Fully-automated synthesis of 16beta-18F-fluoro-5alpha-dihydrotestosterone (FDHT) on the ELIXYS radiosynthesizer Journal Article


Authors: Lazari, M.; Lyashchenko, S. K.; Burnazi, E. M.; Lewis, J. S.; Michael van Dam, R.; Murphy, J. M.
Article Title: Fully-automated synthesis of 16beta-18F-fluoro-5alpha-dihydrotestosterone (FDHT) on the ELIXYS radiosynthesizer
Abstract: Noninvasive in vivo imaging of androgen receptor (AR) levels with positron emission tomography (PET) is becoming the primary tool in prostate cancer detection and staging. Of the potential 18F-labeled PET tracers, 18F-FDHT has clinically shown to be of highest diagnostic value. We demonstrate the first automated synthesis of 18F-FDHT by adapting the conventional manual synthesis onto the fully-automated ELIXYS radiosynthesizer. Clinically-relevant amounts of 18F-FDHT were synthesized on ELIXYS in 90min with decay-corrected radiochemical yield of 29±5% (n=7). The specific activity was 4.6Ci/μmol (170GBq/μmol) at end of formulation with a starting activity of 1.0Ci (37GBq). The formulated 18F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use. © 2015 Published by Elsevier Ltd.
Keywords: controlled study; unclassified drug; validation process; radiation dose; positron emission tomography; reproducibility; quality control; drug structure; drug synthesis; automation; prostate cancer; radioactivity; urology; radiopharmaceutical agent; high performance liquid chromatography; pet; time series analysis; prostate cancers; diseases; radioisotope decay; synthesis; room temperature; positron emission tomography (pet); androstanolone; radiochemistry; 16 beta fluoro 5 alpha dihydrotestosterone f 18; fdht; prostate cancer detection; polyethylene terephthalates; fluorine-18; chemical parameters; fully automated; priority journal; article; fully-automated; lialh<inf>4</inf> reduction; noninvasive in vivo imaging; quality control tests; biochemical equipment; decay corrected radiochemical yield; fully automated synthesis; manual radiosynthesis; radiosynthesizer; solvent effect; synthesis time
Journal Title: Applied Radiation and Isotopes
Volume: 103
ISSN: 0969-8043
Publisher: Pergamon-Elsevier Science Ltd  
Date Published: 2015-09-01
Start Page: 9
End Page: 14
Language: English
DOI: 10.1016/j.apradiso.2015.05.010
PROVIDER: scopus
PUBMED: 26046518
PMCID: PMC4530021
DOI/URL:
Notes: Export Date: 2 July 2015 -- Source: Scopus
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  1. Eva M Burnazi
    25 Burnazi
  2. Jason S Lewis
    456 Lewis