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Lapaquistat
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Lapaquistat : ウィキペディア英語版
Lapaquistat

Lapaquistat (TAK-475) is a cholesterol-lowering drug. Unlike statins, which inhibit HMG-CoA reductase, lapaquistat metabolites inhibit squalene synthase, which is further downstream in the synthesis of cholesterol. It is hoped that side effects can be reduced by not disturbing the mevalonate pathway, which is important for other biochemical molecules besides cholesterol.
However, there is increasing evidence that statins (which inhibit the mevalonate pathway) may be clinically useful ''because'' they affect these other molecules (including protein prenylation).
On March 28, 2008, Takeda halted further development of lapaquistat.〔( Takeda Pharmaceutical Company Limited press release - Discontinuation of Development of TAK-475, A Compound for Treatment of Hypercholesterolemia )〕 While effective at lowering low-density lipoprotein cholesterol in a dose-dependent manner, development of the drug was ceased over potential hepatic safety issues. 〔 〕
==References==

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抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
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