Ezetimibe
ez-ET-i-mibe
Category
Compound type
Phase / Status
FDA approved for hypercholesterolemia
Standard Dose
Daily
Half-life
Plasma elimination
Route(s)
Oral
Research Stage
Regulatory approval granted; post-market monitoring ongoing.
Overview
Ezetimibe works in the gut by blocking uptake of dietary and biliary cholesterol, which can lower LDL levels over time. Because it has limited systemic exposure, it's often well tolerated. Treatment choice should still be individualized based on cardiovascular risk, other medications, and any liver-related considerations.
Plain-language summary
Ezetimibe works in the gut by blocking uptake of dietary and biliary cholesterol, which can lower LDL levels over time. Because it has limited systemic exposure, it's often well tolerated. Treatment choice should still be individualized based on cardiovascular risk, other medications, and any liver-related considerations.
Administration Routes
- Oral
Also known as
Mechanisms
Cholesterol absorption inhibitor
Detailed mechanism
Selective inhibitor of Niemann-Pick C1-Like 1 (NPC1L1) protein, which is involved in intestinal absorption of cholesterol and related phytosterols.
Safety
Side effects
- Mild GI upset
- Headache
- Fatigue
- Diarrhea
Reported benefits
- Lowers LDL by 18-25%
- No muscle side effects
- Good with statins
- Well tolerated
Safety profile
Well-tolerated with minimal side effects. Can be used alone or in combination with statins.
Clinical trials
Completed clinical trials leading to FDA approval for hypercholesterolemia.
Structure
Verified structure
Ezetimibe
Exact 2D structure can be rendered from a PubChem-backed canonical SMILES string.
- Chemical Formula
- C24H21F2NO3
- Molecular Weight
- 388.96 g/mol
- CAS Number
- 163222-33-1
- InChIKey
- OLNTVTPDXPETLC-XPWALMASSA-N
Stack Context
Stacks with
References
- 1View source
Ezetimibe added to statin therapy after acute coronary syndromes (IMPROVE-IT, NEJM)
2015
- 2View source
Ezetimibe coadministered with atorvastatin in 628 patients with primary hypercholesterolemia (Am J Cardiol)
2003
- 3View source
The effects of lowering LDL cholesterol with simvastatin plus ezetimibe in patients with chronic kidney disease (SHARP, Lancet)
2011
This profile summarizes research literature for education only. It is not medical advice, and it does not diagnose, treat, or recommend a dose. Consult a qualified professional before changing a protocol.