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lapaquistat acetate + simvastatin
- Development stage
- Discontinued
- Lead developer
- Takeda
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Lapaquistat acetate + simvastatin is a discontinued investigational combination therapy for the treatment of hypercholesterolemia and primary dyslipidemia. Lapaquistat acetate is a small molecule squalene synthase inhibitor that reduces cholesterol biosynthesis downstream of HMG-CoA reductase, leading to decreased low-density lipoprotein (LDL) cholesterol and other cardiovascular risk markers[1][3][7]. Simvastatin is an HMG-CoA reductase inhibitor (statin) that lowers lipid levels by inhibiting the conversion of HMG-CoA to mevalonate, an early step in cholesterol synthesis[6]. The combination was studied in phase 2 and 3 clinical trials for its additive effects on lowering LDL cholesterol. However, development was terminated due to hepatic safety concerns associated with lapaquistat acetate[1][3].
- Brand names
- Zocor (simvastatin)
- Other names
- lapaquistat acetate + simvastatin
02
Targets
HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)FDFT1 (Squalene synthase)
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