Ezetimibe
Metabolic Health · NPC1L1 inhibitor
Also known as: Zetia
Tier A+
Bottom line
Read Off Label grades Ezetimibe as A+ (8.4/10) based on strong evidence, moderate benefit magnitude, and a very low-risk safety profile.
Generic, inexpensive, exceptionally well-tolerated.
Typical use: 10 mg PO daily — Rx.
What this is
Generic, inexpensive, exceptionally well-tolerated. Should be first-line add-on when statin monotherapy is insufficient. Often underused. IMPROVE-IT 2015 established CV benefit of ezetimibe-on-statin in post-ACS.
Mechanism
Inhibits Niemann-Pick C1-like 1 transporter at intestinal brush border; reduces dietary and biliary cholesterol absorption; ~15-20% LDL reduction as monotherapy; synergistic with statins
Dose & route
10 mg PO daily
Citations
- https://pubmed.ncbi.nlm.nih.gov/26039521/
- https://pubmed.ncbi.nlm.nih.gov/23470236/
- https://pmc.ncbi.nlm.nih.gov/articles/PMC5363762/
- https://doi.org/10.1007/s40261-026-01559-7
Links go to the source. If a link is dead or you want something re-checked, let me know.
Common questions
- Does Ezetimibe work?
- Read Off Label rates the evidence for Ezetimibe as Strong and the benefit magnitude as moderate, producing an overall grade of A+ (8.4/10). Generic, inexpensive, exceptionally well-tolerated.
- Is Ezetimibe safe?
- Ezetimibe has a very low risk profile in published human data. Legal status: Rx (generic). This is not medical advice — see the disclaimer.
- What is the typical dose for Ezetimibe?
- 10 mg PO daily
- How does Ezetimibe work?
- Inhibits Niemann-Pick C1-like 1 transporter at intestinal brush border; reduces dietary and biliary cholesterol absorption; ~15-20% LDL reduction as monotherapy; synergistic with statins
This is an independent synthesis of published research by a non-clinician. Scores are opinions supported by citations, not prescriptions. See the full disclaimer and methodology for how this score was produced and what it does and doesn't mean.