This review describes the major developments in lipid-regulating drugs duri
ng the past two years. Most of the novel compounds that have been launched
or were in their final stages of development during this period are aimed p
rimarily at lowering low-density Lipoprotein (LDL)-cholesterol. These inclu
de bile acid sequestrants, HMG-CoA reductase inhibitors and a cholesterol a
bsorption inhibitor. In addition, there have been preclinical reports sugge
sting the potential usefulness of orally bioavailable inhibitors of cholest
erol ester transfer protein in plasma and of acylcoA:cholesterol acyltransf
erase in monocyte-macrophages. The recent discovery of the roles of the sca
venger receptor class B Type 1 and ATP-binding cassette transporter 1 in hi
gh-density lipoprotein (HDL)-cholesterol transport may shift the trend of f
uture developments away from compounds that lower LDL to those aimed at pro
moting HDL turnover.