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

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...

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Veröffentlicht in:Applied radiation and isotopes 2019-12, Vol.154, p.108854
Hauptverfasser: Tejería, Emilia, Giglio, Javier, Fernández, Leticia, Rey, Ana
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Sprache:eng
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Zusammenfassung: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.
ISSN:1872-9800
DOI:10.1016/j.apradiso.2019.108854