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

REKTOR, Ivan. Perampanel, a novel, non-competitive, selective AMPA receptor antagonist as adjunctive therapy for treatment-resistant partial-onset seizures. EXPERT OPINION ON PHARMACOTHERAPY. LONDON: INFORMA HEALTHCARE, 2013, vol. 14, No 2, p. 225-235. ISSN 1465-6566. Available from: https://dx.doi.org/10.1517/14656566.2013.754883.

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

• Original language: English
• Type of outcome: Article in a journal
• Field of Study: 30104 Pharmacology and pharmacy
• Country of publisher: United Kingdom of Great Britain and Northern Ireland
• Confidentiality degree: is not subject to a state or trade secret
• WWW: URL
• Impact factor: Impact factor: 3.085
• RIV identification code: RIV/00216224:14740/13:00070575
• Organization unit: Central European Institute of Technology
• Doi: http://dx.doi.org/10.1517/14656566.2013.754883
• UT WoS: 000313674700008
• Keywords in English: AMPA receptor antagonist; anticonvulsant agent; partial-onset seizures; perampanel; refractory epilepsy
• Tags: ok, rivok
• Tags: International impact, Reviewed

Abstract

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