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Anavex reports animal study results as lead Alzheimer's compound approaches phase 1 clinical trials
Date:5/4/2010

utive Chairman of ANAVEX. "The highly selective binding properties of ANAVEX 2-73 has led to beneficial effects at very low doses, which may ultimately lead to a favorable tolerability profile and offer a wide therapeutic index. This may mean many patients could benefit from low doses, although going to higher doses may be possible in some patients to offer greater efficacy without compromising on the tolerability profile. ANAVEX is confident in the emerging profile of ANAVEX 2-73 as it prepares for Phase 1 clinical trials. We have established that sigma receptors are druggable targets and we have worked to shape ANAVEX 2-73 as our optimized lead compound, which may prove to be neuroprotective."

When administered prior to amyloid-beta 25-35 peptide, ANAVEX 2-73 protected against the amyloid peptide-induced learning deficits, hippocampal lipid peroxidation and cell loss in the CA1 pyramidal layer and showed potent neuroprotective activity. Extensive in-vitro receptor binding and electrophysiology studies, sigma receptor binding studies and electrophysiological effects on sodium and calcium currents have been completed.

The binding affinities of ANAVEX 2-73 for more than 50 receptors were studied. The potency of ANAVEX 2-73, inhibiting enzyme activities was also studied on enzyme assays including calpain, nitric oxide synthase (constitutive and inducible form), protein kinase (PKCa and PKCss), EGF receptor kinase and calcineurin.

"On average in the industry, it takes six and a half years for discovery and preclinical testing to yield a potentially viable lead compound. Over 80% of compounds fail in preclinical stages, before arriving at this stage of research. ANAVEX 2-73 is a novel oral disease modification agent that is believed to act at several levels, including the mitochondria, and may offer a therapy that could be used as a standalone or in combination with other age
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SOURCE Anavex Life Sciences Corp.
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