Germany based Evotec has announced the positive preliminary findings of a double-blind, single-dose, three-way cross-over study with its orally active NR2B subtype selective NMDA receptor antagonist, EVT 101.
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The study was performed in 19 healthy young subjects to investigate short-term effects of two doses of EVT 101 and placebo. The effects of the compound on cognitive endpoints, changes in local cerebral blood flow, reflecting neuronal activation or deactivation during the performance of cognitive tasks, as well as base-line regional cerebral blood flow, were explored.
All treatments were well tolerated confirming previous observations in healthy subjects. While there was no evidence of acute improvement in cognitive function, the activity of a number of brain regions, known for their role as a memory retrieval network, were selectively modified during the performance of certain tasks, as assessed by analysis of the changes in local cerebral blood flow.
These findings represent the first demonstration of effects of EVT 101 on human brain function at doses that are well tolerated and predicted to be clinically relevant. In addition, Evotec has satisfactorily completed dosing of its four week higher repeat dose study conducted in France. Encouragingly, initial findings regarding the cerebrospinal fluid (CSF) penetration of EVT 101 assessed in a subgroup receiving EVT 101 showed that the compound demonstrated penetration into the CSF at levels predicted to inhibit NR2B receptors to a significantly higher amount than memantine at its therapeutic dose in Alzheimer’s disease.
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