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Updated: Apr 28, 2026
MR Molecular Imaging of Prostate Cancer with a Small Molecular CLT1 Peptide Targeted Contrast Agent
Published on: September 3, 2013
GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4: a first-in-man study
Stephen J Mather1, Berthold A Nock, Theodosia Maina
1Centre for Molecular Oncology, Barts Cancer Institute, London, EC1M 6BQ, UK, s.j.mather@qmul.ac.uk.
Purpose:
We explored the imaging of bombesin receptors and evaluated the clinical use of [(99m)Tc]Demobesin 4 ([(99m)Tc]DB4) in prostate cancer patients.
Procedures:
[(99m)Tc]DB4 was prepared according to Good Manufacturing Practice. Patients with prostate cancer underwent serial planar and SPECT imaging up to 3 h after administration. Blood and urine samples were taken to assess pharmacokinetics.
Results:
[(99m)Tc]DB4 is safe and clears rapidly from the bloodstream via the kidneys resulting in low background activity. The tracer binds strongly to the gastrin-releasing peptide receptor (GRPR) in vivo as indicated by the high uptake in the pancreas seen in all patients. In patients who had undergone hormone therapy, [(99m)Tc]DB4 did not efficiently image metastatic prostate cancer. In contrast, in newly diagnosed patients local disease was visualised.
Conclusions:
The GRPR is an unsuitable target for imaging refractory prostate cancer but may be useful in untreated disease. [(99m)Tc]DB4 is a promising radiopharmaceutical which merits further exploration in this specific group of patients.
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