AGI-1067, a novel vascular protectant, anti-inflammatory drug and mild antiplatelet agent for treatment of atherosclerosis

Victor L. Serebruany, Alex Malinin, Christian Eisert, Stephen Ong

Research output: Contribution to journalArticlepeer-review

Abstract

Oxidation-sensitive signals play an important role in platelet activation. AGI-1067 is a novel, phenolic, intra- and extracellular antioxidant that inhibits the expression of a number of proinflammatory genes involved in atherosclerosis. AGI-1067 is the metabolically stable monosuccinic acid ester of probucol, and a potent phenolic antioxidant representing a novel class of orally bioavailable compounds termed vascular protectants. AGI-1067 exhibits antioxidant activity equipotent to probucol. In addition, animal studies have demonstrated dual pharmacological activities of AGI-1067: the ability to block the expression of oxidation-sensitive inflammatory genes including genes that code for vascular cell adhesion molecule-1 and monocyte chemotactic protein-1. Importantly, AGI-1067 also exhibits mild antiplatelet properties inhibiting surface expression of various key platelet receptors, the formation of platelet monocyte microparticles and PAR-1 thrombin receptors. AGI-1067 is currently being tested in the late trials, and if proven to improve clinical outcomes (ARISE trial), the drug will ultimately be used in patients with different manifestations of atherosclerosis and atherothrombosis.

Original languageEnglish (US)
Pages (from-to)635-641
Number of pages7
JournalExpert Review of Cardiovascular Therapy
Volume5
Issue number4
DOIs
StatePublished - Jul 2007
Externally publishedYes

Keywords

  • AGI-1067
  • Anti-inflammatory
  • Antioxidant
  • Antiplatelet
  • Atherosclerosis
  • Clinical trial
  • Vascular protectant

ASJC Scopus subject areas

  • Cardiology and Cardiovascular Medicine

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