Development of perampanel in epilepsy.

Abstract

Alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA)-type glutamate receptors play a key role in mediating glutamatergic transmission in the cortex. Perampanel (2-[2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl] benzonitrile) is a potent, orally active, highly selective, non-competitive AMPA-type glutamate receptor antagonist, identified via a focused discovery program at Eisai Research Laboratories. Development of perampanel as adjunctive therapy for the treatment of partial-onset seizures was planned in keeping with regulatory guidance and guidelines on antiepileptic drug (AED) development. This is the first AED with a specific action on glutamate-mediated excitatory neurotransmission to show evidence of efficacy and tolerability in reducing treatment-refractory partial-onset seizures in Phase III clinical trials. Perampanel (Fycompa(®)) has been approved in the EU and the United States for adjunctive treatment of partial-onset seizures.

• Authors: A Satlin, L D Kramer, A Laurenza
• Journal: Acta neurologica Scandinavica. Supplementum (Acta Neurol Scand Suppl) Issue 197 Pg. 3-8 ( 2013) ISSN: 1600-5449 [Electronic] Denmark
• PMID: 23480150 (Publication Type: Journal Article, Review)
• Copyright: © 2013 John Wiley & Sons A/S.

Chemical References

• Anticonvulsants
• Nitriles
• Pyridones
• perampanel

Topics

• Animals
• Anticonvulsants (therapeutic use)
• Clinical Trials as Topic
• Drug Evaluation, Preclinical
• Epilepsy (drug therapy)
• Humans
• Nitriles
• Pyridones (therapeutic use)