AGI-1067: a novel vascular protectant for prevention of restenosis

Ann Pharmacother. 2006 Jan;40(1):66-73. doi: 10.1345/aph.1G142. Epub 2005 Nov 22.


Objective: To review the synthesis, pharmacology, clinical trials, and adverse effects of AGI-1067, a novel agent for preventing restenosis.

Data sources: Literature searches were conducted using MEDLINE (1966-July 2005) and International Pharmaceutical Abstracts (1970-July 2005) for English-language articles containing the search terms AGI-1067, AGI 1067, and probucol. In addition, bibliographies from relevant articles were reviewed for additional references.

Study selection and data extraction: All articles identified from data sources were reviewed for relevant information. Applicable information was included in this review.

Data synthesis: AGI-1067, a derivative of the lipid-lowering agent probucol, is the first of a new class of drugs termed vascular protectants. It has antioxidant and lipid-lowering effects. In addition, it inhibits inflammatory processes without resultant immunosuppression through its selective inhibition of vascular cell adhesion molecule-1 expression. AGI-1067 also exhibited anti-atherosclerotic effects in preclinical studies. Relatively short-term treatment with AGI-1067 showed positive results compared with probucol in preventing restenosis in patients undergoing percutaneous coronary intervention. AGI-1067 appears to be well tolerated and holds important advantages over probucol in that it has fewer adverse effects on high-density lipoprotein cholesterol and the QT interval.

Conclusions: The favorable safety profile of AGI-1067 offers potential advantages over its precursor, probucol. Preclinical and clinical studies indicate that it possesses antioxidant, antiinflammatory, and lipid-lowering properties. Ongoing Phase II and III studies will determine AGI-1067's place in therapy for the prevention of restenosis and reduction in cardiovascular events in patients undergoing percutaneous intervention for coronary atherosclerosis.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Antioxidants / chemistry
  • Antioxidants / pharmacology
  • Antioxidants / therapeutic use
  • Clinical Trials as Topic
  • Coronary Restenosis / drug therapy
  • Coronary Restenosis / prevention & control*
  • Drugs, Investigational / pharmacology
  • Drugs, Investigational / therapeutic use
  • Humans
  • Molecular Structure
  • Probucol / analogs & derivatives*
  • Probucol / chemistry
  • Probucol / pharmacology
  • Probucol / therapeutic use


  • Antioxidants
  • Drugs, Investigational
  • succinobucol
  • Probucol