Accession Number:



Radiolabeled PARP Inhibitors for Imaging and Targeted Radiotherapy of Prostate Cancer

Descriptive Note:

[Technical Report, Annual Report]

Corporate Author:


Personal Author(s):

Report Date:


Pagination or Media Count:



The of this grant is to investigate a 77Br-labeled polyADP-ribose polymerase-1 PARP-1 inhibitor for Augerradiation targeted radiotherapy of mCRPC. PARP-1 is a nuclear enzyme which initiates DNA repair by binding tothe sites of single- or double-strand breaks SSBDSB. The major goals of this reporting period were to 1.Determine the maximum tolerated dose and toxicity of 77BrWC-DZ-Br, 2. Conduct single dose therapy studies of77BrWC-DZ-Br in tumor bearing mice, 3. determine the dosimetry of 77BrWC-DZ-Br in normal mice, and 4. Starttherapy in a metastatic model. The major activities conducted in this reporting period were to evaluate 77BrWCDZ-Br in vivo to determine its therapeutic efficacy and toxicity after a single administration. The significant results ofthis reporting period were that 77BrWC-DZ-Br was relatively non-toxic in mice and that it demonstrated significanttumor growth delay in mice bearing subcutaneous PC-3 and IGR-CaP1 tumors. In addition, we have madeprogress in establishing the metatstatic IGR-CaP1 model.

Subject Categories:

  • Medicine and Medical Research
  • Radioactivity, Radioactive Wastes and Fission Products

Distribution Statement:

[A, Approved For Public Release]