2012年10月23日，卫材公司宣布美国食品药品管理局(FDA)已批准Fycompa(吡仑帕奈)用于≥12岁癫痫患者部分性发作的辅助治疗，无论患者是否伴有继发性全面发作。
Fycompa是一种α-氨基-3-羟基-5甲基-4-异唑丙酸(AMPA)受体拮抗剂，它通过抑制突触后AMPA受体谷氨酸活性，减少神经元过度兴奋。这是FDA批准的首个具有该作用机理的抗癫痫药物。
该批准令主要基于3项关键的国际多中心、随机、双盲、安慰剂对照、剂量递增的3期临床试验数据，共纳入1480例部分发作患者。这些伴有或无继发性全身发作的部分发作患者的发作频率显著减少。
受试患者报告的最常见不良事件包括头晕、嗜睡、疲劳、易怒、跌倒、恶心、共济失调、平衡障碍、步态不稳、眩晕和体重增加。
Fycompa标签中包含一项黑框警告，警示医生和患者应注意系列神经精神事件风险，包括易怒、攻击行为、愤怒、焦虑、偏执、欣快情绪、烦躁以及精神状态变化。有报告称上述某些事件较为严重和危及生命，还观察到少数患者有暴力想法或危险行为。建议患者和看护者如果发现患者情绪或行为异常变化，应及时通知医护专业人员。在剂量递增期间，当用药剂量较高时，医护专业人员应对患者进行密切监测。
应用包括Fycompa在内的抗癫痫药物可导致极少数患者出现自杀想法或行为。应嘱咐患者，如果出现任何新的或更为严重的抑郁症状，以及新的或更为严重的任何情绪、感觉和行为异常或突然变化、自杀想法或行为及自我伤害想法时，立即通知医护人员。
必须嘱咐患者，在没有征求医生意见的情况下不应停用Fycompa。突然停药或可导致严重问题和发作频率反弹。
FDA已建议美国毒品管制局(DEA)按照美国《管制物品法》将Fycompa列为管制药品。在DEA完成最终管制分类后，卫材公司将宣布Fycompa上市时间。
ST LOUIS (MD Consult) - On October 23, 2012, Eisai announced that the US Food and Drug Administration (FDA) has approved Fycompa (perampanel) as an adjunctive treatment of partial-onset seizures with or without secondarily generalized seizures in patients with epilepsy aged 12 years and older. Fycompa is an alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. Fycompa reduces neuronal hyperexcitation associated with seizures by inhibiting glutamate activity at post-synaptic AMPA receptors. This is the first antiepileptic agent approved by the FDA to work in this manner.
The approval was granted primarily on the basis of clinical data from 3 pivotal phase 3, global, randomized, double-blind, placebo-controlled, dose-escalation studies that included 1480 patients with partial-onset seizures. Patients with partial-onset seizures with or without secondary generalized seizures experienced a significant reduction in seizure frequency.
The most commonly reported adverse events in study patients were dizziness, somnolence, fatigue, irritability, falls, nausea, ataxia, balance disorder, gait disturbance, vertigo, and weight gain.
Fycompa's label contains a Boxed Warning to alert prescribers and patients about the risk of serious neuropsychiatric events, including irritability, aggression, anger, anxiety, paranoia, euphoric mood, agitation, and mental status changes. Some of these events were reported as serious and life-threatening. Violent thoughts or threatening behavior was also observed in a few patients. Patients and caregivers should be advised to alert a health care professional immediately if atypical changes in mood or behavior are observed. Health care professionals should closely monitor patients during the titration period when higher doses are used.
The use of antiepileptic drugs, including Fycompa, may cause suicidal thoughts or actions in a very small number of persons. Patients should be instructed to call their health care provider immediately if any new or worsening symptoms of depression arise, as well as any unusual or sudden changes in mood, feelings, behavior, or suicidal thoughts, behavior, or thoughts of self-harm that they have never had before or may be worse than before.
Patients must be told not to stop taking Fycompa without first talking to a health care provider. Abrupt discontinuation of Fycompa may lead to serious problems and can cause a rebound in seizure frequency.
The FDA has recommended that Fycompa be classified by the US Drug Enforcement Administration (DEA) as a scheduled drug under the country's Controlled Substances Act. After the DEA has provided the final scheduling designation, Eisai will announce when Fycompa will be made available to patients and physicians.