Recent Advances in the Development of Tetrazine Ligation Tools for Pretargeted Nuclear Imaging

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Tetrazine ligation has gained interest as a bio-orthogonal chemistry tool within the last decade. In nuclear medicine, tetrazine ligation is currently being explored for pretargeted approaches, which have the potential to revolutionize state-of-the-art theranostic strategies. Pretargeting has been shown to increase target-to-background ratios for radiopharmaceuticals based on nanomedicines, especially within early timeframes. This allows the use of radionuclides with short half-lives which are more suited for clinical applications. Pretargeting bears the potential to increase the therapeutic dose delivered to the target as well as reduce the respective dose to healthy tissue. Combined with the possibility to be applied for diagnostic imaging, pretargeting could be optimal for theranostic approaches. In this review, we highlight efforts that have been made to radiolabel tetrazines with an emphasis on imaging.

Original languageEnglish
Article number685
JournalPharmaceuticals
Volume15
Issue number6
Number of pages25
ISSN1424-8247
DOIs
Publication statusPublished - 2022

Bibliographical note

Funding Information:
Funding: This project received funding from the European Union’s EU Framework Programme for Research and Innovation Horizon 2020 under grant agreement no. 668532, and from the European Union’s Horizon 2020 research and innovation program under the Marie Skłodowska-Curie grant agreement no. 813528. M.M.H. received funding from the European Union’s EU Framework Programme for Research and Innovation Horizon 2020 (grant agreement no. 670261). The Lundbeck Foundation, the Novo Nordisk Foundation, the Innovation Fund Denmark, and the Research Council for Independent Research (grant agreement no. 8022-00187B) are further acknowledged.

    Research areas

  • bio-orthogonal chemistry, molecular imaging, pretargeted imaging, tetrazine ligation

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