帕金森病新药Opicapone的研究进展

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摘要帕金森病（PD）是发病率仅次于阿尔茨海默病的第二大神经系统退行性病变。当前治疗PD的主要途径仍然是左旋多巴治疗，然而长期服用左旋多巴会导致一系列副作用，如运动障碍、疗效减退、“开-关”现象和剂末效应等。儿茶酚-O-甲基转移酶（COMT）抑制剂能抑制周围左旋多巴的代谢，增加左旋多巴的传输量，从而用于左旋多巴附加疗法，用来增强左旋多巴疗效。作为一种新的三代COMT抑制剂，Opicapone能用于左旋多巴附加疗法中，用来改善波动效应和剂末现象。Opicapone在体内具有长时间的持续活性，当前建议剂量是每天睡前口服50 mg。Opicapone诱导的COMT抑制剂的半衰期较前两代Opicapone抑制剂更长，且能显著升高左旋多巴全身性暴露，具有更有效、更安全、更持久的特性。

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	陈信捷1 罗恩丽2 陈雅芳1 雒晓东2 郑春叶2

关键词 ：帕金森病, Opicapone, 左旋多巴, 儿茶酚氧位甲基转移酶抑制剂

Abstract：Parkinson′s disease (PD) is the second most common neurodegenerative disease after Alzheimer′s disease. At present, the main way to treat PD is still Levodopa therapy. However, long-term use of Levodopa can lead to a series of side effects, such as dyskinesia, decreased efficacy, "on-off" phenomena, end of dose phenomena, and soon. The catechol-O-methyltransferase (COMT) inhibitor can inhibit the metabolism of surrounding Levodopa and increase the transmission amount of Levodopa, so it is used in Levodopa additional therapy to enhance the efficacy of Levodopa. As a new third-generation COMT inhibitor, Opicapone can be used in Levodopa addition therapy to improve the motor fluctuations and end of dose phenomena. Opicapone has sustained activity in vivo for a long time. The current recommended dose is 50 mg per day taken orally before bedtime. The half-life of opicapone-induced COMT inhibitors is longer than that of the previous two generations of Opicapone inhibitors, and can significantly increase Levodopa systemic exposure, with more effective, safer and more lasting properties.

Key words： Parkinson′s disease Opicapone Levodopa Catechol-O-methyltransferase inhibitor

基金资助:国家自然科学基金面上项目（81873358、81373712）。

通讯作者: 罗恩丽（1973.11-），女，医学博士，主任医师；研究方向：帕金森病与运动障碍性疾病。

引用本文:

陈信捷1 罗恩丽2 陈雅芳1 雒晓东2 郑春叶2. 帕金森病新药Opicapone的研究进展[J]. 中国医药导报, 2019, 16(20): 29-33.
CHEN Xinjie1 LUO Enli2 CHEN Yafang1 LUO Xiaodong2 ZHENG Chunye2. Research progress of new drug Opicapone for Parkinson′s disease. 中国医药导报, 2019, 16(20): 29-33.

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http://www.yiyaodaobao.com.cn/CN/ 或 http://www.yiyaodaobao.com.cn/CN/Y2019/V16/I20/29

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