NicOx SA announced successful Phase I pharmacokinetic results with HCT 1026 in development for Alzheimer's Disease. The pharmacokinetic study in healthy volunteers showed penetration of the bloodbrain barrier and presence of effective drug concentrations in the cerebrospinal fluid after repeated oral dosing. Several clinical epidemiological studies have shown the beneficial effect of NSAIDs (Non Steroidal Anti -Inflammatory Drugs) in reducing the risk and delaying the clinical progression of Alzheimer's Disease. However, the chronic use of NSAIDs is limited by the number of serious gastrointestinal and renal side effects including peptic ulcers and impaired kidney function. Nitric oxide is capable of preventing or repairing injury to the gastrointestinal tract.

HCT 1026 is a patented nitric oxide-donating derivative of flurbiprofen, with excellent activity and safety in animal models of Alzheimer's Disease and other neurodegenerative diseases. The mechanism underlying HCT 1026 activity and safety profile is based on nitric oxide release and the multiple inhibition of several inflammatory mediators such as prostanoids, cytokines, free radicals, likely through inhibition of nuclear transcription factors.

Previous Phase I and Phase II studies in more than 200 subjects have shown excellent overall tolerability of the drug. Phase I clinical trials with endoscopic analysis have shown that HCT 1026 has superior gastric tolerability.

The recently completed Phase I trial assessing drug penetration into the cerebrospinal fluid (CSF) was conducted in 24 subjects in a randomised, parallel group, multiple dose, pharmacokinetic study. The trial showed that pharmacologically effective drug levels inhibiting prostaglandins were found in the cerebrospinal fluid after repeated oral administration of HCT 1026 (75mg bid and 150mg bid) for seven days. The overall information from this study will also allow selection of the correct dose and posology for subsequent clinical studies in Alzheimer's Disease.