Ezetimibe · Zetia, MK0653

What is Ezetimibe?

Ezetimibe is a small-molecule inhibitor of the sterol transporter NPC1L1 at the intestinal brush border. It reduces blood cholesterol by blocking intestinal cholesterol and phytosterol absorption, decreasing hepatic cholesterol stores and increasing LDL receptors.

Summary written with AI from the sources listed at the end of this page.

At a glance

Also known as

Zetia, MK0653, NSC-758923, SCH-58235

Drug type

Small molecule

Targets

Niemann-Pick C1-Like 1 (NPC1L1)

Mechanism

Inhibitor of Niemann-Pick C1-Like 1 (NPC1L1)

Pathways

cholesterol absorption, LDL receptor upregulation

Therapy area

Metabolic

Developer

Organon Llc

In trials of

AZN

FDA status

Approved as Zetia, NDA021445 · FDA label

UNII

EOR26LQQ24

✅ FDA-approved uses

• Primary hyperlipidemia, including heterozygous familial hypercholesterolemia (HeFH)
• Heterozygous familial hypercholesterolemia (HeFH) in pediatric patients 10 years and older
• Mixed hyperlipidemia
• Homozygous familial hypercholesterolemia (HoFH)
• Homozygous familial sitosterolemia

From the indications section of the FDA label (version of Nov 25, 2025). Read the full label for the exact wording, limitations and safety information.

🧪 Clinical trials

Trials of the companies BioRadar tracks, from ClinicalTrials.gov, most advanced phase first.

Conditions studied

Healthy Participants

Sources

• FDA label (DailyMed)
• FDA label Zetia (2025-11-25), indications
• ClinicalTrials.gov NCT07622433

Updated Oct 3, 2026.