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

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.

Automated summary

Tetrazine ligation, as a bio-orthogonal chemistry tool, has gained interest in nuclear medicine for pretargeted approaches, with the potential to revolutionize theranostic strategies. Pretargeting can increase target-to-background ratios and reduce dose to healthy tissue. Combined with diagnostic imaging, pretargeting may be optimal for theranostic approaches.