their very nature, involve
inherent
risks and uncertainties, both general and specific, whether known or
unknown,
and/or any other factor that may materially differ from the plans,
objectives,
expectations, estimates and intentions expressed or implied in
such forward-looking statements. Such may in particular cause actual
results with allosteric
modulators of mGlu2, mGlu4, mGlu5, GABA-BR or other therapeutic targets
to be
materially different from any future results, performance or
achievements
expressed or implied by such statements. There can be no guarantee
that
allosteric modulators of mGlu2, mGlu4, mGlu5, GABA-BR or other
therapeutics
targets will be approved for sale in any market or by any regulatory
authority.
Nor can there be any guarantee that allosteric modulators of mGlu2,
mGlu4,
mGlu5, GABA-BR or other therapeutic targets will achieve any particular
levels
of revenue (if any) in the future. In particular, management's
expectations
regarding allosteric modulators of mGlu2, mGlu4, mGlu5, GABA-BR or
other
therapeutic targets could be affected by, among other things, unexpected
actions
by our partners, unexpected regulatory actions or delays or
government
regulation generally; unexpected clinical trial results, including
unexpected
new clinical data and unexpected additional analysis of existing clinical
data;
competition in general; government, industry and general public
pricing
pressures; the company's ability to obtain or maintain patent or
other
proprietary intellectual property protection. Should one or more of these
risks
or uncertainties materialize, or should underlying assumptions prove
incorrect,
actual results may vary materially from those anticipated, believed,
estimated
or expected. Addex Therapeutics is providing the information in this
press
release as of this date and does not undertake any obligation to
update any
forward-looking statements contained in this press release as a result
of new
information, future events or otherwise, except as may be required by
applicable
laws.
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Source: Addex Therapeutics via Thomson Reuters ONE
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