Addex R&D Day Highlights Broadened Therapeutic Potential of
Allosteric Modulation Platform to Include Cytokine Receptors as well
as GPCRs
Webcast at www.addexpharma.com from 11am CEST to 3:30 pm CEST
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Geneva, Switzerland, 16 July 2009 - At its R&D Day today, allosteric
modulation company Addex Pharmaceuticals (SIX:ADXN) will disclose for
the first time the successful adaptation of its innovative and
proprietary allosteric modulator platform beyond G-protein coupled
receptors (GPCR) targets to include discovery of orally active, small
molecule drugs targeting type I transmembrane proteins, including
cytokine receptors. GPCR and cytokine receptors are among the most
important therapeutic targets, with many drugs against these types of
receptors on the market or in development. Addex also will provide a
status report on all of its clinical and earlier stage programs.
"In addition to expanding our efforts beyond the mGluRs to include
some equally challenging GPCR targets, like the A2A receptor and the
Orexin 2 receptor, we have successfully adapted our proprietary
screening platform to include receptor targets like TNF-R1, IL-1R1,
GIPR and GLP-1R that have previously only been addressed by protein
or peptide therapeutics," said Vincent Mutel, CEO of Addex. "We
believe allosteric modulators will provide drug makers a bridge
traversing the gap between classical small molecule drugs and protein
therapeutics, offering potential for a totally new kind of highly
differentiated therapeutic class. We intend to leverage of our
first-mover advantage in developing tools to discover this new class
of small molecule drugs in order to retain important intellectual
property and forge exciting new partnerships."
Proprietary Discovery Platform Progress
Addex has executed on its plan announced at the April 2008 R&D Day to
organize itself into three business units (CNS, Inflammation and
Metabolic Disorders), supported by Core Biology and Core Chemistry
teams for discovery and medicinal chemistry. As programs progress,
non-clinical and clinical development teams are charged with
developing projects coming out of discovery. This structure allows
for efficient use of resources and has enabled broadening the scope
of the platform into new therapeutic targets while reducing the need
to spread highly specialized proprietary tools and expertise across
multiple departments.
Addex' Core Biology in collaboration with researchers in the
Inflammation Business Unit have developed new proprietary discovery
tools to identify negative allosteric modulators of Tumor Necrosis
Factor-Receptor 1 (TNF-R1), an important therapeutic target in
rheumatoid arthritis (RA) and other inflammatory diseases. The first
screening has been completed and primary hits have been identified.
To date, successful targeting of TNF has only been achieved using
large molecule biological drugs, or so called protein therapeutics,
which need to be injected and have a high cost of goods compared to
orally available small molecule drugs.
The same interdisciplinary team has adapted this proprietary
technology to identify adenosine 2A receptor (A2AR) positive
allosteric modulators (PAM). The first screening has been completed
and primary hits have been identified. The same tools are now being
adapted to screen the interleukin-1 receptor 1 (IL-1R1). TNF-R1 NAM,
A2AR PAM and IL-1R1 NAM programs have potential for the treatment of
RA and other inflammatory diseases like psoriasis, osteoarthritis,
gout and even Alzheimer's disease or Type II diabetes.
Similarly, Core Biology, working with the Metabolic Disorders Unit,
have used Addex' proprietary tools to discover Gastric Inhibitory
Polypeptide Receptor (GIPR) allosteric agonist and continue
optimization of glucagon-like peptide 1 receptor (GLP-1R) PAM. Both
programs have potential to treat Type II Diabetes.
"We believe these carefully tailored proprietary screening assays,
together with our unique growing allostery biased library, will
enable us to continue to target a broad range of well validated
important therapeutic targets that were not previously accessible to
small molecule chemistry," said CEO Vincent Mutel.
With the CNS Business unit, Addex' proprietary assays have been
adapted for screening of Orexin-2 receptor NAM, which has potential
for the treatment of sleep disorders. The first screening has been
completed and primary hits have been identified. In addition, the
optimization of metabotropic glutamate receptor 4 (mGluR4) PAM (part
of a collaboration with Merck & Co., Inc. to develop drugs for
Parkinson's disease and undisclosed indications) continues to move
forward; last week Addex announced that mGluR4 PAM showed activity as
a non-dopaminergic drug after oral administration in an animal model
of PD, thereby achieving a second preclinical milestone. The CNS
Business Unit also has progressed optimization of its mGluR2 NAM,
with potential for cognitive deficits in Alzheimer's disease and for
depression as well as mGluR7 NAM, which have potential for treatment
of depression and post-traumatic-stress disorder.
Significant progress has been made in studying ADX68692, a follicle
stimulating hormone (FSH) NAM. New data to be presented today suggest
that the product might be suited for treatment of hormone refractory
prostate cancer. In vivo proof of concept studies for hormone
refractory prostate cancer will continue, while development of
ADX68692 in other indications, such as contraception and osteoporosis
will be put on hold.
Previously undisclosed projects for obesity and migraine have also
been put on hold to prioritize other programs. Addex has terminated
development of its Adenosine A3 antagonist for glaucoma but continues
to make the product available for out-licensing.
Clinical Programs
Enrollment in the three Phase IIb trials of ADX10059 in both GERD and
migraine prevention is proceeding as planned. The data from the two
GERD studies are expected in the fourth quarter of 2009. The data
from the migraine prevention study are expected in the first half of
2010.
Preclinical data, disclosed for the first time today, show that both
ADX10059 and ADX48621 reversed haloperidol induced catalepsy in a
rodent model of Parkinson's disease (PD). Data from ongoing studies
in a primate monkey model of PD are expected in the coming months.
ADX10059 and ADX48621 are mGluR5 NAM. ADX48621 completed Phase I
testing in healthy volunteers earlier this year and is scheduled to
start Phase IIa testing in PD patients before the end of 2009.
Addex partner, Ortho-McNeil-Janssen Pharmaceuticals Inc., a Johnson &
Johnson company, started last month Phase I testing of ADX71149, an
mGluR2 PAM with potential for treatment of schizophrenia and anxiety.
R&D Day webcasts
The live webcasts, slides and recorded webcasts will be available via
www.addexpharma.com.
The webcast program is as follows (times are Central European Summer
Time):
11:00 Overview (Vincent Mutel, Chief Executive
Officer)
11:30 Allostery Platform: Chemistry (Jean-Philippe
Rocher, Head of Core Chemistry)
12:00 Allostery Platform: Biology (Robert Lütjens,
Head of Core Biology)
12:30 Inflammation Business Unit (Laurent Galibert,
Head of Inflammation)
13:00 Lunch Break
13:30 Metabolic Disease Business Unit (Vincent Mutel,
CEO & acting Head of Metabolic Disorders)
14:00 CNS Business Unit (Emmanuel Le Poul, Head of
CNS)
14:30 Non-clinical Development (Sonia Poli, Head of
Non-Clinical Development)
15:00 Clinical Development (Charlotte Keywood, Chief
Medical Officer)
15:30 Conclusion (Vincent Mutel, Chief Executive
Officer)
Questions will be invited during each presentation. Webcast viewers
also will be able to ask questions, at any time, using an instant
messenger located in the webcast browser window. Recordings and
slides will be made available via www.addexpharma.com.
Addex Pharmaceuticals (www.addexpharma.com) discovers and develops
allosteric modulators for human health. Allosteric modulators are a
different kind of orally available small molecule therapeutic agent,
which we believe will offer a competitive advantage over classical
drugs. Our lead allosteric modulator product, ADX10059, has achieved
clinical proof of concept and is in Phase IIb testing for the
treatment of GERD and, separately, migraine headache. Both are
important diseases for which existing products with limited efficacy
have established multi-billion dollar markets despite sub-optimal
efficacy. ADX10059 is a first-in-class mGluR5 inhibitor, a
therapeutic strategy that also is being pursued in multiple
indications by large pharma competitors.
Our products and technology already have proven their value through
our relationships with four of the top 10 pharmaceutical companies in
the world. Specifically, under an agreement with Ortho-McNeil-Janssen
Inc., a Johnson & Johnson company, ADX71149, a positive allosteric
modulator (PAM) of mGluR2, is undergoing Phase I clinical testing and
has potential for treatment of schizophrenia and anxiety. Under two
separate agreements with Merck & Co., Inc., we are developing PAMs of
mGluR4 and mGluR5 as drugs to treat Parkinson's disease and
schizophrenia, respectively. In addition, GlaxoSmithKline and Roche
have made equity investments in Addex.
Chris Maggos
Head of IR & Communications
Addex Pharmaceuticals
+41 22 884 15 11
chris.maggos@addexpharma.com
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 Pharmaceuticals Ltd,
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 Pharmaceuticals Ltd 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 mGluR2, mGluR4,
mGluR5, mGluR7 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 mGluR2, mGluR4, mGluR5, mGluR7 will be
approved for sale in any market or by any regulatory authority. Nor
can there be any guarantee that allosteric modulators of mGluR2,
mGluR4, mGluR5, mGluR7 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 mGluR2,
mGluR4, mGluR5, mGluR7 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 Pharmaceuticals Ltd 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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