The bile acid-binding resins cholestyramine (CH) and colestipol (CO) are effective drugs for the treatment of patients with elevated low-density lipoprotein (LDL) cholesterol plasma concentrations without concurrent hypertriglyceridemia. Since the bile acid sequestrants are not absorbed in the gastrointestinal tract, they cannot cause direct systemic side effects. They activate the natural pathway for LDL elimination from the circulation by stimulating the expression of LDL receptors. Thus, the sequestrants are ideal drugs for treatment of LDL hypercholesterolemia from the pharmacologist’s point of view. However, their mode of administration as a bulky powder and the gastrointestinal side effects may cause practical problems.