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Organ protection in PSMA-targeted radionuclide therapy of prostate cancer

  • US 9,956,305 B2
  • Filed: 09/04/2015
  • Issued: 05/01/2018
  • Est. Priority Date: 09/08/2014
  • Status: Active Grant
First Claim
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1. A method of reducing radiation exposure of a non-cancerous tissue of a patient diagnosed with prostate cancer, the method comprising:

  • administering to the patient a compound comprising a radionuclide and a recognition moiety for Prostate Specific Membrane Antigen (“

    PSMA”

    ), the compound binding to both cancerous prostate tissue and the non-cancerous tissue, and,after a waiting period of 1 hour to 60 hours, administering an agent in an amount sufficient to cause a displacement of the bound compound from the binding sites in the non-cancerous tissue by binding of the agent thereto while retaining the radionuclide in the cancerous tissue thereby reducing the exposure of the non-cancerous tissue to the radionuclide;

    wherein;

    the binding sites are attached to both the agent and the compound, andthe agent has a different chemical structure from the compound, orthe agent has the same chemical structure as the compound absent the radionuclide, andthe agent comprises a recognition moiety for PSMA;

    the compound is a Glu-urea-based PSMA ligand; and

    the agent comprises a Glu-urea-based PSMA ligand, a phosphinyl containing moiety, 7-(L-2-amino-2-carboxyethylthio)-2-(2,2-dimethylcyclopropanecarboxamide)-2-heptenoic acid, 2-(phosphonomethyl)pentanedioic acid, or 2-(3-mercaptopropyl)pentanedioic acid (2-MPPA).

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