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异他林:一种腺苷A2A受体拮抗剂,用于减少帕金森病的“关”期时间。

Istradefylline: adenosine A2A receptor antagonist to reduce "OFF" time in Parkinson's disease.

作者信息

Paton D M

机构信息

Professor Emeritus of Pharmacology, University of Auckland, Auckland, New Zealand and Professor Emeritus of Oral Biology, University of Alberta, Edmonton, Alberta, Canada.

出版信息

Drugs Today (Barc). 2020 Feb;56(2):125-134. doi: 10.1358/dot.2020.56.2.3098156.

DOI:10.1358/dot.2020.56.2.3098156
PMID:32163528
Abstract

Parkinson's disease (PD) is an extremely common degenerative disease with a progressive course. Unfortunately, the longer patients are treated with levodopa, the more likely they are to suffer from increasingly long periods of immobility or "OFF" time. For over 30 years Kyowa Kirin Co., Ltd. (formerly Kyowa Hakko Kirin Co., Ltd.) has been researching the possibility of finding drugs that affect adenosine receptors and that can be used successfully as additional drugs in the treatment of PD. Istradefylline is an adenosine A2A receptor antagonist that significantly reduces the "OFF" time and improves the motor function of patients with PD, as measured by the Unified Parkinson's Disease Rating Scale (UPDRS) Part III, while increasing the time without troublesome dyskinesia. It was approved for use in PD in Japan in 2013 and in the United States in 2019.

摘要

帕金森病(PD)是一种极为常见的进行性退行性疾病。不幸的是,患者使用左旋多巴治疗的时间越长,就越有可能遭受越来越长的不动期或“关”期。30多年来,协和麒麟株式会社(原协和发酵麒麟株式会社)一直在研究寻找影响腺苷受体且能成功用作帕金森病治疗辅助药物的药物的可能性。依曲茶碱是一种腺苷A2A受体拮抗剂,通过统一帕金森病评定量表(UPDRS)第三部分测量,它能显著减少“关”期时间,并改善帕金森病患者的运动功能,同时增加无麻烦异动症的时间。它于2013年在日本获批用于帕金森病治疗,2019年在美国获批。

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