Addex Validates Potential Efficacy Biomarker for Phase 1 Trial of its GABA-B Positive Allosteric modulator, ADX71441
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Addex Therapeutics /
Addex Validates Potential Efficacy Biomarker for Phase 1 Trial of its GABA-B
Positive Allosteric modulator, ADX71441
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The issuer is solely responsible for the content of this announcement.
· ADX71441 produced dose-dependent changes on growth hormone (GH) plasma
concentrations in a preclinical model
· The data confirms the role of gamma-aminobutyric acid (GABA) in
modulating GH plasma concentrations previously reported in humans and animals
· GH plasma concentrations occurred at doses and plasma concentrations
of ADX71441 which have been demonstrated to induce pharmacological and
efficacious effects in preclinical models of CMT1A, anxiety, pain, overactive
bladder and alcohol addiction
· ADX71441 on track to initiate Phase 1 testing in H1 2013
Geneva, Switzerland, 21 May 2013 - Addex Therapeutics (SIX: ADXN), a leading
company pioneering allosteric modulation-based drug discovery and development,
announced today that its gamma-aminobutyric acid B (GABA-B) receptor positive
allosteric modulator, ADX71441, caused dose dependent changes in growth hormone
(GH) plasma concentrations compared to vehicle control in a rodent preclinical
model. These data are consistent with published scientific literature
demonstrating that GABA, the endogenous neurotransmitter for GABA-B receptors,
plays both a stimulatory and inhibitory role in modulating the neuro-endocrine
regulation of GH secretion in both animals and humans. GH plasma concentration
changes occurred at doses and plasma concentrations of ADX71441 which have been
demonstrated to induce pharmacological and efficacious effects in preclinical
models of CMT1A, anxiety, pain, overactive bladder and alcohol addiction.
"The data obtained with ADX71441 demonstrate that growth hormone can be used as
a potential biomarker for an efficacy signal and fully supports its inclusion in
our first-in-man program," stated Graham Dixon, Ph.D., CSO at Addex. "The use
of growth hormone as a biomarker in the Phase 1 will allow us to obtain early
information about target engagement, guide dose selection for further clinical
development and possibly provide us an understanding of the therapeutic
potential of ADX71441."
The study was performed on samples from single oral treatment studies where
ADX71441 was given at doses of 5, 20 and 80 mg/kg. Assessment of GH and ADX71441
plasma concentrations were performed at 4 and 24 hours post-treatment. The
results demonstrate a direct relationship between plasma concentrations of
ADX71441 and effect on GH levels. GH changes occur at doses (<10 mg/kg) and
plasma concentrations (between 300 and 600 ng/mL) that have been shown to induce
pharmacological and efficacious effects in several preclinical models, including
CMT1A, anxiety, pain, overactive bladder and alcohol addiction.
About ADX71441 and GABAB Activation
ADX71441 is a potent, selective, orally available small molecule that is brain
penetrant and shows good pharmacokinetic properties for once-daily dosing.
Activation of gamma-aminobutyric acid subtype B (GABA-B) receptor, a Family C
class of GPCR, is clinically and commercially validated. Generic GABA-B
receptor agonist, baclofen, is marketed for spasticity and some spinal cord
injuries, and used for overactive bladder (OAB), but is not commonly used due to
severe side effects of the drug and rapid clearance. Orthosteric GABA-B
receptor agonists have also shown clinical validation in gastroesophageal reflux
disease (GERD). Addex' GABA-B receptor PAMs have shown efficacy in multiple
preclinical models including: CMT1a, OAB, pain, osteoarthritis pain and anxiety.
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(at)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, potential
efficacy or clinical promise of its products, 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, 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 factors
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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(ii) they are solely responsible for the content, accuracy and
originality of the information contained therein.
Source: Addex Therapeutics via Thomson Reuters ONE
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Datum: 21.05.2013 - 07:30 Uhr
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News-ID 261754
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