Ezetimibe

Category: pharmacological

Aliases: Zetia, Ezetrol

Pharmacological Mechanism

Inhibits Niemann-Pick C1-like 1 (NPC1L1) at the intestinal brush border → blocks dietary cholesterol + phytosterol absorption. Non-statin mechanism → additive LDL reduction when combined with statin. IMPROVE-IT trial established CV benefit of ezetimibe-statin combination.

Half-Life (t½)

PO: 24.3h

Dosing Guidelines

• PO: Typical 10 mg (Range: 10–10 mg)

Target Organ Systems

• cardiovascular
• digestive

Interactions

• Atorvastatin / statins (synergistic): Additive LDL reduction; many combination products (Vytorin = simvastatin + ezetimibe).

Pathways It Modulates

• Atherosclerosis plaque pathology (inhibitor) — NPC1L1 (intestinal cholesterol absorption)
• Cholesterol absorption + reverse transport (inhibitor) — NPC1L1 — intestinal cholesterol absorption (~50% reduction); additive to statins
• LDL receptor + PCSK9 axis (inhibitor) — NPC1L1 (intestinal cholesterol absorption)

Chemical Identifiers

• PubChem CID: 150311
• Formula: C24H21F2NO3
• Molecular weight: 409.43 g/mol
• InChIKey: OLNTVTPDXPETLC-XPWALMASSA-N
• SMILES: C1=CC(=CC=C1[C@@H]2[C@H](C(=O)N2C3=CC=C(C=C3)F)CC[C@@H](C4=CC=C(C=C4)F)O)O

References

• PMID 15871634