Selective intestinal cholesterol absorption inhibitor
ATC code: C10AX09 (Ezetimibe)
Selectively inhibits the NPC1L1 (Niemann-Pick C1-like 1) transporter on the small-intestine enterocyte brush border. Blocks absorption of dietary cholesterol and biliary sterols, without affecting triglyceride, fat-soluble vitamin, or bile acid uptake. Reduced cholesterol delivery to the liver upregulates receptors, increasing LDL clearance from blood. Lowers LDL by 17–20% as monotherapy and adds another 15–25% on top of a statin.
Second line
Preferred second-line agent when targets are not met on a maximum-tolerated statin under 2019. In IMPROVE-IT, adding ezetimibe to simvastatin after acute coronary syndrome reduced cardiovascular events by 6.4% over 7 years, confirming benefit of further LDL lowering. Dose 10 mg once daily with or without food. In statin-intolerant patients, ezetimibe monotherapy is used.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Ezetimibe is an intestinal cholesterol absorption inhibitor. It is prescribed in addition to a statin for hyperlipidemia and for secondary CV prevention ( 2019; IMPROVE-IT 2015 showed benefit when added to simvastatin after acute coronary syndrome). In healthy adults with normal lipid profile, ezetimibe is used for anti-aging protection against atherosclerosis. In people without confirmed hyperlipidemia or high CV risk, no clinical studies of prophylactic use exist. The drug is relatively safe but can cause myalgia, elevated liver enzymes, and diarrhea. If ezetimibe was prescribed at a normal lipid profile, consider seeking a second opinion.
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Safety not established. T1 use is not recommended. Lipid lowering is usually not a priority during pregnancy – stop statins and ezetimibe before conception.
No data on milk excretion. Use during lactation is not recommended.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Ezetimibe is evaluated for the following indications with varying evidence strength: Primary hypercholesterolemia (evidence tier A), Anti-aging and longevity (evidence tier F). See the full indication matrix with dosing and citations above on this page.
Common side effects of Ezetimibe (≥ 1 in 100): Diarrhea, Abdominal pain, Fatigue, Myalgia (less common than with statins). See the Safety section for uncommon and serious reactions.
FDA category C. Safety not established. T1 use is not recommended. Lipid lowering is usually not a priority during pregnancy – stop statins and ezetimibe before conception.
No data on milk excretion. Use during lactation is not recommended.
Ezetimibe is contraindicated in: Ezetimibe hypersensitivity; Active hepatic disease or unexplained transaminase elevation more than 3× ULN (when combined with a statin). Full list in the Safety section.