Columbia Technology Ventures

Cardiovascular disease treatment by PEGylated high-density lipoprotein particles

Atherosclerosis, a cardiovascular disease characterized by plaque in the arteries, is the leading cause of mortality in industrialized nations. Lipid abnormalities are one of the key risk factors for this disease, and drugs that modify lipids are widely used to reduce the risk of cardiovascular events. While high-density lipoproteins (HDL) such as human apolipoprotein A-I (apoAI) have the potential to be a strong therapeutic agent for cardiovascular disease, they also cause adverse biological effects if administered in large quantities. This technology is a new method for obtaining a form of human apoA-I that exhibits increased half-life in plasma and preserves its biological activity, reducing the adverse effects seen in other agents. This new form of human apoA-I may provide a new, more potent therapeutic treatment for atherosclerosis and cardiovascular disease that is safer and more effective than existing options.

PEGylation of high-density lipoprotein particles increases half-life while maintaining biological activity

This technology increases the specificity and efficiency of PEGylation of HDL producing a homogenous product. By PEGylating HDL using this method, the resulting particle has an increased potency towards apolipoprotein therapy. This technology produces a novel form of HDL particles that have an increased half-life in blood plasma. In addition, no reduction in biological activities, such as promotion of cholesterol efflux, is observed using these HDL particles. This has been demonstrated by experiments performed in labeled murine macrophage-like RAW cells with cholesterol tracers. In addition, it has been found that the PEGylated apoA-I has an increased half-life in vivo of approximately 24 hours. PEGylated apoA-I remained in blood plasma after a period of 3 days.

Lead Inventor:

Alan Tall, M.D.

Applications:

  • A therapeutic treatment of atherosclerosis and cardiovascular diseases
  • A method for targeted PEGylation of biological molecules

Advantages:

  • Specific and efficient PEGylation
  • HDL particles with increased half-life in blood plasma
  • No decrease in biological activity of the HDL particles

Patent Information:

Patent Issued (WO/2012/135046)

Tech Ventures Reference: IR 2911

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