CAS 163222-33-1

General Information

Ezetimibe belongs to a class of substances used to lower cholesterol levels in the blood. It has a distinct mechanism as a selective uptake inhibitor and can be used alone or in combination with statins or fenofibrate.


Therapy is indicated as an adjunct to diet. Ezetimibe is used to treat hyperlipidemia (increased levels of lipids in the blood, including cholesterol and triglycerides). Specifically, it is prescribed for primary hyperlipidemia (as monotherapy or with a statin); mixed perlipidemia, in combination with fenofibrate; homozygous familial hypercholesterolemia (HoFH), in combination with specific statins and other lipid-lowering treatments; and homozygous sitosterolemia.


Ezetimibe is orally administered alone or as a combination tablet with either simvastatin or atorvastatin.


Ezetimibe was approved in 2002 by the FDA, under the trade name Zetia. It is approved for use in the EU as Ezetrol and other trade names. It is produced through a multi-step chemical process.

About the API

Technology Synthetic Organic Chemistry
Therapeutic category Lipid lowering
Available formulations Oral Solid
Regulations Canada DMF Flag Canada DMF EU DMF Flag EU DMF Korea DMF Flag Korea DMF Other Flag Other US DMF Flag US DMF