Abstract / Summary
Dyslipidemia is a primary driver of atherosclerotic cardiovascular disease. While statins reduce LDL-C and cardiovascular events, statin intolerance and failure to achieve guideline targets limit their utility. To review the mechanism, efficacy, safety, and clinical positioning of current and emerging antihyperlipidemic agents as of May 2026. High-intensity statins remain first-line with 50-60% LDL-C reduction. Ezetimibe and bempedoic acid provide incremental LDL-C lowering of 15-28% without muscle toxicity. PCSK9 inhibitors and inclisiran achieve 50-60% reduction via distinct mechanisms, with inclisiran offering twice-yearly dosing. Bempedoic acid and inclisiran demonstrated cardiovascular outcome benefit in statin-intolerant populations. Gene editing therapy VERVE-101 showed single-dose LDL-C reductions of 39-55% in early trials. Therapeutic options now address statin intolerance, adherence barriers, and residual risk. A stepwise algorithm starting with oral agents and escalating to RNA-based therapies optimizes outcomes and resource use.