ArticleEJNMMI research2016
Automated synthesis of [(18)F]DCFPyL via direct radiofluorination and validation in preclinical prostate cancer models.
Article in EJNMMI research, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 38 papers.
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Who cites it
38 citing papers in PubMed, 90 citations in OpenAlex.
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- Development and Internal Validation of a Novel Nomogram Predicting the Outcome of Salvage Radiation Therapy for Biochemical Recurrence after Radical Prostatectomy in Patients without Metastases on Restaging Prostate-specific Membrane Antigen Positron Emission Tomography/Computed Tomography.European urology open science · 2024Article
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- Medicinal (Radio) Chemistry: Building Radiopharmaceuticals for the Future.Current medicinal chemistry · 2024Review
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- The Probability of Metastases Within Different Prostate-specific Antigen Ranges Using Prostate-specific Membrane Antigen Positron Emission Tomography in Patients with Newly Diagnosed Prostate Cancer.European urology open science · 2024Article
- Radiochemical and Biological Evaluation of 3p-Pharmaceuticals (Basel, Switzerland) · 2023Article
- Outcome of patients with biochemical recurrence of prostate cancer after PSMA PET/CT-directed radiotherapy or surgery without systemic therapy.Cancer imaging : the official publication of the International Cancer Imaging Society · 2023Article
- Synthesis and radiolabelling of PSMA-targeted derivatives containing GYK/MVK cleavable linkers.Royal Society open science · 2023Article
- PSA-Stratified Performance of [Diagnostics (Basel, Switzerland) · 2022Article
- A Pilot Study of DynamicMolecular imaging and biology · 2022Article
- Predicting early outcomes in patients with intermediate- and high-risk prostate cancer using prostate-specific membrane antigen positron emission tomography and magnetic resonance imaging.BJU international · 2022Observational
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- The aluminium-[EJNMMI radiopharmacy and chemistry · 2021Review
- Management impact ofEuropean journal of nuclear medicine and molecular imaging · 2021Article
- Prostate specific membrane antigen positron emission tomography for lesion-directed high-dose-rate brachytherapy dose escalation.Physics and imaging in radiation oncology · 2021Article
- Preclinical Evaluation of a Fluorine-18 Labeled Probe for the Detection of the Expression of PSMA Level in Cancer.ACS omega · 2021Article
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Authors and funding
8 authors at 3 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundProstate-specific membrane antigen (PSMA) is frequently overexpressed and upregulated in prostate cancer. To date, various (18)F- and (68)Ga-labeled urea-based radiotracers for PET imaging of PSMA have been developed and entered clinical trials. Here, we describe an automated synthesis of [(18)F]DCFPyL via direct radiofluorination and validation in preclinical models of prostate cancer.
methods[(18)F]DCFPyL was synthesized via direct nucleophilic heteroaromatic substitution reaction in a single reactor TRACERlab FXFN automated synthesis unit. Radiopharmacological evaluation of [(18)F]DCFPyL involved internalization experiments, dynamic PET imaging in LNCaP (PSMA+) and PC3 (PSMA-) tumor-bearing BALB/c nude mice, biodistribution studies, and metabolic profiling. In addition, reversible two-tissue compartmental model analysis was used to quantify pharmacokinetics of [(18)F]DCFPyL in LNCaP and PC3 tumor models.
resultsAutomated radiosynthesis afforded radiotracer [(18)F]DCFPyL in decay-corrected radiochemical yields of 23 ± 5 % (n = 10) within 55 min, including HPLC purification. Dynamic PET analysis revealed rapid and high uptake of radioactivity (SUV5min 0.95) in LNCaP tumors which increased over time (SUV60min 1.1). Radioactivity uptake in LNCaP tumors was blocked in the presence of nonradioactive DCFPyL (SUV60min 0.22). The muscle as reference tissue showed rapid and continuous clearance over time (SUV60min 0.06). Fast blood clearance of radioactivity resulted in tumor-blood ratios of 1.0 after 10 min and 8.3 after 60 min. PC3 tumors also showed continuous clearance of radioactivity over time (SUV60min 0.11). Kinetic analysis of PET data revealed the two-tissue compartmental model as best fit with K 1 = 0.12, k 2 = 0.18, k 3 = 0.08, and k 4 = 0.004 min(-1), confirming molecular trapping of [(18)F]DCFPyL in PSMA+ LNCaP cells.
conclusions[(18)F]DCFPyL can be prepared for clinical applications simply and in good radiochemical yields via a direct radiofluorination synthesis route in a single reactor automated synthesis unit. Radiopharmacological evaluation of [(18)F]DCFPyL confirmed high PSMA-mediated tumor uptake combined with superior clearance parameters. Compartmental model analysis points to a two-step molecular trapping mechanism based on PSMA binding and subsequent internalization leading to retention of radioactivity in PSMA+ LNCaP tumors.
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