Statins are powerful agents for the reduction of low-density lipoprotein ch
olesterol (LDL-C) and reduction of cardiovascular risk. Newly developed sta
tins with increased potency, such as rosuvastatin (Crestor(TM)) and NK-104
(in earlier clinical development), are capable of achieving marked LDL-C re
ductions. Cholesterol-lowering agents with mechanisms of action distinct fr
om those of the statins are in active development. These include bile trans
port inhibitors, such as improved bile acid-absorbing resins and specific i
nhibitors 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 treatme
nt. Another approach is to reduce cardiovascular risk by modifying atherosc
lerotic 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 storag
e.