Radiolabeled PARP Inhibitors for Imaging and Targeted Radiotherapy of Prostate Cancer
Abstract
The of this grant is to investigate a 77Br-labeled poly(ADP-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 (SSB/DSB). The major goals of this reporting period were to 1.)Determine the maximum tolerated dose and toxicity of [77Br]WC-DZ-Br, 2.) Conduct single dose therapy studies of[77Br]WC-DZ-Br in tumor bearing mice, 3.) determine the dosimetry of [77Br]WC-DZ-Br in normal mice, and 4.) Starttherapy in a metastatic model. The major activities conducted in this reporting period were to evaluate [77Br]WCDZ-Br in vivo to determine its therapeutic efficacy and toxicity after a single administration. The significant results ofthis reporting period were that [77Br]WC-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.
Document Details
- Document Type
- Technical Report
- Publication Date
- Sep 01, 2021
- Accession Number
- AD1160815
Entities
People
- Buck Rogers
Organizations
- Washington University in St. Louis