治疗儿童Dravet综合征新药Fintepla  

Fintepla,a new approved drug for the treatment of dravet syndrome in children

作　　者：何心 李妍 HE Xin;LI Yan(Department of Pharmacy,Women’s Hospital of Nanjing Medical University,Nanjing Maternity and Child Health Care Hospital,Nanjing 210004,Jiangsu Province,China;Department of Pharmacy,Children Hospital and Maternal and Child Hospital of Shanxi Province,Taiyuan 030013,Shanxi Province,China)

机构地区：[1]南京医科大学附属妇产医院、南京市妇幼保健院药学部,江苏南京210004 [2]山西省儿童医院、山西省妇幼保健院药剂科,山西太原030013

出　　处：《中国临床药理学杂志》2021年第14期1890-1893,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：Fintepla(ZX008,fenfluramine oral solution,芬氟拉明口服液)是2020年6月由美国食品药品监督管理局(FDA)正式批准用于年龄≥2岁的患者治疗与Dravet综合征相关的癫痫。Fintepla是一种液体制剂的低剂量芬氟拉明,可通过激活5-HT2受体,启动谷氨酸N-甲基-D-天冬氨酸受体(NMDAR)促进其激活和释放。当NMDAR达到高水平时,破坏σ1R与NMDAR NR1亚基的结合抑制NMDAR活性,来降低癫痫发作频率,避免NMDAR直接拮抗剂的药物不良反应。现对其作用机制、药效学、药代动力学、临床研究及安全性等做一介绍。Fintepla(ZX008,fenfluramine oral solution)has been approved by the U.S.Food and Drug Administration(FDA)for the treatment of epilepsy associated with Dravet syndrome in patients over 2 years old in June 2020.Fintepla is a liquid preparation of low-dose fenfluramine,which can promote the activation and release of N-methyl-D-aspartate(NMDAR)by activating 5-HT2 receptor.When NMDAR reaches a high level,the binding ofσ1R and NMDAR NR1 subunit is destroyed by Fintepla to inhibit the activity of NMDAR,so as to reduce the seizure frequency and avoid the side effects of NMDAR direct antagonists.The mechanism of action,pharmacodynamics,pharmacokinetics,clinical study and safety were introduced.

关 键 词：芬氟拉明口服液 小儿癫痫 DRAVET综合征 

分 类 号：R985[医药卫生—药品]