Lapaquistat acetate (TAK-475) 是一种角鲨烯合酶 (squalene synthase) 抑制剂，可阻止法呢基二磷酸酯 (FPP) 转化为角鲨烯。Lapaquistat acetate (TAK-475) 最初旨在用于甲羟戊酸激酶缺乏症 (MKD)，可有效降低低密度脂蛋白胆固醇，但可能引起肝脏损害。
Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene[1]. Lapaquistat acetate (TAK-475) is originally intended use to Mevalonate Kinase Deficiency (MKD), it is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage[2].
[1]. Stein EA, et al. Lapaquistat acetate: development of a squalene synthase inhibitor for the treatment of hypercholesterolemia. Circulation. 2011 May 10;123(18):1974-85. [2]. Marcuzzi A, et al. Repositioning of Tak-475 In Mevalonate Kinase Disease: Translating Theory Into Practice. Curr Med Chem. 2018;25(24):2783-2796.
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