ACS 化学生物学神经科学分子聚焦 ELND006：另一种 γ-分泌酶抑制剂在临床中失败。
ACS chemical neuroscience molecule spotlight on ELND006: another γ-secretase inhibitor fails in the clinic.
机构信息
Department of Pharmacology and Vanderbilt Center for Neuroscience Drug Discovery, Vanderbilt University Medical Center, Vanderbilt University , Nashville, Tennessee 37232-6600, United States.
出版信息
ACS Chem Neurosci. 2011 Jun 15;2(6):279-80. doi: 10.1021/cn2000469.
Abstract
ELND006 is a novel γ-secretase inhibitor by Elan Corporation that was in the clinic as a potential treatment for Alzheimer's disease (AD). The clinical trial for ELND006 was halted in October 2010 due to liver side effects that are thought to be unrelated to the mechanism of action. However, this represents another small molecule γ-secretase inhibitor that has failed in clinical trials (semagacestat) (http://newsroom.lilly.com/releasedetail.cfm?releaseid=499794) which raises serious questions regarding this mechanism for the treatment of AD.
摘要
ELND006 是一种新型的γ-分泌酶抑制剂，由爱尔兰艾尔建公司研发，曾作为治疗阿尔茨海默病（AD）的潜在药物在临床上使用。由于推测与作用机制无关的肝脏副作用，ELND006 的临床试验于 2010 年 10 月停止。然而，这代表了另一种在临床试验中失败的小分子 γ-分泌酶抑制剂（西玛卡塞他）（http://newsroom.lilly.com/releasedetail.cfm?releaseid=499794），这引发了人们对该机制治疗 AD 的严重质疑。
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