What is the primary mechanism of ezetimibe?

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Multiple Choice

What is the primary mechanism of ezetimibe?

The mechanism hinges on blocking intestinal cholesterol uptake. Ezetimibe inhibits the NPC1L1 transporter on the enterocytes at the brush border, preventing dietary and biliary cholesterol from entering the gut cells. With less cholesterol reaching the liver, hepatic cholesterol content falls, which signals the liver to upregulate LDL receptors and pull more LDL from the bloodstream, lowering plasma LDL-C. This is distinct from statins, which inhibit HMG-CoA reductase, and from bile acid sequestrants, which prevent reabsorption of bile acids. Used with or without a statin, ezetimibe provides additional LDL lowering by reducing intestinal cholesterol absorption.

The mechanism hinges on blocking intestinal cholesterol uptake. Ezetimibe inhibits the NPC1L1 transporter on the enterocytes at the brush border, preventing dietary and biliary cholesterol from entering the gut cells. With less cholesterol reaching the liver, hepatic cholesterol content falls, which signals the liver to upregulate LDL receptors and pull more LDL from the bloodstream, lowering plasma LDL-C. This is distinct from statins, which inhibit HMG-CoA reductase, and from bile acid sequestrants, which prevent reabsorption of bile acids. Used with or without a statin, ezetimibe provides additional LDL lowering by reducing intestinal cholesterol absorption.

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