Considerable research efforts have focused on the discovery of safe an
d efficacious acyl-CoA cholesterol acyltransferase (ACAT) inhibitors a
s cholesterol-lowering and/or antiatherosclerotic agents, Although cli
nical success remains elusive, recent developments in the molecular bi
ology of ACAT and success in identifying potent and bioavailable inhib
itors that are not adrenotoxic has led to renewed hope that ACAT inhib
ition may ultimately yield agents that will have value in treating hum
an atherosclerotic disease.