Cholesterol absorption inhibitors in development as potential therapeutics

Drugs that lower low-density lipoprotein cholesterol through their actions in the gastrointestinal tract have been used for > 30 years. Bile acid sequestrants have very excellent safety profiles but their poor tolerability means they have limited clinical use. Recently developed new compounds are better tolerated in clinical trials and show greater benefit in reducing low-density lipoprotein cholesterol level, as compared to "older" sequestrants. Cholesterol absorption inhibitors and bile acid transporter inhibitors have recently been reported to show clinical efficacy and safety as novel gut-acting drugs for lowering cholesterol. Further advances in our understanding of the cholesterol absorption mechanism will provide novel therapeutic targets, such as the ATP-binding cassette transporter. This approach in the treatment of lowering cholesterol appears to play a more significant role in the clinical field of atherosclerotic vascular disease.