Dipraglurant is a selective, orally available, small molecule drug candidate which acts as a negative allosteric modulator (NAM) of the metabotropic glutamate receptor 5 (mGlu5 receptor).
Dipraglurant is in clinical development for the treatment of levodopa induced dyskinesia (LID) in Parkinson’s patients. LID invariably develop as a consequence of long-term use of levodopa and often become as disabling as the parkinsonian symptoms themselves. Dipraglurant has received orphan drug designation in the US for the treatment of LID
Dipraglurant is to be taken at the same time as levodopa and it is currently formulated as an immediate release (IR) capsule which appears particularly effective in treating LID because of its fast onset of action and rapid wash-out which mirrors the time course of LID in PD patients.
Dipraglurant has been studied in four Phase 1 clinical studies and a Phase 2a LID Proof of Concept (POC) trial in PD patients, where it demonstrated clinically significant improvement in LID scores at doses that were generally safe and well tolerated (Tison 2016).
Phase 2b/3 studies have been designed to further evidence and confirm the treatment effect of dipraglurant in LID.
Dipraglurant was discovered at Addex - composition of matter patents have been granted in the US and Europe and are fully owned by the company. Additional patents covering Polymorph 1 and formulations are likely to further extend the patent life of dipraglurant.