Last reviewed 2026-04-20 · How we verify

Zetia (EZETIMIBE)

Zetia works by blocking the absorption of cholesterol in the small intestine.

Zetia (ezetimibe) is a small molecule dietary cholesterol absorption inhibitor that targets the Niemann-Pick C1-like protein 1. It is used to treat various lipid disorders, including familial hypercholesterolemia, hypercholesterolemia, and mixed hyperlipidemia. Originally developed by MSD INTL GMBH, Zetia is now owned by Organon and was FDA-approved in 2002. The drug has a half-life of 22 hours and is available as a generic medication from multiple manufacturers. Key safety considerations include monitoring liver function and potential interactions with other medications.

At a glance

Mechanism of action

Ezetimibe reduces blood cholesterol by inhibiting the absorption of cholesterol by the small intestine. In 2-week clinical study in 18 hypercholesterolemic patients, ezetimibe inhibited intestinal cholesterol absorption by 54%, compared with placebo. Ezetimibe had no clinically meaningful effect on the plasma concentrations of the fat-soluble vitamins A, D, and (in study of 113 patients), and did not impair adrenocortical steroid hormone production (in study of 118 patients).The cholesterol content of the liver is derived predominantly from three sources. The liver can synthesize cholesterol, take up cholesterol from the blood from circulating lipoproteins, or take up cholesterol absorbed by the small intestine. Intestinal cholesterol is derived primarily from cholesterol secreted in the bile and from dietary cholesterol. Ezetimibe has mechanism of action that differs from those of other classes of cholesterol-reducing compounds (statins, bile acid sequestrants

Approved indications

• Familial hypercholesterolemia - heterozygous
• Familial hypercholesterolemia - homozygous
• Hypercholesterolemia
• Hyperlipidemia
• Mixed hyperlipidemia
• Sitosterolemia

Common side effects

• Upper respiratory tract infection
• Diarrhea
• Arthralgia
• Sinusitis
• Pain in extremity
• Nasopharyngitis
• Myalgia
• Alanine aminotransferase increased
• Fatigue
• Influenza
• Headache
• Aspartate aminotransferase increased

Drug interactions

• gemfibrozil

Key clinical trials

• A Study to Evaluate the Efficacy and Safety of Enlicitide (MK-0616, Oral PCSK9 Inhibitor) Compared With Ezetimibe or Bempedoic Acid or Ezetimibe and Bempedoic Acid in Adults With Hypercholesterolemia (MK-0616-018/CORALreef AddOn) (PHASE3)
• A Prospective, Open, Observational Study to Confirm the Lipid-lowering Effect, Changes in Glucose Metabolism, and Safety After 6 Months of Administration of Atostazet to Hypercholesterolemic Patients 65 Years of Age or Older
• Treatment With Bempedoic Acid and/or Its Fixed-dose Combination With Ezetimibe in Primary Hypercholesterolemia or Mixed Dyslipidemia
• A Study of Bempedoic Acid/Ezetimibe/High-intensity Statin in Patients Without Cardiovascular Events (PHASE3)
• Cholesterol Disruption in Combination With the Standard of Care in Patients With Advanced Pancreatic Adenocarcinoma (EARLY_PHASE1)
• Intensive Cholesterol-Lowering and CD8+ T Cells in Prostate Cancer (PHASE2)
• Moderate-intensity Statin vs. Individualized LDL-C Target-based Therapy in Older Adults With Type 2 Diabetes (iTARGET-Elderly Study) (NA)
• A Study to Evaluate the Effect of Obicetrapib/Ezetimibe 10 mg Fixed-Dose Combination or Obicetrapib 10 mg Daily on Top of Guideline-Recommended Lipid-Lowering Therapy in Participants With Type 2 Diabetes and/or Metabolic Syndrome (PHASE3)

Patents

Primary sources

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