Ezetimibe
Ezetimibe is a selective inhibitor of intestinal biliary and dietary
absorption of cholesterol due to interaction with Niemann-Pick C1-like 1
(NPC1L1) transporter protein located in the brush border of enterocytes
(41). The reduction in cholesterol content of chylomicrons and remnants
produces an increase of LDLr expression, thus reducing circulating LDL-C
concentration. Ezetimibe in monotherapy reduces LDL-C by 15-22% (42).
The overall impact of adding ezetimibe compared with statin monotherapy
was a 23% lower LDL-C (43). The IMPROVE-IT study showed that ezetimibe,
when added to a statin, reduced major cardiovascular events in patients
after suffering an acute coronary syndrome. In addition to proving its
safety, there was no increased risk of muscle or liver toxicity,
gallbladder lithiasis or cancer (19).