lapaquistat

Lapaquistat (TAK-475) is a small molecule cholesterol-lowering drug candidate that was developed by Takeda for the treatment of hypercholesterolemia and dyslipidemia. Unlike statins, which inhibit HMG-CoA reductase early in the cholesterol biosynthesis pathway, lapaquistat acts as a squalene synthase inhibitor, targeting an enzyme further downstream in the pathway. By inhibiting squalene synthase, it reduces cholesterol synthesis without affecting other products of the mevalonate pathway. Clinical trials demonstrated that lapaquistat effectively lowered low-density lipoprotein (LDL) cholesterol and other cardiovascular risk markers both as monotherapy and in combination with statins. However, development was terminated due to concerns about hepatic safety—specifically elevations in liver enzymes and rare cases meeting Hy's law criteria for potential drug-induced liver injury[1][3][4][6][8].

Other names

lapaquistat acetate