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Heskamp S, Raavé R, Boerman O, Rijpkema M, Goncalves V, Denat F.

Bioconjug Chem. 2017 Aug 24. doi: 10.1021/acs.bioconjchem.7b00325.

Abstract

Immuno-positron emission tomography (immunoPET) with ⁸⁹Zr-labeled antibodies has shown great potential in cancer imaging. It can provide important information about the pharmacokinetics and tumor-targeting properties of monoclonal antibodies and may help in anticipating on toxicity. Furthermore, it allows accurate dose planning for individualized radioimmunotherapy and may aid in patient selection and early-response monitoring for targeted therapies. The most commonly used chelator for ⁸⁹Zr is desferrioxamine (DFO). Preclinical studies have shown that DFO is not an ideal chelator because the ⁸⁹Zr–DFO complex is partly unstable in vivo, which results in the release of ⁸⁹Zr from the chelator and the subsequent accumulation of ⁸⁹Zr in bone. This bone accumulation interferes with accurate interpretation and quantification of bone uptake on PET images. Therefore, there is a need for novel chelators that allow more stable complexation of ⁸⁹Zr. In this Review, we will describe the most recent developments in ⁸⁹Zr radiochemistry, including novel chelators and site-specific conjugation methods.