Retigabine ASIA medica

Research output: Contribution to journalArticle

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Abstract

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 [249117], and a multicenter placebo-controlled dosage-finding study has begun in Europe and Australia [392702]. Retigabine is also undergoing phase II testing in Germany, Switzerland, Russia and the US for the potential treatment of epilepsy [323383]. Phase II trials have shown >50% reduction in seizure frequency in 12 of 35 patients with refractory epilepsy [373379]. Phase I clinical trials for epilepsy were successfully completed in Germany in 1995 [180371]. Single and multiple dose trials demonstrated the tolerability and favorable pharmacokinetic behavior of the compound [264306]. 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 [276123]. The spectrum of activity of retigabine resembles that of valproate, but its potency is greater and toxicity is reduced [373379]. 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 [273670]. In addition it demonstrates potentiation of GABA transmission and possibly also weak modulation of sodium and calcium channels [299344]. 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 [249381]. In February 2000, Lehman Brothers predicted product launch could be as early as 2002 for epilepsy in the US [357788]. 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 [319225]. @ PharmaPress Ltd.

Original languageEnglish
Pages (from-to)93-98
Number of pages6
JournalIDrugs
Volume4
Issue number1
Publication statusPublished - 2001

Fingerprint

Epilepsy
Germany
Siblings
Seizures
Clinical Trials, Phase I
Sodium Channels
Potassium Channels
Russia
Urethane
Huntington Disease
Valproic Acid
Calcium Channels
Switzerland
Neurodegenerative Diseases
Anticonvulsants
gamma-Aminobutyric Acid
Nausea
Multiple Sclerosis
Fatigue
ezogabine

ASJC Scopus subject areas

  • Pharmacology

Cite this

Retigabine ASIA medica. / Fatope, Majekodunmi O.

In: IDrugs, Vol. 4, No. 1, 2001, p. 93-98.

Research output: Contribution to journalArticle

Fatope, MO 2001, 'Retigabine ASIA medica', IDrugs, vol. 4, no. 1, pp. 93-98.
Fatope, Majekodunmi O. / Retigabine ASIA medica. In: IDrugs. 2001 ; Vol. 4, No. 1. pp. 93-98.
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