title: Dosimetry and first clinical evaluation of the new 18F-radiolabeled bombesin analogue BAY 864367 in patients with prostate cancer.
abstract: The aim of this first-in-man study was to demonstrate the feasibility, safety, and tolerability, as well as provide dosimetric data and evaluate the imaging properties, of the bombesin analogue BAY 864367 for PET/CT in a small group of patients with primary and recurrent prostate cancer (PCa).
  
  
  METHODS
  Ten patients with biopsy-proven PCa (5 with primary PCa and 5 with prostate-specific antigen recurrence after radical prostatectomy) were prospectively selected for this exploratory clinical trial with BAY 864367, a new (18)F-labeled bombesin analogue. PET scans were assessed at 6 time points, up to 110 min after intravenous administration of 302 ± 11 MBq of BAY 864367. Imaging results were compared with (18)F-fluorocholine PET/CT scans. Dosimetry was calculated using the OLINDA/EXM software.
  
  
  RESULTS
  Three of 5 patients with primary disease showed positive tumor delineation in the prostate, and 2 of 5 patients with biochemical relapse showed a lesion suggestive of recurrence on the BAY 864367 scan. Tumor-to-background ratio averaged 12.9 ± 7.0. The ratio of malignant prostate tissue to normal prostate tissue was 4.4 ± 0.6 in 3 patients with tracer uptake in the primary PCa. Mean effective dose was 4.3 ± 0.3 mSv/patient (range, 3.7-4.9 mSv).
  
  
  CONCLUSIONS
  BAY 864367, a novel (18)F-labeled bombesin tracer, was successfully investigated in a first-in-man clinical trial of PCa and showed favorable dosimetric values. Additionally, the application was safe and well tolerated. The tracer delineated tumors in a subset of patients, demonstrating the potential of gastrin-releasing-peptide receptor imaging.
authors: Division of Nuclear Medicine, Department of Medical Radiology, University Hospital of Zurich, Zurich, Switzerland.
authors: Bert-Ram
authors: BR
authors: Sah
authors: Division of Nuclear Medicine, Department of Medical Radiology, University Hospital of Zurich, Zurich, Switzerland.
authors: Irene A
authors: IA
authors: Burger
authors: Center for Radiopharmaceutical Science, Paul Scherrer Institute, Villigen PSI, Switzerland Department of Chemistry and Applied Biosciences of the Eidgenössische Technische Hochschule Zürich, Zurich, Switzerland.
authors: Roger
authors: R
authors: Schibli
authors: Piramal, Molecular Imaging Division, Piramal Imaging GmbH, Berlin, Germany.
authors: Matthias
authors: M
authors: Friebe
authors: Piramal, Molecular Imaging Division, Piramal Imaging GmbH, Berlin, Germany.
authors: Ludger
authors: L
authors: Dinkelborg
authors: Bayer Healthcare, Global Drug Discovery, Berlin, Germany.
authors: Keith
authors: K
authors: Graham
authors: Bayer Healthcare, Global Drug Discovery, Berlin, Germany.
authors: Sandra
authors: S
authors: Borkowski
authors: Bayer Healthcare, Global Drug Discovery, Berlin, Germany.
authors: Claudia
authors: C
authors: Bacher-Stier
authors: Bayer Healthcare, Global Drug Discovery, Berlin, Germany.
authors: Ray
authors: R
authors: Valencia
authors: Bayer Healthcare, Global Drug Discovery, Berlin, Germany.
authors: Ananth
authors: A
authors: Srinivasan
authors: Division of Nuclear Medicine, Department of Medical Radiology, University Hospital of Zurich, Zurich, Switzerland.
authors: Thomas F
authors: TF
authors: Hany
authors: Division of Nuclear Medicine, Department of Medical Radiology, University Hospital of Zurich, Zurich, Switzerland.
authors: Linjing
authors: L
authors: Mu
authors: Department of Pathology, University Hospital of Zurich, Zurich, Switzerland; and.
authors: Peter J
authors: PJ
authors: Wild
authors: Division of Nuclear Medicine, Department of Medical Radiology, University Hospital of Zurich, Zurich, Switzerland Division of Medical Oncology, Department of Internal Medicine, University Hospital of Zurich, Zurich, Switzerland niklaus.schaefer@usz.ch.
authors: Niklaus G
authors: NG
authors: Schaefer
mesh_terms: D061605:Administration, Intravenous; D000368:Aged; D000465:Algorithms; D001706:Biopsy; D001839:Bombesin / Q000031:analogs & derivatives*; D005462:Fluorine Radioisotopes; D019886:Gastrin-Releasing Peptide / Q000737:chemistry; D006801:Humans; D008297:Male; D008875:Middle Aged; D009364:Neoplasm Recurrence, Local / Q000000981:diagnostic imaging; D049268:Positron-Emission Tomography; D017430:Prostate-Specific Antigen / Q000378:metabolism; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging*; D011874:Radiometry / Q000379:methods*; D019275:Radiopharmaceuticals; D012984:Software; D014057:Tomography, X-Ray Computed
chemical_list: C556307:BAY 86-4367; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; D019886:Gastrin-Releasing Peptide; D017430:Prostate-Specific Antigen; D001839:Bombesin
keywords: 18F-radiolabeled bombesin analogue; GRP receptor imaging; dosimetry; gastrin-releasing peptide; prostate cancer