Ezetimibe (also known as Ezetrol, SCH 58235) is a cholesterol absorption inhibitor for lowering plasma cholesterol levels. It inhibits intestinal cholesterol absorption by preventing cholesterol uptake by the Niemann-Pick C1-like 1 (NPC1L1) protein, a cholesterol transporter located in the apical membrane of enterocytes.
Comparison of the activity and disposition of the novel cholesterol absorption inhibitor, SCH58235, and its glucuronide, SCH60663.
The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1).
Regulation of intestinal cholesterol absorption.