J 2013

Perampanel, a novel, non-competitive, selective AMPA receptor antagonist as adjunctive therapy for treatment-resistant partial-onset seizures

REKTOR, Ivan

Basic information

Original name

Perampanel, a novel, non-competitive, selective AMPA receptor antagonist as adjunctive therapy for treatment-resistant partial-onset seizures

Authors

REKTOR, Ivan (203 Czech Republic, guarantor, belonging to the institution)

Edition

EXPERT OPINION ON PHARMACOTHERAPY, LONDON, INFORMA HEALTHCARE, 2013, 1465-6566

Other information

Language

English

Type of outcome

Článek v odborném periodiku

Field of Study

30104 Pharmacology and pharmacy

Country of publisher

United Kingdom of Great Britain and Northern Ireland

Confidentiality degree

není předmětem státního či obchodního tajemství

References:

Impact factor

Impact factor: 3.085

RIV identification code

RIV/00216224:14740/13:00070575

Organization unit

Central European Institute of Technology

DOI

UT WoS

000313674700008

Keywords in English

AMPA receptor antagonist; anticonvulsant agent; partial-onset seizures; perampanel; refractory epilepsy

Tags

Tags

International impact, Reviewed
Změněno: 20/12/2013 11:38, Olga Křížová

Abstract

V originále

Introduction: In the search for new antiepileptic drugs (AEDs), AMPA-type receptor antagonists have a novel target and the potential to improve seizure control in patients with refractory seizures. This article reviews preclinical and clinical data for 2-(2-oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile, perampanel, a new chemical entity developed for the treatment of partial-onset seizures. Areas covered: Perampanel is a selective, non-competitive AMPA receptor antagonist. The preclinical profile of perampanel and its clinical development are reviewed. Expert opinion: Unlike many traditional AEDs, perampanel demonstrated efficacy in a broad spectrum of preclinical seizure models. Phase I and II clinical studies suggested perampanel had a favorable safety and tolerability profile and demonstrated proof of concept for its mechanism of action in patients with treatment-resistant partial-onset seizures. Three Phase III studies have additionally demonstrated that adjunctive perampanel 4 - 12 mg/day is well-tolerated and significantly improves seizure control in these patients. Median reductions in seizure frequency were 23.3% (4 mg), 26.3 - 30.8% (8 mg) and 17.6 - 34.5% (12 mg) versus 9.7 - 21.0% for placebo. Responder rates were 28.5% (4 mg), 33.3 - 37.6% (8 mg) and 33.9 - 36.1% (12 mg) versus 14.7 - 26.4% for placebo. Perampanel may offer an alternative treatment option in the management of patients with refractory partial-onset seizures.

Links

ED1.1.00/02.0068, research and development project
Name: CEITEC - central european institute of technology