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Review Article

氘化药物的临床应用及合成方法

卷 30, 期 36, 2023

发表于: 12 January, 2023

页: [4096 - 4129] 页: 34

弟呕挨: 10.2174/0929867330666221122123201

价格: $65

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摘要

许多药物具有不良的吸收、分布、代谢和排泄(ADME)特性，这阻止了它们的广泛使用或限制了它们在某些适应症中的使用。除了制备技术和前药策略外，氘修饰是改善ADME性能的可行方法。近年来，氘化药物越来越受到制药行业的关注。到目前为止，FDA已经批准了两种氘化药物。2017年，austedo被FDA批准为美国亨廷顿病新药，这是第一个在全球上市的氘药物。近日(2021年6月9日)，多纳非尼在中国上市;这一结果引起了各大制药公司和制药行业对氘技术的重新重视。此外，BMS-986165、RT001、ALK-001、HC-1119、AVP-786等药物正在进行III期临床研究，部分固体氘化合物已进入I、II期临床试验。氘策略在药学研究中得到了广泛的应用，成为近年来药学研究的热点。本文综述了氘化药物的研究与发展，重点介绍了氘修饰对药物的影响、氘策略的优点以及氘化药物的合成策略。希望为临床应用、新的氘化学实体的发现和新型氘化药物的研发提供参考。

关键词: 氘化药物，单胺氧化酶，毒性，药物代谢，药物合成，ADME性质。

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