High levels of cholesterol and other lipid constituents are major risk factors in the development of atherosclerosis as well as diseases and disorders associated with it. Though, drugs of various categories acting through different mechanisms are available for antihyperlipidemic therapy, there are limitations associated with each of them, keeping the interest in discovery of newer and better antihyperlipidemic drugs alive. Identification and exploitation of novel molecular targets for discovery of new antihyperlipidemic drugs is an important area of research. Twenty such drug targets are elaborated herein, for their biochemical roles, structures, estimations, as well as, exploitation for new drug discovery research. Few recently discovered drugs are based on such molecular targets are also discussed.