080210xf's Blog

L'X fragile sera vaincu | Fragile X will be conquered

mGluR5 inhibition and Fragile X syndrome, pain, anxiety, depression and gastroesophageal reflux disease (GERD)

Addexpharma.com |

Dipraglurant (ADX48621) is a negative allosteric modulator (NAM) of metabotropic glutamate receptor 5 (mGluR5). This mechanism has been clinically validated and has blockbuster potential in several indications, including: anxiety; gastroesophageal reflux disease (GERD); acute treatment of migraine; Fragile X syndrome; Parkinson’s disease levodopa-induced dyskinesia (PD-LID); and nonparkinsonian dystonias, like idiopathic torsion dystonia (ITD, also early-onset generalized dystonia) and cervical dystonia (spasmodic torticollis).

PD-LID and dystonia have been chosen as the lead indications because preclinical data indicate that dipraglurant may be particularly well suited for these indications. Specifically, dipraglurant is the first drugcandidate in preclinical testing reported to reduce both of the major PD-LID symptoms, chorea (rapid uncontrolled movements) and dystonia (writhing and cramping movements). While dystonia is a significant problem for PD patients, dytonias also occur as a variety of separate conditions of either primary (e.g. hereditary) or secondary (drug-induced or otherwise acquired) origin. There are currently no products specifically licensed for treatment of dystonias and there is a large unmet medical need with substantial commercial potential for an effective product in this indication. This differentiation may ultimately mean that dipraglurant could become the best-in-class product for PD-LID and one of the first meaningful treatments for dystonia.

Because of its unique properties (and their long standing interest in the mGluR5 NAM mechanism) The Michael J. Fox Foundation for Parkinson’s Research awarded a USD900,000 grant to Addex to support the Phase IIa PD-LID trial of dipraglurant in September 2010. The foundation, which involves some of the world’s leading Parkinson’s researchers via its scientific advisory board, is known for actively supporting cutting edge research and products.

An immediate release formulation of dipraglurant, dipraglurant-IR, will enter Phase IIa clinical testing in patients with PD-LID in the first half of 2011.

Development of an extended-release formulation of dipraglurant was performed in 2010 and Phase I testing of dipraglurant-ER will commence mid-2011. Dipraglurant-ER has been developed for clinical testing for treatment of non- Parkinsonian dystonia and potentially by a licensee for other indications, including Fragile X syndrome, pain, anxiety, depression and gastroesophageal reflux disease (GERD), all of which have validation. A Phase IIa study of dipraglurant- ER for the treatment of non-Parkinsonian dystonias, is scheduled to start in 2012.

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