Lapaquistat (TAK-475) is a novel potent, competitive, orally active squalene synthase inhibitor with IC50 of 78 nM.
Lapaquistat (TAK-475) displays no effect on plasma aspartate aminotransferase and alanine aminotransferase activities.
Lapaquistat (TAK-475) effectively inhibits cholesterol synthesis in rat liver with ED50 of 2.9 mg/kg (p.o.), lowers plasma total cholesterol, triglyceride and phospholipid levels in rabbits, also inhibits the secretion of cholesterol, triglyceride and phospholipid components of very-low-density lipoprotein (VLDL) from liver.
