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

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

Gesche Wieser  1 , Rosalba Mansi  1 , Anca L Grosu  2 , Wolfgang Schultze-Seemann  3 , Rebecca A Dumont-Walter  4 , Philipp T Meyer  5 , Helmut R Maecke  5 , Jean Claude Reubi  6 , Wolfgang A Weber  7
Affiliations
Clinical Trial

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

Gesche Wieser et al. Theranostics. .

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.

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..

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Conflict of interest statement

Competing Interests: The authors have declared that no competing interest exists.

Figures

Figure 1
Figure 1
Chemical structure of 64Cu-CB-TE2A-AR06.
Figure 2
Figure 2
64Cu-CB-TE2A-AR06 PET/CT study of patient 2. Images were acquired 4 h p.i.. A, B: Coronal sections of PET and fused PET/CT. C: Axial PET/CT fusion images at the levels indicated by dotted lines in A. There is intense uptake by the prostate tumor (red arrows) and the pancreas. Kidneys, liver and intestines show only low tracer uptake. The PET images are scaled to an SUV of 5 (color bar).
Figure 3
Figure 3
Correlation between in vivo PET and ex vivo autoradiography. A, B: Transaxial fused PET/CT and PET 4 h p.i.. C: Ex vivo GRP receptor autoradiography demonstrating GRPr expression by the tumor.
Figure 4
Figure 4
A: Radioactivity concentration in the blood over time (mean and standard deviation) and bi-exponential fit of the data. The initial half-life of 64Cu-CB-TE2A-AR06 is 5 minutes and the terminal half-life 165 minutes. B: Radioactivity concentration in the tumors over time.
Figure 5
Figure 5
Tumor-to-normal-organ ratios over time.
See this image and copyright information in PMC

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