Blocks the intestinal sterol transporter NPC1L1, reducing cholesterol absorption. Source
Adults with primary hyperlipidemia
Study contextSelected approval record (2002-10-25): FDA approved ezetimibe as Zetia for lipid lowering.
Status sourceStatus & indicationsLDL-C: 18% reduction within arm · 12 weeks
Pooled monotherapy trials · regulatory-label · 10 mg daily · Mean change from untreated baseline; two trials pooled.
Evidence & limitationsLabel risks include hypersensitivity, muscle injury and liver enzyme elevation, especially with a statin.
Safety contextA next milestone is not summarized for this therapy.
Milestone detailsStudy results apply to their own population, dose and analysis. They do not establish a ranking between therapies.
Each result belongs to its own study population, dose and analysis. Open a result for its chart, comparator, safety findings and limitations.
LDL-C: 18% reduction within arm · 12 weeks
10 mg daily
Adults with primary hyperlipidemia
Mean change from untreated baseline; two trials pooled.
Label risks include hypersensitivity, muscle injury and liver enzyme elevation, especially with a statin.
Limitations: Monotherapy result; adding ezetimibe to an existing statin is a different baseline comparison.
Status in this atlas: Selected approval record (2002-10-25): FDA approved ezetimibe as Zetia for lipid lowering. Status source
Blocks the intestinal sterol transporter NPC1L1, reducing cholesterol absorption.
Mechanism sourceMechanism & side effects: Ezetimibe
Uses, doses and availability depend on the formulation, indication and country. Study doses below describe research; they are not prescribing instructions.
Chemical structure of ezetimibe.
Shown: Neutral ezetimibe parent molecule.
The parent drug is shown; its glucuronide metabolite is not included. The optional 3D view is a computed PubChem conformer, not an experimentally measured or protein-bound shape.
PubChem CID 150311Ezetimibe · compound history across indications
Selected sourced milestones, not a complete development history. Dates distinguish study starts, publications, announcements and approvals; the first listed date is not necessarily when development began.
Two placebo-controlled studies evaluated the cholesterol-absorption inhibitor then known as SCH 58235 and helped establish the 10 mg dose.
Bays et al. — ezetimibe phase 2 studiesFDA approved ezetimibe as Zetia for lipid lowering.
FDA — original Zetia approval letterAdding ezetimibe to simvastatin did not significantly improve carotid artery wall-thickness progression despite greater LDL-C lowering. This was an imaging outcome, not a cardiovascular-event trial.
ENHANCE — NEJMAdding ezetimibe to simvastatin reduced the cardiovascular composite after acute coronary syndrome. This supports the combination in that setting, not ezetimibe monotherapy; the trial is plotted on the outcomes page.
IMPROVE-IT — NEJMSelected sources checked Sep 14, 2026. This is not an exhaustive history.
