A patient with moderate hypercholesterolemia inadequately controlled on a statin is given ezetimibe, which lowers LDL by approximately 15 to 20 percent further. Its molecular target is:

• A Pancreatic lipase in the intestinal lumen
• B ACAT-2, the enterocyte cholesterol esterification enzyme
• C ABCG5/G8 sterolin, the canalicular cholesterol efflux pump
• D NPC1L1, the intestinal cholesterol uptake transporter at the brush border ✓

Explanation

Ezetimibe selectively inhibits NPC1L1 (Niemann-Pick C1-like 1), the transporter that internalizes dietary and biliary cholesterol from the intestinal lumen into enterocytes. ABCG5/G8 mediates efflux back into the gut lumen and its gain of function causes sitosterolemia, the opposite direction of flux. Orlistat inhibits pancreatic lipase, and ACAT inhibitors were never approved for dyslipidemia.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.