Automated SPE-based synthesis of 16α-[18F]fluoroestradiol without HPLC purification step

Appl Radiat Isot. 2018 Nov:141:57-63. doi: 10.1016/j.apradiso.2018.08.007. Epub 2018 Aug 10.

Abstract

[18F]fluoroestradiol ([18F]FES) is well-established PET radiotracer for diagnosing and monitoring treatment of estrogen-positive breast cancer. The radiotracer is produced via one-pot two steps synthesis using cyclic sulfate precursor and is usually purified by semi-preparative HPLC. Here we suggested simple SPE purification procedure using OASIS WAX 3cc and Sep-Pak QMA light cartridges that afforded [18F]FES in typically 15% RCY (corrected for decay) within 45 min formulated in 5% EtOH/saline. All purity parameters were well within specifications recommended in the Investigator's Brochure for [18F]Fluoroestradiol.

Keywords: 16α-[(18)F]fluoroestradiol; Estrogen receptor; Fluorine-18; PET; SPE purification; [(18)F]FES.

MeSH terms

  • Automation
  • Breast Neoplasms / diagnostic imaging
  • Breast Neoplasms / metabolism
  • Chromatography, High Pressure Liquid
  • Estradiol / analogs & derivatives*
  • Estradiol / chemical synthesis
  • Estradiol / isolation & purification
  • Female
  • Fluorine Radioisotopes / isolation & purification*
  • Humans
  • Positron-Emission Tomography
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / isolation & purification
  • Receptors, Estrogen / metabolism
  • Solid Phase Extraction / instrumentation
  • Solid Phase Extraction / methods*

Substances

  • Fluorine Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Estrogen
  • Estradiol
  • 16-fluoroestradiol