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Radiolabeled PARP Inhibitors for Imaging and Targeted Radiotherapy of Prostate Cancer
[Technical Report, Annual Report]
WASHINGTON UNIV ST LOUIS MO
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 biodistribution of 77BrWC-DZ-Br in PC-3 and IGR-CaP1 subcutaneous models, 2. conduct singledose therapy studies of 77BrWC-DZ-Br in a metastatic model, 3. conduct a multi-dose therapy study of 77BrWCDZ-Br in a metastatic model. The major activities conducted in this reporting period were to evaluate 77BrWC-DZBr in vivo to determine its tissue localization and therapeutic efficacy after a single administration. The significantresults of this reporting period were that 77BrWC-DZ-Br had good, specific uptake in PC-3 and IGR-CaP1 tumorsat 4 h after injection and this uptake was higher than all other tissues except for the liver. In addition, in themetastatic IGR-CaP1 model, injection of 77BrWC-DZ-Br showed a trend of increasing survival, but this did notreach significance.
[A, Approved For Public Release]