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

Henry F. VanBrocklin, Pamela A. Rocque, Henry V. Lee, Kathryn E. Carlson, John A. Katzenellenbogen, Michael J. Welch

Research output: Contribution to journalArticlepeer-review

Abstract

16β-[18F]Fluoromoxestrol (βFMOX, 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 16α-[18F]fluoroestradiol (FES), most likely due to the extended lifetime of the labeled βFMOX 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 βFMOX and FES. Dosimetry studies indicate radiation absorbed doses comparable to FES. βFMOX possesses desirable imaging characteristics and may prove to be a clinically useful imaging agent.

Original languageEnglish (US)
Pages (from-to)811-819
Number of pages9
JournalLife Sciences
Volume53
Issue number10
DOIs
StatePublished - 1993

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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