ASTA Medica is developing retigabine, a carbamic acid ethyl ester and a selective potassium channel opener, for the treatment of complex partial seizures. Phase II trials have commenced , and a multicenter placebo-controlled dosage-finding study has begun in Europe and Australia . Retigabine is also undergoing phase II testing in Germany, Switzerland, Russia and the US for the potential treatment of epilepsy . Phase II trials have shown >50% reduction in seizure frequency in 12 of 35 patients with refractory epilepsy . Phase I clinical trials for epilepsy were successfully completed in Germany in 1995 . Single and multiple dose trials demonstrated the tolerability and favorable pharmacokinetic behavior of the compound . The compound showed good compatibility and exhibits an antisense anticonvulsive effect in various preclinical epilepsy models [250565,299344]. Side effects of mild to moderate tiredness, fatigue and nausea were observed . The spectrum of activity of retigabine resembles that of valproate, but its potency is greater and toxicity is reduced . The mechanism of action of retigabine is probably multifnotarial. Research has shown that retigabine acts as a selective K + channel opener in neuronal cells and this can be expected to contributejito its anticonvulsant effect . In addition it demonstrates potentiation of GABA transmission and possibly also weak modulation of sodium and calcium channels . Retigabine also has neuroprotective activity with potential for the treatment of stroke and neurodegenerative diseases, such as Alzheimer's disease, Huntington's disease and multiple sclerosis . In February 2000, Lehman Brothers predicted product launch could be as early as 2002 for epilepsy in the US . In February 1999, Lehman Brothers predicted that the first major launch date of the drug would be 2003, and the year of peak sales to be 2011 . @ PharmaPress Ltd.
|Number of pages||6|
|Publication status||Published - 2001|
ASJC Scopus subject areas
- Drug Discovery