Development and evaluation of a 99mTc(V)-nitrido complex derived from estradiol for breast cancer imaging

Appl Radiat Isot. 2019 Dec:154:108854. doi: 10.1016/j.apradiso.2019.108854. Epub 2019 Aug 13.

Abstract

Estrogen receptors are overexpressed in 70% of breast cancer and identification of their presence is important to select the appropriate treatment. This work proposes the preparation and evaluation of an estradiol derived as potential ER imaging agent. Ethinylestradiol was derivatized to introduce a dithiocarbamate function for Tc coordination. Labeling was achieved through the formation of a symmetric Tc(V)-nitrido complex with a radiochemical purity (RCP) > 95%. Physicochemical evaluation, cell uptake, biodistribution in normal animals and in nude mice bearing induced ER + breast tumors showed promising results.

Keywords: Estrogen receptors; Nitrido complexes; Radiopharmaceuticals; Technetium.

MeSH terms

  • Animals
  • Breast Neoplasms / diagnostic imaging*
  • Breast Neoplasms / metabolism
  • Drug Stability
  • Estradiol / analogs & derivatives
  • Estradiol / chemical synthesis
  • Estradiol / chemistry
  • Female
  • Humans
  • MCF-7 Cells
  • Mice
  • Mice, Nude
  • Neoplasm Transplantation
  • Organotechnetium Compounds* / chemical synthesis
  • Organotechnetium Compounds* / chemistry
  • Organotechnetium Compounds* / pharmacokinetics
  • Protein Binding
  • Radiopharmaceuticals* / chemical synthesis
  • Radiopharmaceuticals* / chemistry
  • Radiopharmaceuticals* / pharmacokinetics
  • Rats
  • Rats, Wistar
  • Receptors, Estrogen / metabolism
  • Tissue Distribution

Substances

  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Receptors, Estrogen
  • Estradiol