Colesevelam hydrochloride: evidence for its use in the treatment of hypercholesterolemia and type 2 diabetes mellitus with insights into mechanism of action.

Colesevelam hydrochloride is a molecularly engineered, second-generation bile acid sequestrant demonstrating enhanced specificity for bile acids which has been approved for use as adjunctive therapy to diet and exercise as monotherapy or in combination with a β-hydroxymethylglutaryl-coenzyme A reductase inhibitor for the reduction of elevated low-density lipoprotein cholesterol in patients with primary hypercholesterolemia. It is also the only lipid-lowering agent currently available in the United States which has been approved for use as adjunctive therapy in patients with type 2 diabetes mellitus whose glycemia remains inadequately controlled on therapy with metformin, sulfonylurea, or insulin. With the recent emphasis upon drug safety by the Food and Drug Administration and various consumer agencies, it is fitting that the role of nonsystemic lipid-lowering therapies such as bile acid sequestrants - with nearly 90 years of in-class, clinically safe experience - should be reexamined.

Add-on therapy for hypercholesterolemia: a pilot comparison of two gastrointestinally-acting agents in statin-treated patients.

Background: Both colesevelam hydrochloride (colesevelam) and ezetimibe monotherapy have been reported to lower low-density lipoprotein cholesterol (LDL-C) approximately 15-17% in patients with hypercholesterolemia. When statin therapy is inadequate to reach desired LDL-C goals, the choice of add-on therapy, while multifactorial, must consider efficacy of additional LDL-C reduction.

Objective: To provide pilot study data in assessing the relative potential of ezetimibe or colesevelam to further reduce LDL-C in statin-treated patients.