Drug intelligence / Profile preview

colesevelam + ezetimibe

Development stage
Unknown
Lead developer
Daiichi Sankyo
Modality
Small Molecules
Administration
Oral
01

Overview

**Colesevelam + ezetimibe** is a combination of two lipid-lowering agents used primarily in the management of hypercholesterolemia in patients who are intolerant to, or refuse, statin therapy. Colesevelam is a bile acid sequestrant that acts by binding bile acids in the intestine, thereby interrupting their reabsorption and promoting cholesterol conversion to bile acids in the liver. Ezetimibe is a cholesterol absorption inhibitor that blocks absorption of cholesterol at the intestinal brush border by inhibiting the Niemann-Pick C1-Like 1 (NPC1L1) protein. Used together, these agents produce an additive reduction in low-density lipoprotein cholesterol (LDL-C), with effects similar to those achieved by low-dose statin monotherapy. This combination has demonstrated a favorable safety profile and is particularly considered in statin-intolerant populations. However, this combination is considered an unlicensed indication in some regions and should be used cautiously and under medical guidance[1][2][4].

Other names
colesevelam and ezetimibe
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)

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