Biomedical, Engineering and physical science

Anticoagulant Intellectual Property Portfolio Sulfated Heparin Mimetics

The technology

Market need

The current treatment and prevention of thromboembolic diseases, Heparin, has numerous disadvantages. Heparins usually consist of a heterogeneous mixture, and thus contain many additional ingredients which result in a variety of side effects. Concern has also arisen with the purity and safety of the supply of heparin. Additionally, heparins are highly sulfated molecules, and thus highly hydrophilic and result in poor bioavailability. Some of the side effects observed with heparin usage are thrombocytopenia, osteoporosis, as well as concern if the dosage is incorrect and the patient is overdosed. There is a clinical need for a new anticoagulant with heparin-like activity without the many potentially lethal side effects currently observed with its use.

Technology summary

Nonpathogenic Bacteria Derived – Developed process for making low molecular weight heparosan and cleaving enzymes.

Chemically Derived – Chemically synthesized sulfated low molecular weight lignins that shows potent anticoagulant activity both in vitro and ex vivo were synthesized.

Factor XIa inhibitors – These small molecules may be the most promising group of direct inhibitors. The developed molecules include sulfated gallic acids, sulfated inositol analogs, and sulfated quinazolinones. These compounds act via an entirely new allosteric mechanism, providing higher efficacy and safety.

Technology status

In-vitro and ex vivo studies demonstrate efficacy

Publications:

More publications can be found on Dr. Desai’s webpage

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Benefits:

  • Reversible with existing FDA approved drug
  • Easily synthesized- inexpensive to make-no animal sources
  • Novel mechanism of action
    • Reduced side effects, Low cellular toxicity
    • Targets Factor Xia-proposed to be a very safe target
  • Can be given orally and IV
  • Reduced patient response variability

Applications:

  • Therapy for thromboembolic disease and cardiovascular disease
  • Anticoagulant
  • Anti-thrombosis treatment during surgery
  • Coatings for stents, tubes and other devices
  • Some formulations may also be:
    • Possible cancer therapeutic
    • Possible anti-herpes agent
    • Research tool

Additional information

Investigators:

  • Umesh R. Desai, Ph.D.
  • Rajesh Karuturi, Ph.D.
  • Rami A. Al Horani
  • Akul Mehta
  • Jay Thakkar

Patent status:

Issued patent: 8,262,881 Patents pending: App No 13/057,374 (U.S. rights only). Provisional: US and foreign rights.

License status:

This technology is available for licensing to industry for further development and commercialization.

Category:

Biomedical, Engineering and physical science

VCU Tech #:

11-91, 12-53, 17-61

Contact us about
this technology

Magdalena K. Morgan, Ph.D.
Licensing Associate
mkmorgan@vcu.edu
(804) 827-6095