a Reta Lila Weston Institute for Neurological Studies, UCL , London , UK.
b Centro de Estudos Egas Moniz , Hospital de Santa Maria , Lisbon , Portugal.
Expert Rev Neurother. 2017 Jul;17(7):649-659. doi: 10.1080/14737175.2017.1336086. Epub 2017 Jun 5.
Opicapone is a third generation, highly potent and effective catechol O‑methyltransferase (COMT) inhibitor that optimizes the pharmacokinetics and bioavailability of L-DOPA therapy. Areas covered: In this review, the authors describe the preclinical and clinical development of opicapone. In PD patients with motor fluctuations, once daily opicapone administration was well-tolerated and consistently reduced OFF-time and increased ON-time without increasing the frequency of troublesome dyskinesia, and these benefits were maintained over at least a year of continued open-label therapy. Expert commentary: With its convenient once-daily regimen, adjunct opicapone should be considered as an effective option for use in L-DOPA treated PD patients experiencing motor fluctuations.
阿扑卡朋是第三代强效、高选择性儿茶酚-O-甲基转移酶(COMT)抑制剂,可优化左旋多巴治疗的药代动力学和生物利用度。
在这篇综述中,作者描述了阿扑卡朋的临床前和临床开发。在伴有运动波动的 PD 患者中,每日一次阿扑卡朋给药耐受良好,持续减少关期时间并增加开期时间,而不增加令人困扰的运动障碍的发生频率,且这些益处至少在持续的开放性治疗一年中得到维持。
凭借其方便的每日一次的给药方案,辅助用阿扑卡朋应该被认为是一种有效的选择,可用于正在接受左旋多巴治疗、出现运动波动的 PD 患者。