Key result
Inhibition of CETP and ANGPTL3 effectively lowers LDL cholesterol, with ANGPTL3 inhibition showing significant reductions even in patients with familial hypercholesterolemia.
Why the study?
Do novel pharmaceuticals targeting CETP, ANGPTL3, and apoC-III reduce LDL cholesterol in patients with familial hypercholesterolemia?
Do novel pharmaceuticals targeting CETP, ANGPTL3, and apoC-III reduce LDL cholesterol in patients with familial hypercholesterolemia?
Pharmaceuticals inhibiting CETP and ANGPTL3 represent promising novel therapeutic strategies for lowering LDL cholesterol, particularly in patients with familial hypercholesterolemia who may not respond adequately to conventional therapies.
Supports exploration of ANGPTL3 inhibition for LDL lowering in familial hypercholesterolemia; leaves open clinical adoption pending randomized trials.
PURPOSE OF REVIEW: Familial hypercholesterolemia is characterized by high LDL cholesterol and an elevated risk to develop coronary heart disease. Mutations in LDL receptor-mediated cholesterol uptake are the main cause of familial hypercholesterolemia. However, multiple mutations in various other genes are also associated with high LDL cholesterol and even familial hypercholesterolemia. Thus, pharmaceuticals that target these genes and proteins might be attractive treatment options to reduce LDL cholesterol. This review provides an overview of the recent developments and clinical testing of such pharmaceuticals. RECENT FINDINGS: About 80 genes are associated with hypercholesterolemia but only pharmaceuticals that inhibit cholesteryl ester transfer protein (CETP), angiopoietin-related protein 3 (ANGPTL3), and apolipoprotein C-III (apoC-III) have recently been tested in clinical trials. Inhibition of CETP and ANGPTL3 lowered LDL cholesterol. ANGPTL3 inhibition had the largest effect and was even effective in familial hypercholesterolemia patients. The effect of apoC-III inhibition on LDL cholesterol is not conclusive. SUMMARY: Of the many potential pharmaceutical targets involved in LDL cholesterol, only a few have been studied so far. Of these, pharmaceuticals that inhibit CETP or ANGPTL3 are promising novel treatment options to reduce LDL cholesterol but the effect of apoC-III inhibition requires more research.
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Volta et al. (2018) conducted a review in Familial hypercholesterolemia. CETP, ANGPTL3, and apoC-III inhibitors was evaluated. Inhibition of CETP and ANGPTL3 effectively lowers LDL cholesterol, with ANGPTL3 inhibition showing significant reductions even in patients with familial hypercholesterolemia.
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