Ezetimibe

Ezetimibe is a cholesterol-lowering drug that inhibits the NPC1L1 transporter, reducing absorption of cholesterol in the small intestine.

NPC1L1: NPC1L1 is a membrane protein that transports cholesterol and related sterols into intestinal cells. Ezetimibe lowers cholesterol absorption by inhibiting this transporter.
Hypercholesterolemia: Hypercholesterolemia is an elevated concentration of cholesterol in the blood. Ezetimibe is used to lower cholesterol in this condition.
Schering-Plough: Schering-Plough was a pharmaceutical company that developed and marketed ezetimibe. The company developed ezetimibe before its 2002 US approval.
PCSK9 inhibitor: PCSK9 inhibitors are drugs that increase LDL-receptor availability by blocking PCSK9, thereby lowering blood LDL cholesterol. They lower LDL by increasing clearance from blood, not by reducing intestinal cholesterol uptake.
Cholesterol absorption: Cholesterol absorption is the uptake of dietary and biliary cholesterol from the intestine into the body. It is the process ezetimibe directly reduces.
Ezetimibe/simvastatin: Ezetimibe/simvastatin is a fixed-dose combination that inhibits intestinal cholesterol absorption and hepatic cholesterol synthesis. Combining the drugs targets two distinct sources of circulating cholesterol.
Ezetimibe discovery: Ezetimibe discovery was the medicinal-chemistry program that produced a selective inhibitor of intestinal cholesterol absorption. This program yielded the drug’s distinctive transporter-targeting approach.
Bempedoic acid: Bempedoic acid is an oral drug that inhibits ATP citrate lyase, an enzyme involved in hepatic cholesterol synthesis. It reduces liver cholesterol production, unlike ezetimibe’s intestinal action.
Low-density lipoprotein: Low-density lipoprotein is a cholesterol-carrying particle that transports cholesterol through the bloodstream. Reduced intestinal uptake ultimately lowers circulating LDL cholesterol.
Familial hypercholesterolemia: Familial hypercholesterolemia is an inherited disorder causing markedly elevated LDL cholesterol from birth. Ezetimibe can supplement other treatment when inherited LDL elevation is difficult to control.

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