5HT6 Antagonists in the Treatment of Alzheimer's Dementia: Current Progress.
5HT6 Antagonists in the Treatment of Alzheimer's Dementia: Current Progress.
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DOI：
10.1007/s40120-018-0095-y
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发表时间：
2018-06
影响因子：
3.7
通讯作者：
Sabbagh MN
中科院分区：
文献类型：
--
作者：
Andrews M;Tousi B;Sabbagh MN
阿尔茨海默病是一种重要的疾病，有相当大的和未满足的疾病负担，需要继续研究和更多的治疗选择。5HT6拮抗剂是一类新的药物。因为它们是前胆碱能药物，这些药物被用作乙酰胆碱酯酶抑制剂（如多奈哌齐）的辅助药物，进一步增加中枢神经系统（CNS）中的乙酰胆碱。5HT6拮抗剂的早期试验显示，当作为阿尔茨海默氏痴呆症的辅助疗法使用时，认知和日常生活活动得到改善。然而，最近的III期试验未能显示认知功能有统计学意义上的显著改善。本文将全面回顾5HT6拮抗剂在药物开发中的应用，包括一些最近已停止使用的拮抗剂。我们将讨论这类药物的成功和失败，并为其继续研究和开发提供理由。
Alzheimer’s disease is an important condition with a considerable and unmet disease burden in large need of continued research and more treatment options. The 5HT6 antagonists are a new class of medications to be offered. Because they are pro-cholinergic, these medications are to be used as adjuncts to acetylcholinesterase inhibitors (such as donepezil), further increasing acetylcholine in the central nervous system (CNS). Early trials of the 5HT6 antagonists showed improvements in cognition and activities of daily living when used as adjuncts to current therapies for Alzheimer’s dementia. However, recent phase III trials have failed to show a statistically significant improvement in cognitive function. This article will provide a comprehensive review of 5HT6 antagonists in drug development, including some that have been recently discontinued. We will discuss both the successes and failures of this drug class and provide rationale for their continued research and development.
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作者：
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期刊：
Alzheimer's & dementia (New York, N. Y.)
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