Ezetimibe lowers plasma LDL-chosterol by a mechanism distinct from statins. Its molecular target is:

• A Pancreatic lipase in the intestinal lumen
• B The LDL receptor on hepatocyte membranes
• C ACAT-2 esterification of cholesterol within enterocytes
• D NPC1L1, the cholesterol transporter at the enterocyte brush border ✓

Explanation

Ezetimibe selectively inhibits NPC1L1 (Niemann-Pick C1-like 1 protein) on the jejunal brush border, blocking uptake of both dietary and biliary cholesterol and reducing its delivery to the liver, which secondarily upregulates LDL receptors and clears more circulating LDL. Pancreatic lipase inhibition defines orlistat, ACAT inhibitors remain investigational, and ezetimibe does not interact directly with the LDL receptor. This complementary mechanism explains additive LDL lowering when combined with a statin.

Reference: Katzung's Basic and Clinical Pharmacology, 16th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.