The macrophage and its related
cholesterol efflux are considered to be a key player in atherosclerotic formation in relation to the function of
high-density lipoprotein (HDL). The HDL function can be evaluated by the reaction between
lipid-loaded macrophages and
lipid-acceptors in the HDL fraction from the plasma,
apolipoprotein B-depleted serum, and/or whole serum/plasma. Recent studies have reported that an impaired
cholesterol efflux of HDL is observed in patients with cardiometabolic diseases, such as
dyslipidemia,
diabetes mellitus, and
chronic kidney disease. A population-based cohort study has reported an inverse association between the
cholesterol efflux capacity of HDL and the incidence of atherosclerotic disease, regardless of the serum
HDL-cholesterol level. Moreover, in this paper, when we summarized several clinical interventional studies of
statin treatment that examined
cholesterol efflux, a potential increase in the efflux in patients treated with
statins was implied. However, the effect was not fully defined in the current situation because of the small sample sizes, lack of a unified protocol for measuring the efflux, and short-term intervention periods without cardiovascular outcomes in available studies. Further investigation is necessary to determine the effect of drugs on
cholesterol efflux. With additional advanced studies,
cholesterol efflux is a promising laboratory index to understand the HDL function.