Epilepsy is a term used for recurring seizure disorder, a condition that is characterized by the tendency for an individual to have repeated nervous seizures (interruption of normal brain activity).Epilepsy has two forms, idiopathic seizure disorder, which has no identifiable cause, and symptomatic seizure disorder, which can be traced to a known cause.It is estimated that 70% of epileptics suffer from idiopathic epilepsy, which has no known or avoidable cause.The remaining 30% of epileptics suffer from symptomatic epilepsy that has its causes in events such as problematic births, head trauma, stroke, and an infection of the CNS or a brain tumor.In both types of epilepsy, seizures can occur at any stage in life and can be triggered by hormonal changes in the body or by stimuli such as light, touch or sound. During the past decades, a large number of new antiepileptic drugs have been marketed worldwide. However, the proportion of patients failing to respond to current antiepileptic drugs has not been changed to any significant extend. There is a great demand for new drugs with improved efficacy and tolerability. In addition to that, drugs preventing epilepsy, or its progression would be an important innovation. The world market for Epilepsy therapies, based on 2004 sales is US$10,4 billion and is estimated to grow to US$13.2 billion by 2010 and US$ 15.3 billion by 2015.


ANAVEX 2-73 AND ANAVEX 19-144
ANAVEX 2-73 and its active metabolite ANAVEX 19-144 are new tetrahydrofuranic compounds in advanced preclinical phase for the treatment of epilepsy or as adjunct therapies to existing drugs. They present mixed pharmacological activity involving muscarinic, sodium channel, NMDA and sigma-1 components showing prominent anti-amnesic, anticonvulsant and anti-depressant potential. The drugs act as simultaneous antagonists on presynaptic M2 autoreceptors and on the presynaptic M3 muscarinic heteroreceptors of the glutamatergic neuronal endings, in synergy with their agonism on the intracellular sigma-1 receptor mainly located on the endoplasmic reticulum concerning the first (anti-amnesic) activity and, at higher doses (5 – 50 mg/kg per os or ip) as antagonists on sodium and calcium channels and, like memantine, weak antagonist of NMDA receptors, concerning the anticonvulsive and antidepressive activity. ANAVEX 2-73 was administered at very low doses, 17 to 1700 fold below the dose levels inducing unwanted secondary (cholinergic and other) effects. In epilepsy animal models, both compounds exhibited very efficient anticonvulsive action; inhibition of tonic crises in maximal electroshock seizures (MES) and pentetetrazole (PTZ) models of generalized convulsions.