Biochemistry · Lipid Metabolism (Fatty Acid Synthesis and Oxidation, Lipoproteins, Cholesterol)

A patient with mixed dyslipidemia is prescribed ezetimibe. The drug lowers LDL cholesterol primarily by:

  • A Blocking the NPC1L1 transporter at the jejunal brush border, reducing cholesterol absorption
  • B Inhibiting microsomal triglyceride transfer protein in enterocytes
  • C Activating PPAR-alpha to increase lipoprotein lipase activity
  • D Binding bile acids in the gut lumen and interrupting enterohepatic circulation
Correct answer: A. Blocking the NPC1L1 transporter at the jejunal brush border, reducing cholesterol absorption

Explanation

Ezetimibe selectively inhibits NPC1L1, the canalicular-like transporter at the jejunal brush border responsible for dietary and biliary cholesterol uptake, cutting absorption by about half and lowering LDL modestly. Option B describes lomitapide, option C describes fibrates, and option D describes resins such as cholestyramine. Each distractor maps exactly to another lipid-lowering class, testing precise drug-target pairing.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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