Importance of an alkyl group inserted into the DOTA backbone for reducing renal radioactivity levels of 111In-labeled antibody fragments

Hiroyuki Suzuki; Kento Ichinohe; Mari Araki; Kento Kannaka; Shingo Harada; Tetsuhiro Nemoto; Yasushi Arano; Tomoya Uehara

doi:10.1016/j.nucmedbio.2026.109638

May 1, 2026Nuclear Medicine and BiologyOpen Access

Importance of an alkyl group inserted into the DOTA backbone for reducing renal radioactivity levels of 111In-labeled antibody fragments

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Key Points

This research aims to evaluate how alkyl groups in the DOTA backbone influence the renal radioactivity of 111In-labeled antibody fragments.
Performed DFT calculations to assess coordination environments of In-DO3AEt-Bn and In-DO3A i Bu-Bn.
Compared renal radioactivity levels of [111In]In-DO3AEt-Bn-FGK-Fab with a reference.
Analyzed the structural differences in radiometabolites and their effects on renal cell residence time.
In-DO3AEt-Bn-FGK-Fab exhibited moderate renal radioactivity reduction compared to the reference.
DFT calculations indicated high similarity in coordination environments of different alkyl derivatives.
Small structural changes in radiometabolites led to significant variations in residence time in renal cells.

Implication

Investigates the impact of alkyl groups on renal radioactivity in antibody fragments, suggesting structural changes matter.

Abstract

• DFT calculations suggested that In-DO3AEt-Bn and In-DO3A i Bu-Bn would show a high similarity in their coordination environments. • [ 111 In]In-DO3AEt-Bn-FGK-Fab showed a moderate reduction in renal radioactivity levels compared to the reference • A slight difference in the structure of radiometabolites severely affects their residence time in renal cells.

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Cite This Study

Suzuki et al. (2026) studied this question.

synapsesocial.com/papers/6a192c45fab5b468c441529a https://doi.org/10.1016/j.nucmedbio.2026.109638

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Importance of an alkyl group inserted into the DOTA backbone for reducing renal radioactivity levels of 111In-labeled antibody fragments

Key Points

Implication

Abstract

Discussion

Cite This Study

Importance of an alkyl group inserted into the DOTA backbone for reducing renal radioactivity levels of 111In-labeled antibody fragments

Key Points

Implication

Abstract

Discussion

Cite This Study

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