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lapaquistat acetate + ezetimibe
- Development stage
- Discontinued
- Lead developer
- Takeda
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Lapaquistat acetate + ezetimibe is a combination of two lipid-lowering agents investigated for the treatment of hypercholesterolemia and dyslipidemia. Lapaquistat acetate is a squalene synthase inhibitor that reduces cholesterol biosynthesis in the liver, while ezetimibe inhibits intestinal absorption of cholesterol by blocking the Niemann-Pick C1-Like 1 (NPC1L1) protein at the brush border of the small intestine. The combination was studied to provide additive or synergistic effects on lowering low-density lipoprotein cholesterol (LDL-C). Clinical trials showed significant reductions in LDL-C and other cardiovascular risk markers; however, development of lapaquistat acetate was terminated due to hepatic safety concerns, including elevations in liver enzymes and rare cases meeting Hy's law criteria. Ezetimibe remains an approved therapy for hypercholesterolemia[1][4][5][7][8].
- Brand names
- None
- Other names
- None
02
Targets
FDFT1 (Squalene synthase)NPC1L1 (Niemann-pick C1-Like 1 transporter)
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