A patient intolerant of statins is prescribed ezetimibe for hypercholesterolemia. At which site does ezetimibe exert its lipid-lowering effect?

• A Pancreatic lipase in the intestinal lumen
• B NPC1L1 transporter at the enterocyte brush border ✓
• C ABCG5/G8 sterol exporter at the canalicular membrane
• D ACAT2-mediated esterification within the enterocyte

Explanation

Ezetimibe selectively inhibits the Niemann-Pick C1-like 1 (NPC1L1) protein on the jejunal brush border, blocking dietary and biliary cholesterol uptake into enterocytes and lowering LDL by roughly 15 to 20 percent. Orlistat inhibits pancreatic lipase, ABCG5/G8 mediates biliary sterol efflux, and ACAT2 esterifies absorbed cholesterol intracellularly, but none of these is the ezetimibe target, eliminating options A, C, and D.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

Written and medically reviewed by the StethoPrep medical team.