Summary: Statins are powerful agents for the reduction of low‐density lipoprotein cholesterol (LDL‐C) and reduction of cardiovascular risk. Newly developed statins with increased potency, such as rosuvastatin (Crestor^TM) and NK‐104 (in earlier clinical development), are capable of achieving marked LDL‐C reductions. Cholesterol‐lowering agents with mechanisms of action distinct from those of the statins are in active development. These include bile transport inhibitors. such as improved bile acid‐absorbing resins and specific inhibitors of the ileal Na⁺/bile acid cotransporter. There are also specific inhibitors of cholesterol absorption, such as ezetimibe, which may provide cholesterol lowering that is additive to that achieved with statin treatment. Another approach is to reduce cardiovascular risk by modifying atherosclerotic processes within the arterial wall, as represented by the acyl CoA:cholesterol acyltransferase (ACAT) inhibitor avasimibe; ACAT inhibitors may reduce atherosclerotic lesions by inhibiting macrophage cholesterol storage.