Ezetimibe (Zetia) blocks the NPC1L1 transporter at the intestinal brush border, reducing cholesterol absorption.
Mechanism — Reduces dietary and biliary cholesterol uptake by ~50%. The liver compensates by upregulating LDL receptors, lowering plasma LDL by ~15-20%. Stacks additively with statins.
Use case — Add-on when statin alone is insufficient, statin-intolerant patients, or those preferring lower statin doses. Typical 10 mg/day.
Caveats — Effect alone is modest. Excellent tolerability profile — one of the best in the lipid-lowering class. Pair with bempedoic acid for statin-free regimens in intolerant patients.