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ExonHit's EHT 0202 Counters Scopolamine's Detrimental Effects on Cognition in Humans
Date:3/25/2008

PARIS, March 25 /PRNewswire-FirstCall/ -- ExonHit Therapeutics, a drug and diagnostic discovery company, announced today the results of a Phase 1 study assessing the effects of its lead compound, EHT 0202, on scopolamine-induced brain impairments in humans. ExonHit's EHT 0202 is a compound, with a novel mechanism of action, which has shown preclinical benefits on memory and neuronal loss and is currently tested in a Phase 2 clinical trial on Alzheimer disease (AD) patients.

Scopolamine interferes with the transmission of nerve impulses by acetylcholine, a substance to which it is structurally similar, thus depressing nervous system activity. Cognitive impairment due to central cholinergic dysfunction, or scopolamine administration, is measurable through electroencephalography (EEG) changes under both nonstimulus and stimulus conditions. A number of studies indicate that EEG is a sensitive measure of acetylcholine's activity and of the induced alterations elicited by scopolamine. In addition, scopolamine-induced EEG changes have been considered as possible biomarkers for AD as the impairment acetylcholine's activity is one of the landmarks of this disease.

The Phase 1, randomized, double-blind, placebo-controlled, crossover study with 3 treatments and the placebo being administered over 4 distinct periods in 12 young healthy subjects assessed the effects of single administrations of EHT 0202 (40mg, 80mg, and 120mg) on scopolamine-induced (0.6mg) cognitive impairments by using EEG recordings (spectral analysis and Event Related Potentials - ERPs) at the following time points : 1h15, 2h45 4h15, 5h45 post dose.

As expected, scopolamine significantly reduced vigilance levels and cognition as measured by spectral analysis and ERPs respectively when administered to study subjects.

The results of the spectral analysis indicate that EHT 0202 is associated with an improvement of the vigilance level at 1h15 post-dose, as shown by the signific
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SOURCE ExonHit Therapeutics SA
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