Drug intelligence / Profile preview

ezetimibe + other lipid-lowering medication(s)

Development stage
Unknown
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Ezetimibe is a small molecule cholesterol absorption inhibitor that selectively targets the Niemann-Pick C1 Like 1 (NPC1L1) protein in the enterocytes of the small intestine. By inhibiting this protein, it reduces the absorption of dietary and biliary cholesterol as well as plant sterols. In clinical practice, it is frequently administered as a combination therapy with other lipid-lowering medications, such as statins, to achieve additional LDL-C reduction. This specific combination regimen is indicated for adults with primary hyperlipidemia (including heterozygous familial hypercholesterolemia), homozygous familial hypercholesterolemia (HoFH), and homozygous sitosterolemia. Organon and Co. (specifically its subsidiary Organon LLC) is the developer of Zetia (ezetimibe).

Brand names
Zetia
Other names
ezetimibe combination therapy
02

Targets

NPC1L1 (Niemann-pick C1-Like 1 transporter)

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