title: 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.affiliation: Eisai Neuroscience Product Creation Unit, Woodcliff Lake, NJ 07677, USA. andrew_satlin@eisai.com
authors.forename: A
authors.initials: A
authors.lastname: Satlin
authors.forename: L D
authors.initials: LD
authors.lastname: Kramer
authors.forename: A
authors.initials: A
authors.lastname: Laurenza
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D004353:Drug Evaluation, Preclinical; D004827:Epilepsy / Q000188:drug therapy*; D006801:Humans; D009570:Nitriles; D011728:Pyridones / Q000627:therapeutic use*
chemical_list: D000927:Anticonvulsants; D009570:Nitriles; D011728:Pyridones; C551441:perampanel