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Lapaquistat Acetate

Known as: 2-(1-(2-((3R,5S)-1-(3-Acetoxy-2,2-dimethylpropyl)-7-chloro-5-(2,3- dimethoxyphenyl)-2-oxo-1,2,3,5-tetrahydrobenzo(e)(1,4)oxazepin-3- yl)acetyl)piperidin-4-yl)acetic Acid 
An acetate salt form of lapaquistat, a squalene synthase inhibitor investigated for the treatment of hypercholesterolemia.
National Institutes of Health

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TAK-475

Papers overview

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2016
2016
Pharmacokinetics of TAK-475, a Squalene Synthase Inhibitor, in Rats and Dogs
Abstract The pharmacokinetics of TAK-475 (lapaquistat acetate), a squalene synthase inhibitor, was investigated in rats and dogs… 
2016
2016
Anti-inflammatory and cytoprotective effects of a squalene synthase inhibitor, TAK-475 active metabolite-I, in immune cells simulating mevalonate kinase deficiency (MKD)-like condition
TAK-475 (lapaquistat acetate) and its active metabolite-I (TAK-475 M-I) inhibit squalene synthase, which catalyzes the conversion… 
2016
2016
Characterization of Transporters in the Hepatic Uptake of TAK-475 M-I, a Squalene Synthase Inhibitor, in Rats and Humans
Abstract TAK-475 (lapaquistat acetate) is a squalene synthase inhibitor and M-I is a pharmacologically active metabolite of TAK… 
2011
2011
Squalene synthase inhibitor lapaquistat acetate: could anything be better than statins?
Elevated serum cholesterol level is an important risk factor for cardiovascular disease,1 and cholesterol lowering by 3-hydroxy-3… 
Highly Cited
2010
Highly Cited
2010
Molecular Docking Studies to Map the Binding Site of Squalene Synthase Inhibitors on Dehydrosqualene Synthase of Staphylococcus Aureus
Abstract Dehydrosqualene synthase of Staphylococcus aureus is involved in the synthesis of golden carotenoid pigment… 
2008
2008
Lapaquistat acetate, a squalene synthase inhibitor, changes macrophage/lipid‐rich coronary plaques of hypercholesterolaemic rabbits into fibrous lesions
Inhibition of squalene synthesis could transform unstable, macrophage/lipid‐rich coronary plaques into stable, fibromuscular… 
2007
2007
Protective effects of a squalene synthase inhibitor, lapaquistat acetate (TAK-475), on statin-induced myotoxicity in guinea pigs.
2007
2007
Abstract 193: Lapaquistat Acetate, A Novel Squalene Synthase Inhibitor, Co-administered with Atorvastatin Reduces Plasma Lipids and C-Reactive Protein Levels in Subjects with Primary…
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