ExonHit’s EHT 0202 Counters Scopolamine’s Detrimental Effects on Cognition in Humans
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 significant decrease of the power in Delta and Theta bands (p
Cognitive improvement, as assessed by the analysis of P300 (an ERP wave) amplitude, was shown at an 80mg dose of EHT 0202 regardless the time post-dose (p
These findings add to EHT 0202′s pharmacological properties elicited from preclinical studies in particular its ability to modulate GABA receptors and to redirect APP processing (which plays a pivotal role in the evolution of AD).
“EHT 0202 is not an acetylcholinesterase inhibitor. Evidence of EHT 0202′s pharmacological activity is emphasized in young healthy subjects. Restoring the brain processes that are altered by scopolamine is indeed a very encouraging observation. It is a positive news flow for the future evaluation of EHT 0202 in Alzheimer’s disease,” declares Dr. Fitoussi, MD from MEDISCIS, the clinical research organisation which executed the clinical study.
Bruno Tocque, President of ExonHit’s Management Board said “We are delighted to register this positive effect of our lead compound in this clinical Phase 1 trial. We now know that the compound, administered orally, has a pharmacological effect in man. A Phase 2 clinical trial is currently engaged in order to assess the safety and efficacy profile of EHT 0202 in patients suffering from AD. ExonHit’s strategy is to provide therapeutic and diagnostic solutions in chronic diseases such as Alzheimer’s disease, and we are committed to bring these innovations to the market”.
About ExonHit Therapeutics http://www.exonhit.com/
ExonHit Therapeutics is the world’s leader in the analysis of alternative RNA splicing, a process which when deregulated plays a key role in the onset of various diseases.
ExonHit has a multi-component commercial strategy to capture the maximum value from its leadership in alternative splicing. The Company is already generating revenues from a new generation of microarrays, SpliceArray(TM) family of products that enable life science researchers to detect crucial disease-associated information. These products are marketed worldwide in conjunction with Agilent and Affymetrix. In the field of diagnostics, ExonHit has a major collaboration with bioMerieux to develop completely novel predictive blood-based cancer diagnostics, which could play a key role in improving the treatment of breast cancer and other major cancers and develops its own projects for the detection of other chronic diseases such as Alzheimer’s disease or atherosclerosis.
In parallel, ExonHit is developing its own therapeutic pipeline in the field of neurodegenerative diseases and cancer. The Company has advanced drug candidates into clinical trials and is evaluating several promising pre-clinical compounds. ExonHit also has a strategic partnership with Allergan, to discover and develop new therapeutics in the areas of pain, neurological diseases and ophthalmology. This collaboration provides on-going research funding to ExonHit.
Founded in 1997, ExonHit is headquartered in Paris, France and has a U.S. facility in Gaithersburg, Maryland. The Company is listed on Alternext of Euronext Paris (ticker: ALEHT; ISIN: FR0004054427) since November 17, 2005.
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Contacts ExonHit Therapeutics Bruno TocquÃƒÆ’Ã‚Æ’Ãƒ“šÃ‚©, C.E.O. - Tel: +33-1-58-05-47-00 Philippe Rousseau, C.F.O. - email@example.com
ExonHit Therapeutics SA
CONTACT: Contacts: ExonHit Therapeutics: Bruno TocquÃƒÆ’Ã‚Æ’Ãƒ“šÃ‚©, C.E.O. – Tel:+33-1-58-05-47-00. Philippe Rousseau, C.F.O. – firstname.lastname@example.org