16 beta-[18F]fluoromoxestrol: a potent, metabolically stable positron emission tomography imaging agent for estrogen receptor positive human breast tumors.
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.
VanBrocklin
H F
HF
Division of Radiation Sciences, Mallinckrodt Institute of Radiology, Washington University Medical School, St. Louis, MO 63110.
Rocque
P A
PA
Lee
H V
HV
Carlson
K E
KE
Katzenellenbogen
J A
JA
Welch
M J
MJ
D000818:Animals; D001943:Breast Neoplasms / Q000000981:diagnostic imaging* / Q000648:ultrastructure*; D004997:Ethinyl Estradiol / Q000031:analogs & derivatives*; D005260:Female; D005462:Fluorine Radioisotopes; D006801:Humans; D008099:Liver / Q000166:cytology / Q000378:metabolism; D051381:Rats; D017207:Rats, Sprague-Dawley; D011960:Receptors, Estrogen / Q000032:analysis*; D014055:Tomography, Emission-Computed
D005462:Fluorine Radioisotopes; D011960:Receptors, Estrogen; C082743:fluoromoxestrol; D004997:Ethinyl Estradiol