Office of Technology Transfer – University of Michigan

Plasminogen Activator Inhibitor-1 Inhibitors and Methods of Use Thereof

Technology #5475

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Researchers
Daniel A. Lawrence
Managed By
Tiefei Dong
Senior Licensing Specialist, Life Sciences 734-763-5332
Patent Protection
US Patent Pending 2015‑0315178

Regulation of plasminogen activator inhibitor-1 activity

Blood clotting and formation of fibrous connective tissue are important biological functions that require tight regulation because either excess or insufficient formation of blood clot or connective tissue can lead to devastating health conditions. Plasminogen activator inhibitor-1 (PAI-1) is the critical molecule that modulates both of these biological processes. Although cases of congenital deficiency of PAI-1 are rare, various cancers, obesity, and other metabolic syndromes can lead to chronic increase of PAI-1 and cause pathological formation of blood clot or excessive connective tissues in specific organs. The patent pending technology inhibits PAI-1 activity thereby reducing excessive PAI-1 level in the bloodstream of patients.

A companion therapy for various metabolic syndromes and fibrosis

Elevated level of PAI-1 is common in inflammation related disorders or diseases. Therefore usage of PAI-1 inhibitors can be a useful combinatory treatment for widespread conditions including fibrotic disease, obesity, and type-2 diabetes. The efficacy of the invention was tested in vitro using recombinant active human PAI-1.

Advantageous

  • A PAI-1 inhibitor is useful in the treatment of any condition that lowing of PAI-1 level is beneficial including fibrotic disease, certain cancer cases, obesity, atherosclerosis, and type-2 diabetes.
  • The treatment can be delivered intravenously, orally, or locally via injection.
  • A useful modulator of endogenous fibrinolysis

Applications

  • A treatment for diseases and disorders associated with PAI-1 activity, such as obesity, diabetes, polycystic ovary syndrome, bone loss, and fibrosis
  • A useful inhibitor for regulating anti-blood clot agent in patients