Fully automated synthesis of [(18) F]fluoro-dihydrotestosterone ([(18) F]FDHT) using the FlexLab module

J Labelled Comp Radiopharm. 2016 Aug;59(10):424-8. doi: 10.1002/jlcr.3417. Epub 2016 Jul 4.

Abstract

Imaging of androgen receptor expression in prostate cancer using F-18 FDHT is becoming increasingly popular. With the radiolabelling precursor now commercially available, developing a fully automated synthesis of [(18) F] FDHT is important. We have fully automated the synthesis of F-18 FDHT using the iPhase FlexLab module using only commercially available components. Total synthesis time was 90 min, radiochemical yields were 25-33% (n = 11). Radiochemical purity of the final formulation was > 99% and specific activity was > 18.5 GBq/µmol for all batches. This method can be up-scaled as desired, thus making it possible to study multiple patients in a day. Furthermore, our procedure uses 4 mg of precursor only and is therefore cost-effective. The synthesis has now been validated at Austin Health and is currently used for [(18) F]FDHT studies in patients. We believe that this method can easily adapted by other modules to further widen the availability of [(18) F]FDHT.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Automation
  • Chemistry Techniques, Synthetic / methods*
  • Dihydrotestosterone / analogs & derivatives*
  • Dihydrotestosterone / chemical synthesis
  • Dihydrotestosterone / chemistry
  • Fluorine Radioisotopes*
  • Isotope Labeling
  • Quality Control
  • Radiochemistry / methods*

Substances

  • 16-fluorodihydrotestosterone
  • Fluorine Radioisotopes
  • Dihydrotestosterone