The most important risk factor for cardiovascular disease (CVD) is an elevated circulating concentration of low-density lipoprotein (LDL-C). Therefore, lowering LDL-C concentrations is the most effective cardioprotective intervention and should be pursued by any means necessary. In this paper, we review the actions of a proper, medically-supervised use of nutraceuticals and functional foods to lower LDL-C and, consequently, CVD risk. The most effective compounds, alone or in appropriate combinations, are phytosterols, monacolin K from red yeast rice, berberine, and dietary fiber, namely beta-glucan. It is important that physicians monitor the use of nutraceuticals, verify their regular use, their effects on lipid profile, and the occurrence of untoward effects. Future research will certainly further clarify the efficacy and mechanisms of action of the molecules described in this article, as well as their optimal use by primary care physicians and specialists.Impact statement LDL cholesterol is the major risk factor for cardiovascular disease. The use of validated nutraceuticals in otherwise low-risk patients is effective and should be oversawn by physicians.