Anavex Life Sciences Corp (AVXL)

[JB3729]

A2-73 clinical trial safety data -

From the second Phase 1 trial -

The Phase 1 clinical trial was a randomized, double-blind, placebo-controlled study in 22 healthy male volunteers. The participants received single, ascending oral doses of ANAVEX 2-73 ranging from 1 mg to 60 mg. The primary objective of the trial was to evaluate safety and tolerability together with pharmacokinetic parameters.

•Safety: No serious side effects were reported. There was no study discontinuation due to adverse events. No dose-limiting adverse events or lab abnormalities at doses of 1, 10, 30, 40 and 50mg were observed.

•Tolerability: Maximum tolerated dose (MTD) of ANAVEX 2-73 was defined as 55mg. Observed adverse events at doses above the MTD included dizziness and headache, which were moderate in severity and reversible. These side effects are often seen with drugs that target CNS conditions, including Alzheimer’s disease. Across all doses, there were no differences in blood pressure and resting heart rate. Analysis of electrocardiograms (ECG) did not reveal any dose-related or time-dependent changes and the QT interval did not reveal any clinically significant changes. Additionally, no sign could be detected for any dose- or time-dependent changes for any of the hematology, biochemistry, and coagulation parameters.

•Pharmacokinetics (PK): ANAVEX 2-73 was determined to be suitable for daily oral dosing based on its PK profile. PK data revealed biotransformation of ANAVEX 2-73 to its main metabolite, which also actively targets sigma-1 and muscarinic receptors like its parent drug ANAVEX 2-73. Both maximum plasma concentration (Cmax), which relates to absorption and distribution of the drug in the blood, and area under the plasma concentration-time curve (AUC), which represents the total drug exposure over time, showed dose-proportional linear increases for both ANAVEX 2-73 and its metabolite. The biological half-life (T1/2) for ANAVEX 2-73 was 8.56 hours and 28.74 hours for its metabolite.
http://www.anavex.com/?news=anavex-announces-positive-phase-1-data-for-anavex-2-73-lead-candidate-for-the-treatment-of-alzheimers