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Controlled Clinical Trial
. 2017 Apr;44(4):678-688.
doi: 10.1007/s00259-016-3573-4. Epub 2016 Nov 26.

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

Frederik L Giesel  1 , B Hadaschik  2 , J Cardinale  3 , J Radtke  2 , M Vinsensia  4 , W Lehnert  5 , C Kesch  2 , Y Tolstov  6 , S Singer  6 , N Grabe  7   8   9 , S Duensing  2   6 , M Schäfer  3 , O C Neels  3 , W Mier  4 , U Haberkorn  4 , K Kopka  3 , C Kratochwil  4
Affiliations
Controlled Clinical Trial

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

Frederik L Giesel et al. Eur J Nucl Med Mol Imaging. 2017 Apr.

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.

Keywords: 18F-PSMA; F-18-PSMA; PET/CT; PSMA-1007; Positron emission tomography.

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Conflict of interest statement

Conflict of interest

Patent application for PSMA-617 for KK and UH. Patent application for PSMA-1007 for JC, MS, UH, FLG, KK. The other authors declare that they have no conflict of interest.

Informed consent

All patients were informed about the in-house production of the novel radiopharmaceutical, according to the German Pharmaceuticals Act §13(2b), and gave written informed consent.

Statement of human rights

We retrospectively report observations from clinical practice. For this type of study no formal clinical trial registration is required. Our institutional ethics committee approved (permit S-321/2012) in accordance with our national regulations and to the updated version of the Helsinki declaration.

Disclosure

Part of the pre-clinical PSMA-1007 tracer development has been granted to JC as a Post-Doc position by ABX advanced biochemical compounds.

Figures

Fig. 1
Fig. 1
Comparison of different PSMA-ligands (18F-DCFBC, 18F-DCFPyL, 68Ga-PSMA-617, 68Ga-PSMA-11, 18F-PSMA-1007)
Fig. 2
Fig. 2
Maximum Intensity Projections (MIP) of ten serially performed (5 min–8 h p.i.) 18F-PSMA-1007 PET-scans in one healthy volunteer (a); biodistribution corrected for decay. Time-activity-curves of normal organs derived from PET volume-of-interest (b). Blood and serum time-activity-curves derived from serial blood-sampling, expressed as percent injected dose in a total blood volume of 6.1 l (c)
Fig. 3
Fig. 3
Time-activity-curves of 18F-PSMA-1007 from a volume-of-interest covering the healthy prostate from three volunteers (SUVmean with standard deviations)
Fig. 4
Fig. 4
a: Biodistribution of mean SUVmax of 18F-PSMA-1007 in normal organs (blood, brain, nasal mucosa, lacrimal gland, parotid and submandibularis glands, lungs, liver, spleen, pancreas, small intestines, kidneys and bladder) and tumor lesions (prostate cancer (PCa) and lymph node (LN) metastases) with its standard error. b: Biodistribution of mean SUVmean of 18F-PSMA-1007 in normal organs (blood, brain, nasal mucosa, lacrimal, parotid and submandibularis glands, lungs, liver, spleen, pancreas, small intestines, kidneys and bladder) and tumor lesions (prostate cancer (PCa) and lymph node (LN) metastases) with its standard error. c: Biodistribution of mean SUVmax to background of 18F-PSMA-1007 in normal organs (blood, brain, nasal mucosa, lacrimal, parotid and, submandibular glands, lungs, liver, spleen, pancreas, small intestines, kidneys and bladder) and tumor lesions (prostate cancer (PCa) and lymph node (LN) metastases) with its standard error
Fig. 5
Fig. 5
a: Patient 2, a 72-year-old patient (PSA 15 ng/ml) diagnosed with Gleason 9 (5 + 4) prostate cancer. Patient presented with a large tumor mass in the prostate gland infiltrating the left seminal vesicle and metastases to several lymph nodes in the pelvis. Two metastatic lymph nodes are located outside the pelvis, both paraaortic at level L3/4 and L5. 18F-PSMA-1007 shows high tumor uptake after 1 h and 3 h p.i in the maximum intensity projection PET-scan. Due to the lipophilic characteristics of 18F-PSMA-1007, the hepatobiliary clearance can be observed while urinary excretion is minimal. b: Patient 1, a 77-year-old prostate cancer patient (PSA 40 ng/ml) shows a large tumor mass on the mid and apical prostate and several lymph node metastases
Fig. 6
Fig. 6
Comparison of virtual whole mount histopathology (H&E and PSMA-immunostaining) and PSMA PET-findings. Transaxial PET/CT-scan of patient 1 (a, b, e, f) and corresponding histopathology of the subsequent prostatectomy specimen; H&E staining (c, g); PSMA-immunostaining with outlined tumor contours in red (d, h)
See this image and copyright information in PMC

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