Wieser, GescheGescheWieserMansi, RosalbaRosalbaMansiGrosu, Anca LAnca LGrosuSchultze-Seemann, WolfgangWolfgangSchultze-SeemannDumont-Walter, Rebecca ARebecca ADumont-WalterMeyer, Philipp TPhilipp TMeyerMaecke, Helmut RHelmut RMaeckeReubi-Kattenbusch, Jean-ClaudeJean-ClaudeReubi-KattenbuschWeber, Wolfgang AWolfgang AWeber2024-10-232024-10-232014https://boris-portal.unibe.ch/handle/20.500.12422/131728UNLABELLED Ex vivo studies have shown that the gastrin releasing peptide receptor (GRPr) is overexpressed on almost all primary prostate cancers, making it a promising target for prostate cancer imaging and targeted radiotherapy. METHODS Biodistribution, dosimetry and tumor uptake of the GRPr antagonist ⁶⁴Cu-CB-TE2A-AR06 [(⁶⁴Cu-4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo(6.6.2)hexadecane)-PEG₄-D-Phe-Gln-Trp-Ala-Val-Gly-His-Sta-LeuNH₂] were studied by PET/CT in four patients with newly diagnosed prostate cancer (T1c-T2b, Gleason 6-7). RESULTS No adverse events were observed after injection of ⁶⁴Cu-CB-TE2A-AR06. Three of four tumors were visualized with high contrast [tumor-to-prostate ratio > 4 at 4 hours (h) post injection (p.i.)], one small tumor (T1c, < 5% tumor on biopsy specimens) showed moderate contrast (tumor-to-prostate ratio at 4 h: 1.9). Radioactivity was cleared by the kidneys and only the pancreas demonstrated significant accumulation of radioactivity, which rapidly decreased over time. CONCLUSION ⁶⁴Cu-CB-TE2A-AR06 shows very favorable characteristics for imaging prostate cancer. Future studies evaluating ⁶⁴Cu-CB-TE2A-AR06 PET/CT for prostate cancer detection, staging, active surveillance, and radiation treatment planning are necessary.enGastrin releasing peptide receptorbombesinPET/CTprostate cancer500 - Science::570 - Life sciences; biology600 - Technology::610 - Medicine & healtharticle10.7892/boris.665092457872410.7150/thno.7324