Lipoproteins, differentiated on the basis of density, size, and protein content, are essential for the biogenesis of plasma membranes and maintenance of their integrity. They also serve as sources of energy, hormone precursors, and signaling molecules.4 In blood, lipoproteins transport cholesterol and triglycerides. Abnormalities of lipoprotein metabolism appear to be the result of genetic factors, which modify the sensitivity of individuals to adverse dietary habits and to sedentary lifestyles.
Elevated cholesterol-rich low-density lipoproteins (LDLs) and lipoproteins that are rich in triglycerides (TGs), and decreased levels of high-density lipoproteins (HDLs) are strongly associated with atherosclerosis.4 Diet and exercise can reduce total plasma cholesterol concentrations by as much as 25%. If this approach is insufficient to normalize lipid levels drug therapy is initiated. Drugs in the top 300 that regulate lipoprotein metabolism (Table 1) fall into four major classes.2,4,11
Table 1. Drugs that Affect Cholesterol and Lipoprotein Metabolism.2,4,11,
Drugs (Rank/300)
Mechanisms of Action
Common Indications
Inhibitors of cholesterol synthesis
Atorvastatin (1)
Rosuvastatin (12)
Simvastatin (22)
Pravastatin (57)
Lovastatin (132)
Inhibit HMG-CoA reductase, the rate-limiting enzyme in cholesterol synthesis
Decrease LDL
Decrease TG
Increase HDL
Hypercholesterolemia
Prophylaxis for coronary atherosclerosis
Inhibitors of cholesterol absorption
Ezetimibe (70)
Decrease cholesterol transport into enterocytes
Decrease LDL
Decrease TG
Hypercholesterolemia
Fibrates
Fenofibrate (83)
Agonists of peroxisome proliferator-activated receptor α (PPARα) in hepatocytes
Decrease LDL
Decrease TG
Increase HDL
Hypertriglyceridemia
Omega-3 fatty acids
Omega-3-acid ethyl ester (222)
Regulate hepatic nuclear transcription factors to reduce TG synthesis and increase fatty acid oxidation
