Atherosclerosis is a complex disease process in which genetic, lipid, cellular and immunological factors combine to determine the location, severity and timing of lesion development and clinical events. It has been demonstrated, however, that inflammation governs atherosclerosis during the course of development of atherosclerosis. It has also been demonstrated that regulation of the inflammatory reaction (e.g. statins) is effective in decreasing the cardiovascular events and improving the prognosis of atherosclerotic diseases. Other anti-atherosclerosis agents introduced in this study are adiponectin, testosterone, defibrase, angiotensin-converting enzyme inhibitors, dextromethorphan, paeonol, 15-lipoxygenase inhibitors, curcumin, interferon-beta, quercetin, AGI-1067, peroxisome proliferator-activated receptor gamma ligands and garlic. Some antiplatelet drugs described here are aspirin, clopidogrel and glycoprotein IIb/IIIa receptor antagonist. The mechanism of action of these agents is depicted. A new way of targeting anti-atherosclerosis and antiplatelet drugs to atherosclerosis areas is introduced. The author uses an antioxidized low-density lipoprotein antibody that is also conjugated to a mixture of anti-atherosclerosis agents or antiplatelet drugs to target these agents specifically to the atherosclerosis area. With this kind of targeting, we can use a much higher dose of anti-atherosclerosis agents or antiplatelet drugs and have much fewer side effects.