GENEVA--(Marketwire - Sep 24, 2012) - Addex Therapeutics \/ Addex mGluR4 Allosteric Modulator Effective in Multiple Sclerosis Model - A Novel Oral Small Molecule Approach for the Treatment of Multiple Sclerosis. <\/p>\n
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Addex Therapeutics (SIX: ADXN), a leading company pioneering allosteric modulation-based drug discovery and development, announced today achievement of a positive Proof of Concept for its lead metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulator (PAM) compound series in a validated rodent model for multiple sclerosis (MS). MS is a chronic inflammatory demyelinating auto-immune disease that affects the central nervous system (CNS), leading to serious disability. <\/p>\n
\"We are very excited that this promising Addex mGluR4 PAM series may offer a differentiated approach to treating MS,\" said Professor Ursula Grohmann, of University of Perugia, Italy, in whose laboratories one of these studies was performed. \"These data confirm our previous observations, using an mGluR4 PAM tool compound called PHCCC, which demonstrated efficacy in the industry standard neuroinflammation model of MS, the Relapsing-Remitting Experimental Allergic Encephalomyelitis (RR-EAE) model. In this study, the mGluR4 PAM worked by promoting regulatory T-cell (Treg) formation and reversing pro-inflammatory T-cell release. Therefore, we believe that positive modulation of mGluR4 could potentially stop the destruction of myelin in MS in a robust and durable manner.\" <\/p>\n
Addex lead chemical series is a highly selective orally available mGluR4 PAM and shows good pharmacokinetic properties for potential once-daily dosing. When administered once a day for 3 weeks at 10, 30 and 60 mg\/kg sc, Addex mGluR4 PAM demonstrated a dose-dependent, statistically significant reduction in paralysis (clinical score) and the relapse rate in the RR-EAE model of MS in mice. The presentation of these data is being planned for a major international conference. <\/p>\n
\"Current MS therapies are primarily focused on reinstating motor function after an inflammatory attack, preventing new attacks, and preventing or treating disability and symptoms, such as spasticity. In addition, most of these therapies are primarily based on immunomodulatory strategies, and have serious compliance-limiting side effects\", noted Graham Dixon, CSO of Addex Therapeutics. \"We believe a well-tolerated, oral mGluR4 PAM would represent a major advance in the treatment of MS because of the novel and potentially broader mechanism; having the potential to not only treat symptoms, but slow disease progression and offer neuroprotection. We are now rapidly advancing this lead series towards a clinical candidate and conducting experiments to further elucidate the biological role of mGluR4 PAM in MS.\" <\/p>\n
\"Moving the lead compound from this series into full development in 2012 clearly illustrates our strategy of advancing innovative novel selective oral small molecule drug candidates against previously \"undruggable\" targets\" said Bharatt Chowrira, CEO of Addex Therapeutics. \"These data along with the recently announced data on the role of the mGluR4 PAMs in Parkinson's disease, the positive Phase 2 data for dipraglurant in Parkinson's disease levodopa-induced dyskinesia, the two Phase 2 clinical trials being conducted by our partner Janssen, and our GABABR PAM program advancing towards an IND filing later this year, demonstrate the power of Addex platform that continues to generate multiple, novel high value product opportunities.\" <\/p>\n
About Multiple Sclerosis <\/p>\n
Multiple sclerosis, is an idiopathic inflammatory disease of the central nervous system, characterized pathologically by demyelination and subsequent axonal degeneration. The disease commonly presents in young adults and affects twice as many women as men. Common presenting symptoms include numbness, weakness, visual impairment, loss of balance, dizziness, urinary bladder urgency, fatigue, and depression. Approximately 2.5 million people worldwide are affected with prevalence ranging from 2 and 150 per 100,000, depending on the country and specific population. MS takes several forms. The most common affecting around 85 per cent of everyone diagnosed with MS is relapsing remitting MS (RRMS). It means that symptoms appear (a relapse), and then fade away, either partially or completely (remitting). Secondary progressive MS (SPMS) is a stage of MS which comes after RRMS in many cases. Although the pathogenesis of MS is complex and not fully understood, it is believed that RRMS is characterized by repeated episodes of inflammation which eventually leads to the axonal degeneration through damage to, and loss of the myelin sheath characteristic of SPMS. Given the prominence of immune generated inflammation in MS, treatments for the disease have focused particularly on immunosuppressive anti-inflammatory strategies. Currently approved treatments for RRMS are only partially effective in reducing MS relapses and in particular do not halt disability progression. As these drugs alter immune function, patients can experience serious and sometimes life threatening side effects (e.g. opportunistic infections, emergent malignancies, alopecia, cardiotoxicity and myelosuppression). Furthermore, many of these agents also require regular injection, or parenteral infusions which are uncomfortable and inconvenient for the patient. <\/p>\n<\/p>\n
Original post: GENEVA--(Marketwire - Sep 24, 2012) - Addex Therapeutics \/ Addex mGluR4 Allosteric Modulator Effective in Multiple Sclerosis Model - A Novel Oral Small Molecule Approach for the Treatment of Multiple Sclerosis. Processed and transmitted by Thomson Reuters ONE Continue reading
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