2164u90 and Hypercholesterolemia

The ileal Na+/bile acid cotransporter (IBAT) maintains the reabsorption of bile acids from the ileum in the enterohepatic circulation of bile acids. Interruption of the enterohepatic circulation of bile acids by bile acid sequestrants or partial ileal bypass surgery can cause a significant decrease of serum cholesterol in animals and human patients. Inhibition of IBAT by specific IBAT inhibitors such as S-8921 has been proven to lower serum cholesterol in a variety of experimental animals. IBAT inhibitors, a new class of hypocholesterolemic drugs may be used alone or in combination with HMG-CoA reductase inhibitors in the treatment of hypercholesterolemia with low dosage and high compliance.

Topics: Animals; Bile Acids and Salts; Carrier Proteins; Cholesterol; Drug Design; Enterohepatic Circulation; Humans; Hypercholesterolemia; Hypolipidemic Agents; Ileum; Naphthols; Organic Anion Transporters, Sodium-Dependent; Symporters; Thiazepines