Positron emission tomography (PET) imaging of prostate cancer with a gastrin releasing peptide receptor antagonist--from mice to men

Theranostics. 2014 Feb 1;4(4):412-9. doi: 10.7150/thno.7324. eCollection 2014.


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.

Keywords: Gastrin releasing peptide receptor; PET/CT; bombesin; prostate cancer..

Publication types

  • Clinical Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aged
  • Contrast Media
  • Coordination Complexes / pharmacokinetics*
  • Humans
  • Kidney / drug effects
  • Male
  • Middle Aged
  • Oligopeptides / pharmacokinetics*
  • Organometallic Compounds / pharmacokinetics*
  • Pancreas / drug effects
  • Positron-Emission Tomography / methods*
  • Prostatic Neoplasms / diagnosis*
  • Receptors, Bombesin / antagonists & inhibitors
  • Tissue Distribution


  • (4,11-bis(carboxymethyl)-1,4,8,11-tetraazabicyclo(6.6.2)hexadecane)copper(II)
  • (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
  • Contrast Media
  • Coordination Complexes
  • Oligopeptides
  • Organometallic Compounds
  • Receptors, Bombesin