16 beta-[18F]fluoromoxestrol: a potent, metabolically stable positron emission tomography imaging agent for estrogen receptor positive human breast tumors

Life Sci. 1993;53(10):811-9. doi: 10.1016/0024-3205(93)90503-u.

Abstract

16 beta-[18F]Fluoromoxestrol (beta FMOX, 1) is a highly selective, metabolically stable estrogen with potential as a receptor imaging agent. It demonstrates receptor-mediated uptake in the immature rat in the estrogen receptor-rich primary target tissues, uterus and ovaries, as well as, in receptor-poor secondary target tissues, muscle, thymus and kidneys; uptake in the uterus is nearly four times that of the clinically useful 16 alpha-[18F]fluoroestradiol (FES), most likely due to the extended lifetime of the labeled beta FMOX in the blood afforded by its relatively slow metabolism. In vivo and in vitro studies demonstrate a nearly four-fold decrease in metabolism rate between beta FMOX and FES. Dosimetry studies indicate radiation absorbed doses comparable to FES. beta FMOX possesses desirable imaging characteristics and may prove to be a clinically useful imaging agent.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Breast Neoplasms / diagnostic imaging*
  • Breast Neoplasms / ultrastructure*
  • Ethinyl Estradiol / analogs & derivatives*
  • Female
  • Fluorine Radioisotopes
  • Humans
  • Liver / cytology
  • Liver / metabolism
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Estrogen / analysis*
  • Tomography, Emission-Computed

Substances

  • Fluorine Radioisotopes
  • Receptors, Estrogen
  • fluoromoxestrol
  • Ethinyl Estradiol