Ezetimibe Research Reference

Catalog classification, reference sizes, lab math links, and source-backed data. Educational use only — not medical advice.

Researched for: PepTools vendor-neutral scientific reference catalog

Dietary cholesterol absorption inhibitor; lipid-lowering agent compound Reference approved

Also known as: Zetia, Ezetrol

Quick Facts

Reference Sizes
10 mg oral tablet
Solubility
Virtually insoluble in aqueous media suitable for injection.

Catalog Description

Ezetimibe is a beta-lactam and organofluorine compound classified pharmacologically as a dietary cholesterol absorption inhibitor. It acts at the intestinal brush border by targeting NPC1L1, reducing absorption of dietary and biliary cholesterol and related phytosterols. Ezetimibe is used clinically alone or with other lipid-lowering therapies as an adjunct to dietary therapy for approved hyperlipidemia-related indications.

Catalog descriptions reflect research context only. Not a medical claim or treatment recommendation.

Research Profile

Half-Life
Approximately 22 hours for ezetimibe and approximately 22 hours for ezetimibe-glucuronide.
Administration Routes (Research)
oral

Reported Research Effects

Data source: Primary literature, regulator records, trial registries, and identity-specific evidence search

Reflects preclinical/research literature context only. Not a medical claim, dosing instruction, or treatment recommendation.

Research Notes

The approved oral tablet strength identified in U.S. labeling is 10 mg. Clinical labeling describes oral administration and formation of the active phenolic glucuronide metabolite; these details are provided as neutral reference information and are not individualized dosing guidance. Direct molecular-target evidence identifies NPC1L1 as the ezetimibe-sensitive cholesterol-absorption pathway target.

Supplementary research context only. Not medical advice or a treatment recommendation.

Registry Identifiers

CAS RN 163222-33-1; PubChem CID 150311; molecular formula C24H21F2NO3; molecular weight 409.4 g/mol; IUPAC name (3R,4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-hydroxyphenyl)azetidin-2-one

Source-Backed Observations

The pharmacologically active ezetimibe-glucuronide is the major circulating metabolite. Plasma concentration-time profiles show multiple peaks consistent with enterohepatic recycling. Ezetimibe and ezetimibe-glucuronide are highly bound to human plasma proteins.

Reflects published research. Educational reference — not a recommendation for use.

Sources

Ezetimibe Compound Summary, PubChem CID 150311
https://pubchem.ncbi.nlm.nih.gov/compound/Ezetimibe (accessed 2026-09-07)
ZETIA (ezetimibe) Prescribing Information
https://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=174e45e0-45bb-48b7-9e60-8f6cfc1d22bb (accessed 2026-09-07)
VYTORIN (ezetimibe and simvastatin) FDA Label
https://www.accessdata.fda.gov/drugsatfda_docs/label/2024/021687s066lbl.pdf (accessed 2026-09-07)
The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1)
https://pubmed.ncbi.nlm.nih.gov/15928087/ (accessed 2026-09-07)

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Related Research Articles

Published articles on this site that mention Ezetimibe or one of its catalog aliases.

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Research Use Only. All content is for educational and research reference only. Not medical advice, a treatment recommendation, or guidance on human use. Compounds are not FDA-approved drugs unless specifically noted.

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