A patient with isolated elevation of LDL despite maximally tolerated statin therapy is started on ezetimibe, after which LDL-C falls further. The molecular target of ezetimibe is:
- A Microsomal triglyceride transfer protein
- B ABCG5/ABCG8 sterolin heterodimer
- C NPC1L1 transporter at the enterocyte brush border ✓
- D Hepatic ACAT2
Correct answer: C. NPC1L1 transporter at the enterocyte brush border
Explanation
Ezetimibe selectively inhibits NPC1L1, the Niemann-Pick A1-Like 1 cholesterol uptake transporter on the jejunal brush border, blocking dietary and biliary cholesterol absorption without affecting triglyceride or fat-soluble vitamin uptake. MTP inhibition is the mechanism of lomitapide, ABCG5/8 mediates sterol efflux back into the lumen and is defective in sitosterolemia, and ACAT2 inhibitors are not established drugs.
Reference: Katzung's Basic and Clinical Pharmacology, 16th ed.
High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP
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