title: Positron emission tomography (PET) imaging of prostate cancer with a gastrin releasing peptide receptor antagonist--from mice to men.
abstract: 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.
  
  
  CONCLUSIONS
  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.
authors.affiliation: 1. Department of Nuclear Medicine, University Hospital Freiburg, Germany.
authors.forename: Gesche
authors.initials: G
authors.lastname: Wieser
authors.affiliation: 1. Department of Nuclear Medicine, University Hospital Freiburg, Germany.
authors.forename: Rosalba
authors.initials: R
authors.lastname: Mansi
authors.affiliation: 2. Department of Radiation Oncology, University Hospital Freiburg, Germany.
authors.forename: Anca L
authors.initials: AL
authors.lastname: Grosu
authors.affiliation: 3. Department of Urology, University Hospital Freiburg, Germany.
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Schultze-Seemann
authors.affiliation: 1. Department of Nuclear Medicine, University Hospital Freiburg, Germany. ; 4. Department of Radiology, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA.
authors.forename: Rebecca A
authors.initials: RA
authors.lastname: Dumont-Walter
authors.affiliation: 1. Department of Nuclear Medicine, University Hospital Freiburg, Germany. ; 5. German Cancer Consortium (DKTK).
authors.forename: Philipp T
authors.initials: PT
authors.lastname: Meyer
authors.affiliation: 1. Department of Nuclear Medicine, University Hospital Freiburg, Germany. ; 5. German Cancer Consortium (DKTK).
authors.forename: Helmut R
authors.initials: HR
authors.lastname: Maecke
authors.affiliation: 6. Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Switzerland.
authors.forename: Jean Claude
authors.initials: JC
authors.lastname: Reubi
authors.affiliation: 1. Department of Nuclear Medicine, University Hospital Freiburg, Germany. ; 7. Molecular Imaging and Therapy Service, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
authors.forename: Wolfgang A
authors.initials: WA
authors.lastname: Weber
mesh_terms: D000368:Aged; D003287:Contrast Media; D056831:Coordination Complexes / Q000493:pharmacokinetics*; D006801:Humans; D007668:Kidney / Q000187:drug effects; D008297:Male; D008875:Middle Aged; D009842:Oligopeptides / Q000493:pharmacokinetics*; D009942:Organometallic Compounds / Q000493:pharmacokinetics*; D010179:Pancreas / Q000187:drug effects; D049268:Positron-Emission Tomography / Q000379:methods*; D011471:Prostatic Neoplasms / Q000175:diagnosis*; D018004:Receptors, Bombesin / Q000037:antagonists & inhibitors; D014018:Tissue Distribution
chemical_list: C483895:(4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo(6.6.2)hexadecane)copper(II); C000592691:(64Cu-4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo(6.6.2)hexadecane)-PEG4-phenylalanyl-glutaminyl-tryptophyl-alanyl-valyl-glycyl-histidyl-4-amino-3-hydroxy-6-methylheptanoyl-leucinamide; D003287:Contrast Media; D056831:Coordination Complexes; D009842:Oligopeptides; D009942:Organometallic Compounds; D018004:Receptors, Bombesin
keywords: Gastrin releasing peptide receptor; PET/CT; bombesin; prostate cancer.