GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4: a first-in-man study

Stephen J. Mather, Berthold A. Nock, Theodosia Maina, Vickie Gibson, David Ellison, Iain Murray, Ravin Sobnack, Steve Colebrook, Susan Wan, Gavin Halbert, Teresa Szysko, Thomas Powles, Norbert Avril

Research output: Contribution to journalArticle

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Abstract

We explored the imaging of bombesin receptors and evaluated the clinical use of [(99m)Tc]Demobesin 4 ([(99m)Tc]DB4) in prostate cancer patients.  [(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.  [(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.  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.

LanguageEnglish
Pages888-895
Number of pages8
JournalMolecular Imaging and Biology
Volume16
Issue number6
Early online date11 Jun 2014
DOIs
Publication statusPublished - Dec 2014

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Prostatic Neoplasms
Bombesin Receptors
Radiopharmaceuticals
Single-Photon Emission-Computed Tomography
Pancreas
Pharmacokinetics
Urine
Hormones
Kidney
Therapeutics

Keywords

  • GRP receptor
  • gastrin-releasing peptide receptor
  • peptide
  • imaging

Cite this

Mather, S. J., Nock, B. A., Maina, T., Gibson, V., Ellison, D., Murray, I., ... Avril, N. (2014). GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4: a first-in-man study. Molecular Imaging and Biology, 16(6), 888-895. https://doi.org/10.1007/s11307-014-0754-z
Mather, Stephen J. ; Nock, Berthold A. ; Maina, Theodosia ; Gibson, Vickie ; Ellison, David ; Murray, Iain ; Sobnack, Ravin ; Colebrook, Steve ; Wan, Susan ; Halbert, Gavin ; Szysko, Teresa ; Powles, Thomas ; Avril, Norbert. / GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4 : a first-in-man study. In: Molecular Imaging and Biology. 2014 ; Vol. 16, No. 6. pp. 888-895.
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Mather, SJ, Nock, BA, Maina, T, Gibson, V, Ellison, D, Murray, I, Sobnack, R, Colebrook, S, Wan, S, Halbert, G, Szysko, T, Powles, T & Avril, N 2014, 'GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4: a first-in-man study' Molecular Imaging and Biology, vol. 16, no. 6, pp. 888-895. https://doi.org/10.1007/s11307-014-0754-z

GRP receptor imaging of prostate cancer using [(99m)Tc]Demobesin 4 : a first-in-man study. / Mather, Stephen J.; Nock, Berthold A.; Maina, Theodosia; Gibson, Vickie; Ellison, David; Murray, Iain; Sobnack, Ravin; Colebrook, Steve; Wan, Susan; Halbert, Gavin; Szysko, Teresa; Powles, Thomas; Avril, Norbert.

In: Molecular Imaging and Biology, Vol. 16, No. 6, 12.2014, p. 888-895.

Research output: Contribution to journalArticle

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AU - Nock, Berthold A.

AU - Maina, Theodosia

AU - Gibson, Vickie

AU - Ellison, David

AU - Murray, Iain

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AU - Colebrook, Steve

AU - Wan, Susan

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AU - Powles, Thomas

AU - Avril, Norbert

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AB - We explored the imaging of bombesin receptors and evaluated the clinical use of [(99m)Tc]Demobesin 4 ([(99m)Tc]DB4) in prostate cancer patients.  [(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.  [(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.  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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