Lapaquistat acetate  (Synonyms: TAK-475)

Lapaquistat acetate (TAK-475) is a squalene synthase inhibitor, blocking the conversion of farnesyl diphosphate (FPP) to squalene in the cholesterol biosynthesis pathway^[1]. Lapaquistat acetate is effective at lowering low-density lipoprotein cholesterol, but it might cause liver damage. Lapaquistat acetate is used for hypercholesterolemia and mevalonate kinase deficiency (MKD) research^[2].

Squalene synthase^[1]

Lapaquistat acetate (饮食补充；100 或 200 mg/kg；32 周) 降低血浆胆固醇和甘油三酯水平。它可以延缓冠状动脉粥样硬化的进展，并将冠状动脉粥样斑块从不稳定的、富含巨噬细胞/脂质积累的病变转变为 体内的稳定纤维肌肉病变^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

645.14

C₃₃H₄₁ClN₂O₉

189060-13-7

固体

White to off-white

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]

  [3]. M Shiomi, et al. Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid-rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions. Br J Pharmacol. 2008 Jul;154(5):949-57.  [Content Brief]