Abstract
The potential of both stereoisomers of 11β-methoxy-17α[ 123I]iodovinylestradiol (E- and Z-[ 123I]MIVE) as suitable radioligands for imaging of estrogen receptor(ER)-positive human breast tumours was studied. The 17α-[ 123I]iodovinylestradiol derivatives were prepared stereospecifically by oxidative radioiododestannylation of the corresponding 17α-tri- n-butylstannylvinylestradiol precursors. Both isomers of MIVE showed high in vitro affinity for dimethylbenzanthracene-induced rat and fresh human mammary tumour ER, that of Z-MIVE however being manyfold higher than that of E-MIVE. In vivo distribution studies with E- and Z-[ 123I]MIVE in normal and tumour-bearing female rats showed ER-mediated uptake and retention in uterus, ovaries, pituitary, hypothalamus and mammary tumours, again the highest for Z-[ 123I]MIVE. The uterus- and tumour-to-nontarget tissue (fat, muscle) uptake ratios were also highest for Z-[ 123I]MIVE. Additionally, planar whole body imaging of two breast cancer patients 1–2 h after injection of Z-[ 123I]MIVE showed increased focal uptake at known tumour sites. Therefore, we conclude that Z-[ 123I]MIVE is a promising radioligand for the diagnostic imaging of ER in human breast cancer.
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