A phase 1 clinical trial of the sigma-2 receptor complex allosteric antagonist CT1812, a novel therapeutic candidate for Alzheimer's disease
A phase 1 clinical trial of the sigma-2 receptor complex allosteric antagonist CT1812, a novel therapeutic candidate for Alzheimer's disease
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DOI：
10.1016/j.trci.2018.11.001
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发表时间：
2019-01-01
影响因子：
4.8
通讯作者：
Catalano, Susan M.
中科院分区：
文献类型：
--
作者：
Grundman, Michael;Morgan, Roger;Catalano, Susan M.
背景资料：Elayta（CT 1812）是一种新型的σ-2受体复合物的变构拮抗剂，可阻止和取代A β寡聚体与神经元的结合。通过停止一个关键的起始事件在阿尔茨海默氏病，这种一流的候选药物减轻下游突触毒性和恢复认知功能的老年转基因小鼠模型Alzheimer's diseases.Methods：一个阶段1，两部分的单次和多次递增剂量的研究进行了7和4个队列的健康人类受试者，分别。在A部分中，健康的年轻受试者（
Background: Elayta (CT1812) is a novel allosteric antagonist of the sigma-2 receptor complex that prevents and displaces binding of A beta oligomers to neurons. By stopping a key initiating event in Alzheimer's disease, this first-in-class drug candidate mitigates downstream synaptotoxicity and restores cognitive function in aged transgenic mouse models of Alzheimer's disease.Methods: A phase 1, two-part single and multiple ascending dose study was conducted in 7 and 4 cohorts of healthy human subjects, respectively. In part A, healthy, young subjects (