Office of Technology Transfer – University of Michigan

Cell-Specific Mineralocorticoid Receptor Theranostics for Inflammatory Diseases

Technology #5525

Current mineralocorticoid receptor (MR) antagonists have side effect when treating cardiovascular diseases. Activation of MRs promotes inflammation and cardiovascular disease. Patients suffer from these diseases can benefit from MR blockage by MR antagonists, such as spironolactone and eplerenone. However, these traditional MR antagonists have limitations including off-target effects and difficulties in identifying patients who need more intensive MR blockage.

The combination of organ-specific drug delivery and sensor-tagged MR antagonists makes personalized medicine possible and provides way to monitor efficacy.

A quantifiable fluorescent reporter has been incorporated to eplerenone to allow the monitor of therapeutic efficacy for diagnostic purpose. At the same time, a small molecule delivery system has been developed to enable organ-specific delivery of the fluorescence tagged MR antagonists. These MR sensor-antagonists can block inflammatory responses in a cell-specific manner that provides the therapeutic benefits of MR antagonists, meanwhile, minimize potential systemic toxicities such as hyperkalemia.

Applications

  • Therapeutics for cardiovascular diseases including heart failure and myocardial infarction.
  • Treatment for other inflammatory diseases or inflammatory symptoms in other diseases.

Advantages

  • Organ-specific MR blockade delivers therapeutic benefits without systemic side-effects
  • Diagnostic marker together with therapeutic makes personalized medicine in treating inflammatory cardiovascular diseases possible.