Direct comparison of the in vitro and in vivo stability of DFO, DFO* and DFOcyclo* for ⁸⁹Zr-immunoPET.

ABSTRACT:

Purpose

Currently, the most commonly used chelator for labelling antibodies with ⁸⁹Zr for immunoPET is desferrioxamine B (DFO). However, preclinical studies have shown that the limited in vivo stability of the ⁸⁹Zr-DFO complex results in release of ⁸⁹Zr, which accumulates in mineral bone. Here we report a novel chelator DFOcyclo*, a preorganized extended DFO derivative that enables octacoordination of the ⁸⁹Zr radiometal. The aim was to compare the in vitro and in vivo stability of [⁸⁹Zr]Zr-DFOcyclo*, [⁸⁹Zr]Zr-DFO* and [⁸⁹Zr]Zr-DFO.

Methods

The stability of ⁸⁹Zr-labelled chelators alone and after conjugation to trastuzumab was evaluated in human plasma and PBS, and in the presence of exce

SUBMITTER: Raave R 

PROVIDER: S-EPMC6647232 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature