An <sup>211</sup>At-labeled Tetrazine for Pretargeted Therapy

Pretargeted radioimmunoimaging has been shown to enhance tumor-to-background ratios by up to 125-fold at early time points, leading to more efficient and less toxic radionuclide therapies, particularly with shorter half-lives such as astatine-211 (<sup>211</sup>At). The tetrazine ligation is the most utilized bioorthogonal reaction in these strategies, making tetrazines ideal for <sup>211</sup>At labeling and controlling the biodistribution. We developed a <sup>211</sup>At-labeled pretargeting agent for alpha-radionuclide therapy, achieving a radiochemical yield of approximately 65% and purity over 99%. Our results showed higher tumor-to-blood ratios within the first 24 h compared to directly labeled monoclonal antibodies. This suggests that pretargeted therapy may deliver better tumor doses than conventional methods, although the deastatination observed will need to be addressed in future tetrazine developments.

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Publication Details

Journal
Journal of Medicinal Chemistry
Published
2025-02-18
DOI
https://doi.org/10.1021/acs.jmedchem.4c02281
Citations
6
Primary Topic
Radiopharmaceutical Chemistry and Applications
Type
article
Field-Weighted Citation Impact
8.16

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article

An 211At-labeled Tetrazine for Pretargeted Therapy

Rocío García‐Vázquez, Lars Hvass, Anne Skovsbo Clausen, Christian B. M. Poulie et al.
6 citations
Journal of Medicinal Chemistry
Radiopharmaceutical Chemistry and Applications
8.16
article

An 211At-labeled Tetrazine for Pretargeted Therapy

Rocío García‐Vázquez, Lars Hvass, Anne Skovsbo Clausen, Christian B. M. Poulie, Jesper Tranekjær Jørgensen, Matthias M. Herth, Andreas Kjær, Marius Müller, Ellinor Hansson, Emma Aneheim, Umberto Maria Battisti, Sture Lindegren, Vladimir Shalgunov, Tobias Gustavsson, Holger Jensen
article en
6 citations

Abstract

Pretargeted radioimmunoimaging has been shown to enhance tumor-to-background ratios by up to 125-fold at early time points, leading to more efficient and less toxic radionuclide therapies, particularly with shorter half-lives such as astatine-211 (<sup>211</sup>At). The tetrazine ligation is the most utilized bioorthogonal reaction in these strategies, making tetrazines ideal for <sup>211</sup>At labeling and controlling the biodistribution. We developed a <sup>211</sup>At-labeled pretargeting agent for alpha-radionuclide therapy, achieving a radiochemical yield of approximately 65% and purity over 99%. Our results showed higher tumor-to-blood ratios within the first 24 h compared to directly labeled monoclonal antibodies. This suggests that pretargeted therapy may deliver better tumor doses than conventional methods, although the deastatination observed will need to be addressed in future tetrazine developments.

Journal of Medicinal ChemistryVol. 68(4)
University of Copenhagen (DK), Rigshospitalet (DK), University of Gothenburg (SE)
Innovationsfonden, Carlsbergfondet, Lundbeckfonden, Danmarks Frie Forskningsfond, Novo Nordisk Fonden
Zero hunger
Openalex Percentile: Top 3%
Radiopharmaceutical Chemistry and Applications
8.16
DOISourceOpenAlex
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