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Ezetimibe

(3R,4S)-1-(4-fluorophenyl)-
3-((3S)-3-(4-fluorophenyl)-3-hydroxypropyl)-4-
(4-hydroxyphenyl)-2-azetidinone
CAS number
163222-33-1
ATC code
C10AX09
Chemical formula C24H21F2NO3
Molecular weight 409.4
Bioavailability 35-65%
Metabolism Glucuronidation up to 90%
Elimination half life  ?
Excretion Biliary (78%) and renal (11%)
Pregnancy category C
Legal status  ?
Delivery Oral tablets 5, 10, 20 mg

Ezetimibe (IPA: [ɛˈzɛtɛmɪb]) (Zetia®, Ezemibe®, Ezetrol®) is an anti-hyperlipidemic medication. It acts by decreasing cholesterol absorption in the intestine. It is used together with statins (e.g. ezetimibe/simvastatin) to help lower cholesterol in patients who cannot be controlled on statins alone.

Ezetimibe binds to Niemann-Pick C1 like 1 protein on the gastrointestinal tract epithelium. This protein is required to transport cholesterol into the cells; hence ezetimibe blocks absorption.

The complete prescribing information for Zetia can be found at http://www.zetia.com/ezetimibe/zetia/consumer/product_information/pi/index.jsp

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