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Avasimibe is an investigational acyl-CoA cholesterol acyltransferase (ACAT) inhibitor that was studied as a lipid-lowering and anti-atherosclerotic agent.
- Lowered triglycerides and VLDL cholesterol in early clinical trials
- Reduced foam cell formation in laboratory models of atherosclerosis
Overview
It lowered blood lipids nicely in early trials but didn't actually slow artery plaque buildup, which is why it never made it to market.
Mechanism
Avasimibe inhibits ACAT, the intracellular enzyme that esterifies free cholesterol for storage and lipoprotein assembly. By blocking ACAT in the liver and intestine it reduces secretion of apolipoprotein B-containing lipoproteins (VLDL and LDL); in macrophages it limits foam cell formation by reducing uptake of modified LDL and enhancing free cholesterol efflux.
receptor fingerprint
ACAT (acyl-CoA cholesterol acyltransferase)Inhibitor
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
Early trials in combined hyperlipidemia reported avasimibe was generally tolerated across a 50 to 500 mg/day dose range, with meaningful reductions in triglycerides and VLDL cholesterol. The A-PLUS trial, however, found it did not favorably affect coronary atherosclerosis progression on intravascular ultrasound, and plaque burden trended slightly worse than placebo; this halted its cardiovascular development.
Subjective profileweighing the evidence above
A historical entry with nothing to recommend it. It lowered triglycerides in early trials, but the study that mattered found coronary plaque trending slightly worse than placebo, which ended its development. There is no reason to want it now.
Resources
This entry is here for reference.
Research
- 1.Pharmacology of the ACAT inhibitor avasimibe (CI-1011)
- 2.Efficacy and short-term safety of a new ACAT inhibitor, avasimibe, on lipids, lipoproteins, and apolipoproteins, in patients with combined hyperlipidemia
2 listed here; entry last updated July 2026
Reviews
My notesprivate to this device
FAQ
What is Avasimibe used for?
It was studied as a lipid-lowering drug intended to treat high cholesterol and slow atherosclerosis (artery plaque buildup).
How does Avasimibe work?
It blocks the ACAT enzyme, which normally packages cholesterol for storage and transport, reducing harmful lipoprotein secretion and limiting cholesterol buildup in artery-wall cells.
Is Avasimibe well-researched?
It went through multiple human trials, including a large atherosclerosis-imaging study, but that study found no cardiovascular benefit, so research on it stopped.
Limitations of the evidence
- Did not slow coronary plaque progression in the A-PLUS trial
- Development for cardiovascular disease was discontinued