Because of the potential for off-label usage of the large and growing number of drugs targeting the initiating and potentiating factors associated with cardiovascular disease, the focus of this review is on key enzymes involved in cholesterol and tryglycerides metabolism, respectively, specifically lecithin-cholesterol acyltransferase (LCAT)- and lipoprotein lipase (LPL)-activating compounds. This evidence concerns the gene LCAT and cardiovascular disorder.