Therapy is often required to manage the hyperglycemia, hypertension, and dyslipidemia that occur in patients with type 2 diabetes mellitus (T2DM) in order to control the risk of cardiovascular (CV) events. The importance of managing these risk factors is underscored by the recommendation from the American Diabetes Association and the American Association of Clinical Endocrinologists for treatment of these CV risk factors to target levels. However, relatively few patients achieve simultaneous control of these risk factors. As such, therapy that has positive effects on more than 1 risk factor is of potential benefit. Initially approved as a lipid-lowering agent, the bile acid sequestrant colesevelam hydrochloride (HCl) is now also approved as an adjunct therapy to improve glycemic control in patients with T2DM. This review summarizes the major findings of clinical studies that investigated the glucose-and lipid-lowering effects of colesevelam HCl when added to stable metformin-, sulfonylurea-, or insulin-based antidiabetes therapies in patients with T2DM.