Preclinical Data of ANAVEX 1-41 and ANAVEX 2-73 Show Highly Potent Anti-Amnesic and Neuroprotective Activity Against Amyloid Beta (25-35) Peptide Toxicity in Alzheimer’s Disease (AD) Animal Models
Data on Anavex’s sigma-ligands ANAVEX 1-41 and ANAVEX 2-73 was presented in a poster at the 8e Colloque de la Societe des Neurosciences Meeting being held in Montpellier, France (Abstract D.30) May 22, 2007
Geneva, Switzerland — May 23, 2007 — Anavex Life Sciences Corp. (the “Company”) (OTCBB: AVXL) a biopharmaceutical company, today announced that in vivo preclinical data presented in a poster at the 8e Colloque de la Société des Neurosciences meeting, Montpellier, France, showed that ANAVEX 1-41 and ANAVEX 2-73 –new potent muscarinic ligands with a high affinity for the sigma-1 receptor-suggest a possibly important neuroprotective and anti-amnesic efficacy in Alzheimer’s Disease (AD).
In the poster titled “Anti-amnesic and neuroprotective potentials of aminotetrahydrofuran derivatives, mixed muscarinic/sigma-1 ligands, against amyloid beta (25-35) peptide toxicity in mice”, the following results with regards to potent anti-amnesic and neuroprotective effects were demonstrated:
ANAVEX 1- 41 reversed the learning deficits induced by Aβ25-35 peptide in a dose-dependent manner. The compound was effective in both short-term and long-term memory tests, with active doses at about 30μg/kg. When injected before the peptide, i.e., seven days prior to the tests, ANAVEX 1-41 was effective in preventing the appearance of learning deficits and lipid peroxidation in the hippocampus, measuring the Aβ25-35 peptide-induced oxidative stress. Therefore, the compound showed a potent neuroprotective activity, with active doses between 100 and 1000μg/kg. Pretreatment with the sigma-1 receptor selective antagonist BD1047 or the muscarinic M1 selective antagonist scopolamine differentially blocked the ANAVEX 1-41 effects on short- or long-term memory tests, suggesting that the compound acts as a mixed muscarinic and sigma-1 receptor agonist.
ANAVEX 2-73 also reversed the learning deficits induced by Aβ25-35 peptide in a dose-dependent manner. The compound was effective in both short-term and long-term memory tests, with active doses at about 300-1000μg/kg. When injected prior to the peptide, ANAVEX 2-73 protected against the Aβ25-35 peptide-induced learning deficits and hippocampal lipid peroxidation. The compound showed a potent neuroprotective activity at doses 300-1000μg/kg.
ANAVEX 2-73 appeared moderately sensitive to the BD 1047 pre-treatment in the behavioral tests. This effect was more marked in lipid peroxidation measures. Scopolamine, blocked the behavioral effects of ANAVEX 2-73 particularly at the1000μg/kg dose of the compound.
“We believe that Anavex Life Sciences Corp. will be soon recognized as a leading discovery biopharmaceutical company in the field of sigma ligands like its novel lead candidate compounds ANAVEX 1-41 and ANAVEX 2-73 which are in late-stage preclinical development,” said Panos Kontzalis, Ph.D., Anavex’s Chief Executive Officer. “Our sigma-ligands have demonstrated potent neuroprotective and anti-amnesic activity in AD models. We believe that Anavex’s sigma-ligands represent a novel mechanism of action and we anticipate to advancing these two compounds into investigational new drug (IND) enabling clinical studies in the near term.”
Anavex’s Sigmaceptor-N program involves the discovery and development of novel and original drug candidates targeting neurological and neurodegenerative diseases. The Company’s lead drug candidates exhibit high affinity for sigma receptors with strong evidence for anti-amnesic, nooanaleptic, neuroprotective, anti-apoptotic, anti-oxidatitive, anti-inflammatory, anti-convulsive, anti-depressant, ant-fatigue, anti-addictive and anxiolytic properties.
Anavex’s Sigmaceptor-C program involves the discovery and development of novel and original drug candidates targeting cancer. The Company’s lead drug candidates exhibit high affinity for sigma receptors with strong evidence for selective pro-apoptotic, anti-metastatic and low toxicity properties in various types of cancer such as, colon, prostate, breast and lung.