The use of colesevelam hydrochloride in the treatment of dyslipidemia: a review

Bile-acid sequestrants augment cholesterol excretion via enhanced conversion to bile acids, and act to lower low-density lipoprotein cholesterol (LDL-C), especially when combined with other cholesterol-lowering drugs. Colesevelam hydrochloride (HCL) has become the preferred drug of this class due to fewer gastrointestinal adverse effects. This article reviews the use of colesevelam in the treatment of dyslipidemia. Bile-acid sequestrants are a class of drugs developed to lower LDL-C levels. Two of the bile-acid sequestrants, colestyramine resin and colestipol, have been used since the 1980s, and have proven effective and safe as nonsystemic approaches to cholesterol reduction. However, tolerability and compliance issues related to palatability and gastrointestinal side effects have limited the use of these sequestrants. Colesevelam HCL (Daiichi Sankyo, Inc., Parsippany, NJ) is a nonabsorbed lipid-lowering agent that can be used in monotherapy or in combination with an HMG-CoA reductase inhibitor to reduce LDL-C in patients with primary hypercholesterolernia (Fredrickson type Ila). This article reviews the clinical efficacy and use of colesevelam HCL for the management of clyslipidemia.