DOI: 10.1007/s00259-016-3573-4Pages: 678-688

F-18 labelled PSMA-1007: biodistribution, radiation dosimetry and histopathological validation of tumor lesions in prostate cancer patients

1. University Hospital Heidelberg, Department of Nuclear Medicine

2. University Hospital Heidelberg, Department of Urology

3. German Cancer Research Center (dkfz), Division of Radiopharmaceutical Chemistry

4. ABX-CRO

5. University Hospital Heidelberg, Section of Molecular Urooncology, Department of Urology, Medical Faculty Heidelberg

6. University Hospital Heidelberg, Institute of Pathology

7. University Hospital Heidelberg, Department of Medical Oncology, National Center for Tumor Diseases (NCT)

8. University of Heidelberg, Hamamatsu Tissue Imaging and Analysis Center

Correspondence to:
Frederik L. Giesel
Tel: +49-6221-56-7732
Email: frederik@egiesel.com

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Abstract

Purpose

The prostate-specific membrane antigen (PSMA) targeted positron-emitting-tomography (PET) tracer 68Ga-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 of 18F-labelled analogs. 18F-PSMA-1007 was selected among several 18F-PSMA-ligand candidate compounds because it demonstrated high labelling yields, outstanding tumor uptake and fast, non-urinary background clearance. Here, we describe the properties of 18F-PSMA-1007 in human volunteers and patients.

Methods

Radiation dosimetry of 18F-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 underwent 18F-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 other 18F-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 to 18F-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.

Conclusion

18F-PSMA-1007 performs at least comparably to 68Ga-PSMA-11, but its longer half-life combined with its superior energy characteristics and non-urinary excretion overcomes some practical limitations of 68Ga-labelled PSMA-targeted tracers.

This article is freely available, click here to access the full text/PDF

  • Accepted: Nov 9, 2016
  • Online: Nov 26, 2016

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