Title: An octadentate chelator based on 3,4-hydroxypyridinones for 89Zr4+ and 213Bi3+ chelation
Authors: CUSNIR RUSLANFOLEY CALUM ALANGE JACLYN LIMBERTI CINZIAMORGENSTERN ALFREDBRUCHERTSEIFER FRANKBLOWER PHILMA MICHELLE
Citation: JOURNAL OF NUCLEAR MEDICINE vol. 58 no. S1 p. 889
Publisher: SOC NUCLEAR MEDICINE INC
Publication Year: 2017
JRC N°: JRC105539
ISSN: 0161-5505
URI: http://jnm.snmjournals.org/content/58/supplement_1/889.abstract
http://publications.jrc.ec.europa.eu/repository/handle/JRC105539
Type: Articles in periodicals and books
Abstract: The successful application of radiometals for diagnosis and therapy in nuclear medicine requires chelators that efficiently and stably complex the radiometal at low chelator concentration, preferably under mild reaction conditions. We aim to develop new chelators for the radiometals 89Zr and 213Bi. 89Zr (beta+, t1/2 78 h), has utility in PET imaging of antibodies, which require 2 - 5 days post-injection to localize at target tissue prior to imaging. The hexadentate tris(hydroxamate), desferrioxamine-B can coordinate 89Zr4+, but there is some evidence of in vivo instability. The radiotherapeutic alpha-emitting metal, 213Bi (t1/2 45 min) has demonstrated clinical efficacy, but the currently used chelator, DOTA, requires heating at high temperatures to incorporate 213Bi. Based on our previous experience of hexadentate tris(hydroxypyridinone) chelators that demonstrate high affinity for oxophilic metal ions, we aimed to develop an octadentate tetrakis(hydroxypyridinone) ligand containing four 3,4-hydroxypyridinone groups, and evaluate its ability to coordinate 89Zr4+ and 213Bi3+ under mild reaction conditions.
JRC Directorate:Nuclear Safety and Security

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