The class
A review names CETP inhibition among three specific pharmacological strategies to boost reverse cholesterol transport (Indian J Exp Biol 2013)
Original title: Molecular regulation of cholesterol metabolism: HDL-based intervention through drugs and diet
This review analyzes emerging pharmacological and nutritional strategies to control cholesterol metabolism, given that available anticholesterolemic drugs are incompletely effective and carry adverse effects. Pharmacological interventions center on molecules that interfere with HDL metabolism and reverse cholesterol transport (RCT) through genetic control of apolipoprotein A-I, agonism at liver X receptor alpha, or inhibition of cholesteryl ester transfer protein (CETP), scavenger receptor BI, or ecto F0F1 ATPase/synthase. Nutritional interventions use fibers, phytosterols, and probiotics that interfere with cholesterol absorption and reabsorption by enterocyte and hepatocyte transporters, influencing the final step of RCT. The search for new drugs remains at an early stage, though biotechnological research on probiotics, fibers, and phytosterols is expected to yield promising therapeutic tools with fewer adverse effects and lower cost than traditional drugs.
Original abstract
The overloading of cholesterol in the arteries remains the principal cause of cardiovascular diseases. Since available anticholesterolemic drugs are not completely effective and have several severe adverse effects, the aim of this review is to analyze current research focused on the emerging, innovative therapeutic strategies based on both pharmacological and nutritional interventions to control cholesterol metabolism. Pharmacological interventions mainly involve the use of molecules capable of interfering with high-density lipoprotien (HDL) metabolism and the reverse cholesterol transport (RCT) through genetic control of apolipoprotein A-I (ApoA-I), agonism at liver X-receptor alpha (LXRalpha), or inhibition of cholesteryl ester transport protein (CETP), scavenger receptor BI(SR-BI), and ecto F0F1ATPase/synthase. Nutritional interventions are based on the use of fibres, phytosterols, and probiotics acting through interference with absorption and reabsorption of cholesterol by enterocyte and hepatocyte specific transporters, thus influencing RCT final step. The search for new drugs is still at the very beginning and new molecules are not yet ready to enter clinical use. However, several promising findings coming from innovative biotechnological research are expected shortly to produce probiotics, fibres, and phytosterols to be used as therapeutic tools. Among the most important advantages of natural products in respect to traditional drugs are the lack of severe adverse effects and their low cost.
Summary written by cetpinhibition.org from the published abstract; figures as published. Page updated 19 August 2026. Methods.