Fully-automated synthesis of 16β-(18)F-fluoro-5α-dihydrotestosterone (FDHT) on the ELIXYS radiosynthesizer.

Journal: Applied radiation and isotopes : including data, instrumentation and methods for use in agriculture, industry and medicine
Published Date: May 21, 2015

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 (18)F-labeled PET tracers, (18)F-FDHT has clinically shown to be of highest diagnostic value. We demonstrate the first automated synthesis of (18)F-FDHT by adapting the conventional manual synthesis onto the fully-automated ELIXYS radiosynthesizer. Clinically-relevant amounts of (18)F-FDHT were synthesized on ELIXYS in 90 min with decay-corrected radiochemical yield of 29±5% (n=7). The specific activity was 4.6 Ci/µmol (170 GBq/µmol) at end of formulation with a starting activity of 1.0 Ci (37 GBq). The formulated (18)F-FDHT yielded sufficient activity for multiple patient doses and passed all quality control tests required for routine clinical use.

Authors

  • Mark Lazari
    Department of Bioengineering, Henry Samueli School of Engineering, UCLA, Los Angeles, CA, USA; Crump Institute for Molecular Imaging, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA; Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA.
  • Serge K Lyashchenko
    Radiochemistry & Molecular Imaging Probe Core, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
  • Eva M Burnazi
    Radiochemistry & Molecular Imaging Probe Core, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
  • Jason S Lewis
    Radiochemistry & Molecular Imaging Probe Core, Memorial Sloan Kettering Cancer Center, New York, NY, USA; Radiochemistry and Imaging Sciences Service, Radiology, Memorial Sloan Kettering Cancer Center, New York, NY, USA.
  • R Michael van Dam
    Department of Bioengineering, Henry Samueli School of Engineering, UCLA, Los Angeles, CA, USA; Crump Institute for Molecular Imaging, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA; Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA.
  • Jennifer M Murphy
    Crump Institute for Molecular Imaging, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA; Department of Molecular and Medical Pharmacology, David Geffen School of Medicine, UCLA, Los Angeles, CA, USA. Electronic address: jmmurphy@mednet.ucla.edu.

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