Colesevelam – a bile acid sequestrant for treating hypercholesterolemia and improving hyperglycemia

ABSTRACT

Introduction

Low density Lipoprotein cholesterol)LDL-C) levels show a clear relationship with cardiovascular disease (CVD). Statins are first line agents to reduce LDL-C and CVD risk. However, combination lipid-lowering therapy is often required to achieve large reductions in LDL-C.

Area covered

Colesevelam HCl is a bile acid sequestrant (BAS), which reduces LDL-C by 16–22% in monotherapy and adds a further 12–14% reduction in LDL-C when combined with other lipid-lowering drugs. Like statins, colesevelam reduces C-reactive protein levels by 16% in monotherapy and additional 6% when added to statins. Colesevelam also reduced HbA_1c by 4 mmol/mol (0.5%) when used alone and added to other hypoglycemic drugs in studies of patients with diabetes .

Expert Opinion

Bile acid sequestrants reduce LDL-C and HbA_1c and have some CVD outcome evidence. The uses of these agents are limited in patients with gastrointestinal disease or high triglycerides due to adverse effects on gut function and raising triglycerides and they interfere with the absorption of lipid-soluble drugs. Colesevelam has a higher bile acid binding capacity, and fewer adverse effects than other BAS. Colesevelam may be useful as a third line agent for treatment of hypercholesterolemia with some additional specific benefits on glycemic control.

KEYWORDS:

• Colesevelam HCl
• bile acid sequestrant
• diabetes
• cardiovascular
• cholesterol

Conflicts of interest

A Viljoen has worked as site Principal Investigator in research studies and or/served as advisor for and or/received lecture fees from: Astra Zeneca, Boehringer Ingelheim, Daiichi Sankyo, Lilly, Napp, Novartis, Novo Nordisk, Regeneron, Sanofi, and Tosoh. A S Wierzbicki is a site clinical investigator for trials sponsored by Amgen, Biomarin, Regeneron and Akcea. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

A reviewer on this manuscript has disclosed that they have received research support from Boehringer Ingelheim for an investigator-initiated study evaluating the effects of empagliflozin on DNA and RNA oxidation. All other peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.