title: F-18 labelled PSMA-1007: biodistribution, radiation dosimetry and histopathological validation of tumor lesions in prostate cancer patients.
abstract: OBJECTIVE
  The prostate-specific membrane antigen (PSMA) targeted positron-emitting-tomography (PET) tracer68Ga-PSMA-11 shows great promise in the detection of prostate cancer. However,68Ga has several shortcomings as a radiolabel including short half-life and non-ideal energies, and this has motivated consideration of18F-labelled analogs.18F-PSMA-1007 was selected among several18F-PSMA-ligand candidate compounds because it demonstrated high labelling yields, outstanding tumor uptake and fast, non-urinary background clearance. Here, we describe the properties of18F-PSMA-1007 in human volunteers and patients.
  
  
  METHODS
  Radiation dosimetry of18F-PSMA-1007 was determined in three healthy volunteers who underwent whole-body PET-scans and concomitant blood and urine sampling. Following this, ten patients with high-risk prostate cancer underwent18F-PSMA-1007 PET/CT (1 h and 3 h p.i.) and normal organ biodistribution and tumor uptakes were examined. Eight patients underwent prostatectomy with extended pelvic lymphadenectomy. Uptake in intra-prostatic lesions and lymph node metastases were correlated with final histopathology, including PSMA immunostaining.
  
  
  RESULTS
  With an effective dose of approximately 4.4-5.5 mSv per 200-250 MBq examination,18F-PSMA-1007 behaves similar to other PSMA-PET agents as well as to other18F-labelled PET-tracers. In comparison to other PSMA-targeting PET-tracers,18F-PSMA-1007 has reduced urinary clearance enabling excellent assessment of the prostate. Similar to18F-DCFPyL and with slightly slower clearance kinetics than PSMA-11, favorable tumor-to-background ratios are observed 2-3 h after injection. In eight patients, diagnostic findings were successfully validated by histopathology.18F-PSMA-1007 PET/CT detected 18 of 19 lymph node metastases in the pelvis, including nodes as small as 1 mm in diameter.
  
  
  CONCLUSIONS
  18F-PSMA-1007 performs at least comparably to68Ga-PSMA-11, but its longer half-life combined with its superior energy characteristics and non-urinary excretion overcomes some practical limitations of68Ga-labelled PSMA-targeted tracers.
authors.affiliation: Department of Nuclear Medicine, University Hospital Heidelberg, INF 400, 69120, Heidelberg, Germany. frederik@egiesel.com.
authors.forename: Frederik L
authors.initials: FL
authors.lastname: Giesel
authors.affiliation: Department of Urology, University Hospital Heidelberg, Heidelberg, Germany.
authors.forename: B
authors.initials: B
authors.lastname: Hadaschik
authors.affiliation: Division of Radiopharmaceutical Chemistry, German Cancer Research Center (dkfz), Heidelberg, Germany.
authors.forename: J
authors.initials: J
authors.lastname: Cardinale
authors.affiliation: Department of Urology, University Hospital Heidelberg, Heidelberg, Germany.
authors.forename: J
authors.initials: J
authors.lastname: Radtke
authors.affiliation: Department of Nuclear Medicine, University Hospital Heidelberg, INF 400, 69120, Heidelberg, Germany.
authors.forename: M
authors.initials: M
authors.lastname: Vinsensia
authors.affiliation: ABX-CRO, Dresden, Germany.
authors.forename: W
authors.initials: W
authors.lastname: Lehnert
authors.affiliation: Department of Urology, University Hospital Heidelberg, Heidelberg, Germany.
authors.forename: C
authors.initials: C
authors.lastname: Kesch
authors.affiliation: Section of Molecular Urooncology, Department of Urology, Medical Faculty Heidelberg, University Hospital Heidelberg, Heidelberg, Germany.
authors.forename: Y
authors.initials: Y
authors.lastname: Tolstov
authors.affiliation: Section of Molecular Urooncology, Department of Urology, Medical Faculty Heidelberg, University Hospital Heidelberg, Heidelberg, Germany.
authors.forename: S
authors.initials: S
authors.lastname: Singer
authors.affiliation: Institute of Pathology, University Hospital Heidelberg, Heidelberg, Germany.|Department of Medical Oncology, National Center for Tumor Diseases (NCT), University Hospital Heidelberg, Heidelberg, Germany.|Hamamatsu Tissue Imaging and Analysis Center, University of Heidelberg, Heidelberg, Germany.
authors.forename: N
authors.initials: N
authors.lastname: Grabe
authors.affiliation: Department of Urology, University Hospital Heidelberg, Heidelberg, Germany.|Section of Molecular Urooncology, Department of Urology, Medical Faculty Heidelberg, University Hospital Heidelberg, Heidelberg, Germany.
authors.forename: S
authors.initials: S
authors.lastname: Duensing
authors.affiliation: Division of Radiopharmaceutical Chemistry, German Cancer Research Center (dkfz), Heidelberg, Germany.
authors.forename: M
authors.initials: M
authors.lastname: Schäfer
authors.affiliation: Division of Radiopharmaceutical Chemistry, German Cancer Research Center (dkfz), Heidelberg, Germany.
authors.forename: O C
authors.initials: OC
authors.lastname: Neels
authors.affiliation: Department of Nuclear Medicine, University Hospital Heidelberg, INF 400, 69120, Heidelberg, Germany.
authors.forename: W
authors.initials: W
authors.lastname: Mier
authors.affiliation: Department of Nuclear Medicine, University Hospital Heidelberg, INF 400, 69120, Heidelberg, Germany.
authors.forename: U
authors.initials: U
authors.lastname: Haberkorn
authors.affiliation: Division of Radiopharmaceutical Chemistry, German Cancer Research Center (dkfz), Heidelberg, Germany.
authors.forename: K
authors.initials: K
authors.lastname: Kopka
authors.affiliation: Department of Nuclear Medicine, University Hospital Heidelberg, INF 400, 69120, Heidelberg, Germany.
authors.forename: C
authors.initials: C
authors.lastname: Kratochwil
mesh_terms: D000368:Aged; D000954:Antigens, Surface / Q000378:metabolism*; D005462:Fluorine Radioisotopes; D043425:Glutamate Carboxypeptidase II / Q000378:metabolism*; D006801:Humans; D008207:Lymphatic Metastasis; D008297:Male; D008875:Middle Aged; D000072078:Positron Emission Tomography Computed Tomography; D011471:Prostatic Neoplasms / Q000000981:diagnostic imaging* / Q000473:pathology; D011829:Radiation Dosage; D019275:Radiopharmaceuticals / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D065667:Renal Elimination; D014018:Tissue Distribution
chemical_list: D000954:Antigens, Surface; D005462:Fluorine Radioisotopes; D019275:Radiopharmaceuticals; C473848:FOLH1 protein, human; D043425:Glutamate Carboxypeptidase II
keywords: 18F-PSMA; F-18-PSMA; PET/CT; PSMA-1007; Positron emission tomography