Addex Announces Issuance of a Broad European Composition of Matter Patent for Dipraglurant
Addex Therapeutics /
Addex Announces Issuance of a Broad European Composition of Matter Patent for
Dipraglurant
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The issuer is solely responsible for the content of this announcement.
Dipraglurant, an mGlu5 negative allosteric modulator, in clinical development
for levodopa-induced dyskinesia as well as certain rare dystonias
Geneva, Switzerland, 22 April 2013 - Addex Therapeutics (SIX:ADXN), a leading
company pioneering allosteric modulation-based drug discovery and development,
announced that the European Patent Office granted Addex a broad composition of
matter patent (European patent, EP 1 765 795) covering dipraglurant and other
mGlu5 negative allosteric modulators (NAM). Dipraglurant is currently in
development for the treatment of levodopa-induced dyskinesia in Parkinson's
disease patients as well as rare forms of dystonia.
"The granting of this patent continues to broaden the patent estate around our
lead program," said Bharatt Chowrira, Ph.D., CEO at Addex. "Specifically,
composition of matter patents have now been granted for dipraglurant in all the
major markets - the United States, Europe and Japan. Â Â Our intellectual property
estate continues to yield key patents protecting novel oral small molecules
discovered utilizing our industry leading allosteric modulation technology
platform. This new patent significantly enhances the value of our dipraglurant
franchise and we look forward to advancing dipraglurant into Phase 2 for the
treatment of certain rare dystonias in the coming months."
About Dipraglurant
Dipraglurant is an oral, small molecule allosteric modulator that inhibits
selectively the metabotropic glutamate receptor 5 (mGlu5), a Class C G-Protein
Coupled Receptor (GPCR), with potential to be used in combination with levodopa
or dopamine agonists or as a standalone treatment for Parkinson's disease
levodopa-induced dyskinesia (PD-LID), motor and non-motor symptoms of
Parkinson's disease and other movement disorders. Data from a recent Phase 2a
show that dipraglurant met the primary objective of the study by exhibiting a
good safety and tolerability profile. Dipraglurant also demonstrated a
statistically significant reduction in LID severity with both 50 and 100 mg
doses. Dipraglurant appears to reduce dystonia severity in addition to chorea,
the two major LID components. In a double-blind, placebo-controlled study
conducted in the US and Europe, the primary objective was to demonstrate safety
and tolerability in PD-LID patients. In addition, the trial was designed to
evaluate exploratory efficacy as a secondary objective. Efficacy was measured
using the modified Abnormal Involuntary Movement Scale (mAIMS), patient diaries
documenting "off-time" (impaired voluntary movement), "on-time" (with or without
dyskinesia) and sleep. Additional endpoints include the Unified Parkinson's
Disease Rating Scale (UPDRS), the Clinician & Patient Global Impression of
Change (CGIC & PGIC), and an evaluation of the patients' mood using the Hospital
Anxiety & Depression Score. The trial was supported by a grant from The Michael
J. Fox Foundation for Parkinson's Research.
About mGlu5 Inhibition
There is an increasing body of evidence that mGlu5 inhibition may be a valuable
new strategy for treating a number of important diseases and conditions, such as
Parkinson's disease, Parkinson's disease levodopa-induced dyskinesia (PD-LID),
dystonia, anxiety, depression, pain, tardive dyskinesia, addiction, autism and
Fragile X syndrome. With regards to Parkinson's disease, recent clinical and
preclinical evidence suggest that mGlu5 inhibition may have an effect on
parkinsonian motor symptoms as well as dyskinesia. mGlu5 is found in regions of
the brain considered to be key control points in the neuronal movement circuits
affected by abnormal signaling by the neurotransmitter glutamate in Parkinson's
disease. Perturbations in glutamate signaling (along with disruptions in
dopaminergic signaling) are believed to be an underlying cause of movement
disorders like Parkinson's disease and dystonia. As such, inhibiting mGlu5 could
act to re-establish normal movement via a non-dopaminergic mechanism.
Separately, preclinical findings also suggest that mGlu5 inhibitors may be
neuroprotective and may, therefore, hold potential as disease modifying agents
that can slow or prevent progression of Parkinson's and other neurological
diseases.
About Dystonia
Dystonia is a movement disorder that causes the muscles to contract and spasm
involuntarily, according to the Dystonia Medical Research Foundation. The
involuntary muscle contractions force the body into repetitive and often
twisting movements as well as awkward, irregular postures. There are over 20
forms of dystonia, and dozens of diseases and conditions include dystonia as a
major symptom. Dystonia may affect a single body area or be generalized
throughout multiple muscle groups. Dystonia affects men, women, and children of
all ages and backgrounds. Estimates suggest that no less than 300,000 people in
North America are affected. Dystonia causes varying degrees of disability and
pain, from mild to severe. There is presently no cure, and, although many drugs
are utilized to try to treat dystonia, the leading treatment is botulinum toxin
injections and many patients are left with inadequate efficacy. Patients also
resort to invasive, risky and expensive procedures such as deep brain
stimulation to treat dystonia. Dipraglurant has been shown to effectively
reduce dystonia in both a clinical study and preclinical models of Parkinson's
disease levodopa-induced dyskinesia (PD-LID). The neurophysiology of different
forms of dystonia is thought to be similar and recent preclinical data in
dystonia - suggesting that dipraglurant may also work for non-parkinsonian forms
of dystonia. Addex plans to initiate Phase 2 pilot studies in certain rare forms
of dystonia in the first half of 2013 with the results expected towards the end
of 2013.
About Addex Therapeutics
Addex Therapeutics (www.addextherapeutics.com) is a development stage company
focused on advancing innovative oral small molecules against rare diseases
utilizing its pioneering allosteric modulation-based drug discovery platform.
The Company's two lead products are being investigated in Phase 2 clinical
testing: dipraglurant (dipraglurant, an mGlu5 negative allosteric modulator or
NAM) is being developed by Addex to treat Parkinson's disease levodopa-induced
dyskinesia (PD-LID) and rare forms of dystonia; and ADX71149 (mGlu2 positive
allosteric modulator or PAM) is being developed in collaboration with Janssen
Pharmaceuticals, Inc. to treat both schizophrenia and anxiety as seen in
patients suffering from major depressive disorder. Addex is also advancing
several preclinical programs including: GABA-BR positive allosteric modulator
(PAM) for Charcot-Marie-Tooth (type 1a) disease, spasticity in patients with
multiple sclerosis (MS), pain, overactive bladder and other disorders; and mGlu4
PAM for MS, Parkinson's disease, anxiety and other diseases. Allosteric
modulators are an emerging class of small molecule drugs 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 target receptors and other proteins that
are recognized as essential for the therapeutic modulation of important diseases
with unmet medical needs.
Tim Dyer
Chief Financial Officer
Addex Therapeutics
+41 22 884 15 61
PR@addextherapeutics.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
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
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