Addex to Present Progress on Multiple Allosteric Modulator Programs for Neurodegenerative and other Neurological Disorders
Six Presentations at the 7th International Meeting on Metabotropic Glutamate Receptors
Geneva, Switzerland, October 3, 2011 – Addex Pharmaceuticals (SIX:ADXN), a leading biopharmaceutical company pioneering allosteric modulation-based drug discovery and development, announced today that its scientists will present data on multiple metabotropic glutamate receptor (mGluR) allosteric modulator programs, including small molecule modulators of mGluR subtypes 2, 4, 5 and 7. Held every three years, the prestigious International Meeting on Metabotropic Glutamate Receptors, in Italy, brings together the world’s leading researchers in this field.
“These six presentations represent our continued success in addressing the elusive mGluR targets and re-affirm our leadership position in addressing important previously undruggable targets with oral small molecule allosteric modulators,” said Bharatt Chowrira, CEO of Addex. “Our advances in this field are further illustrated by two lead products targeting mGluR5 and mGluR2, dipraglurant-IR for Parkinson’s disease levodopa-induced dyskinesia (PD-LID) and ADX71149 for schizophrenia, respectively; both are currently in mid-stage clinical testing and each has the potential to be first-in-class and best-in-class in treating these serious neurological disorders.”
Dipraglurant-IR, is an mGluR5 negative allosteric modulator, or NAM, which is in Phase IIa testing for PD-LID. Top-line data are expected to be reported in the first half of 2012. Addex partner Janssen Pharmaceuticals Inc. is developing ADX71149, an mGluR2 positive allosteric modulator, or PAM, currently in Phase IIa testing for the treatment of schizophrenia.
Glutamate, like dopamine and serotonin, is one of the major neurotransmitters in the brain and other parts of the central nervous system. Because of their importance, each of the many glutamate-specific receptors, including all eight subtypes of mGluRs, has been the subject of intense research and drug discovery efforts for more than 20 years. But, despite ever increasing knowledge about their role in various neurologic disorders, the industry has struggled to identify compounds that can selectively differentiate between the various glutamate receptor subtypes using conventional small molecule discovery techniques. In contrast, allosteric modulators have achieved excellent selectivity for each mGluR subtype. This is because the allosteric binding sites are less conserved compared to the receptor’s active site, which is the binding site for the body’s natural activators (i.e. endogenous ligands) and conventional small molecule drugs.
“At Addex, we have developed a proprietary allostery-biased library and highly sensitive HTS screening systems tailored for discovery of selective and potent allosteric modulators. In short, by industrializing the process of discovering allosteric modulators, we are addressing an important bottleneck in small molecule drug discovery that has hindered drug developers for decades and has resulted in a growing number of undruggable validated targets,” said Dr. Sonia Poli, Head of CNS and Non-Clinical Development at Addex. “We believe these orally bioavailable small molecules are able to exert exquisite selectivity at the receptor subtype level and have the potential to be optimized into drugs with the fine-tuned control needed to address major CNS disorders such as schizophrenia, Parkinson’s and Alzheimer’s diseases, as well as non-CNS indications.”
Thursday, October 6, 4.30 – 4.55 pm Request presentation
Selective mGluR2 negative allosteric modulators for the treatment of cognitive deficits associated with Alzheimer’s disease
Friday, October 7, 10.05 – 10.30 am Request presentation
Anti-parkinsonian and anti-dyskinetic effects of dipraglurant (ADX48621), a novel mGluR5 negative allosteric modulator in clinical development
Friday, October 7, 1.25 – 1.50 pm Request presentation
Novel metabotropic glutamate receptor 4 (mGluR4) allosteric potentiators for the treatment of Parkinson’s disease and anxiety
Wednesday, October 5 from 20.00 to 23.00 in the Pharmacology session
Discovery and characterization of novel metabotropic glutamate receptor 4 (mGluR4) allosteric potentiators
Wednesday, October 5 from 20.00 to 23.00 in the Pharmacology session
Identification, synthesis and SAR investigation of a series of novel metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators
Wednesday, October 5 from 20.00 to 23.00 in the Psychiatric Disorders session
Development of novel metabotropic glutamate receptor 7 (mGluR7) negative allosteric modulators for treatment of anxiety disorders
Addex Pharmaceuticals 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 IIa clinical testing: dipraglurant (ADX48621, an mGluR5 negative allosteric modulator or NAM) is being developed by Addex to treat Parkinson’s disease levodopa-induced dyskinesia (PD-LID); and ADX71149 (mGluR2 positive allosteric modulator or PAM) is being developed by our partner Janssen Pharmaceuticals, Inc., to treat schizophrenia. Addex also is advancing several preclinical programs including: GABA-BR PAM for pain, overactive bladder and other disorders; mGluR4 PAM for Parkinson's, anxiety and other diseases; GLP1R PAM for type 2 diabetes; mGluR2 NAM for treating Alzheimer's disease and depression; and FSHR/LHR NAM for sex hormone dependent tumors & reproductive system disorders. In addition, Addex has discovery programs to identify allosteric modulators of: receptor tyrosine kinase (RTK) superfamily, including TrkB PAM for treating neurodegenerative diseases (e.g. Alzheimer’s, Parkinson’s and Huntington’s diseases); and TNF receptor superfamily, including TNFR1 NAM for inflammation (e.g. rheumatoid arthritis) and other diseases.
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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, GABABR, FSHR/LHR, GLP1R, TNFR1, RTK, TrkB 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, GABABR, FSHR/LHR, GLP1R, TNFR1, RTK, TrkB 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 mGluR2, mGluR4, mGluR5, GABABR, FSHR/LHR, GLP1R, TNFR1, RTK, TrkB 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, GABABR, FSHR/LHR, GLP1R, TNFR1, RTK, TrkB 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.