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@article{1137343, author = {Rektor, Ivan}, article_location = {LONDON}, article_number = {2}, doi = {http://dx.doi.org/10.1517/14656566.2013.754883}, keywords = {AMPA receptor antagonist; anticonvulsant agent; partial-onset seizures; perampanel; refractory epilepsy}, language = {eng}, issn = {1465-6566}, journal = {EXPERT OPINION ON PHARMACOTHERAPY}, title = {Perampanel, a novel, non-competitive, selective AMPA receptor antagonist as adjunctive therapy for treatment-resistant partial-onset seizures}, url = {http://informahealthcare.com/doi/abs/10.1517/14656566.2013.754883?journalCode=eop}, volume = {14}, year = {2013} }
TY - JOUR ID - 1137343 AU - Rektor, Ivan PY - 2013 TI - Perampanel, a novel, non-competitive, selective AMPA receptor antagonist as adjunctive therapy for treatment-resistant partial-onset seizures JF - EXPERT OPINION ON PHARMACOTHERAPY VL - 14 IS - 2 SP - 225-235 EP - 225-235 PB - INFORMA HEALTHCARE SN - 14656566 KW - AMPA receptor antagonist KW - anticonvulsant agent KW - partial-onset seizures KW - perampanel KW - refractory epilepsy UR - http://informahealthcare.com/doi/abs/10.1517/14656566.2013.754883?journalCode=eop L2 - http://informahealthcare.com/doi/abs/10.1517/14656566.2013.754883?journalCode=eop N2 - 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. ER -
REKTOR, Ivan. Perampanel, a novel, non-competitive, selective AMPA receptor antagonist as adjunctive therapy for treatment-resistant partial-onset seizures. \textit{EXPERT OPINION ON PHARMACOTHERAPY}. LONDON: INFORMA HEALTHCARE, 2013, roč.~14, č.~2, s.~225-235. ISSN~1465-6566. Dostupné z: https://dx.doi.org/10.1517/14656566.2013.754883.
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