Markham Anthony
Springer, Private Bag 65901, Mairangi Bay, 0754, Auckland, New Zealand.
Drugs. 2016 Mar;76(4):517-22. doi: 10.1007/s40265-016-0555-6.
Brivaracetam (Briviact(®)), a 4-n-propyl analogue of levetiracetam developed by UCB Pharma, has been approved in the EU as an adjunctive therapy for the treatment of partial-onset seizures. Brivaracetam binds to synaptic vesicle glycoprotein 2a (SV2A) in the brain with greater selectivity and 15- to 30-fold higher affinity than levetiracetam, as demonstrated in preclinical models, and has demonstrated efficacy in reducing the frequency of partial onset seizures in clinical trials. This article summarizes the milestones in the development of brivaracetam leading to this first approval for use as adjunctive therapy for uncontrolled partial-onset seizures in adults with epilepsy.
布瓦西坦(Briviact®)是优时比制药公司研发的左乙拉西坦的4 - 正丙基类似物,已在欧盟获批作为辅助疗法用于治疗部分性发作癫痫。如临床前模型所示,布瓦西坦与大脑中的突触小泡糖蛋白2a(SV2A)结合具有更高的选择性,且亲和力比左乙拉西坦高15至30倍,并且在临床试验中已证明其在降低部分性发作癫痫发作频率方面的疗效。本文总结了布瓦西坦研发过程中的重要节点,这些节点促成了其首次获批用于辅助治疗成人癫痫患者无法控制的部分性发作。