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Auger-Emitting Radionuclides in Radiopharmaceutical Research: Decay-Associated Processes, Vector-Dependent
Klaus Schomäcker1, Ferdinand Sudbrock1, Melanie Freifrau von Brandenstein2
1Department of Nuclear Medicine, Faculty of Medicine and University Hospital Cologne, University of Cologne, Kerpener Str. 62, 50937 Cologne, Germany.
International Journal of Molecular Sciences
|July 28, 2026
Summary
Auger-emitting radionuclides offer targeted radiotherapy by concentrating radiation at the nanoscale. Their therapeutic effectiveness depends on decay location and cellular uptake, not just electron emission.
Area of Science:
- Nuclear medicine
- Radiopharmaceutical science
- Radiation biology
Background:
- Auger-electron-emitting radionuclides enable molecular-scale radiotherapy due to highly localized energy deposition.
- Biological effects are dictated by the nanoscale decay location, not long-range penetration.
- Understanding these factors is crucial for developing effective radiopharmaceuticals.
Purpose of the Study:
- To review Auger-emitting radionuclides from a radiopharmaceutical perspective.
- To integrate decay physics, cellular dosimetry, subcellular targeting, and translational relevance.
- To clarify the distinct mechanisms of Auger radiotoxicity based on localization.
Main Methods:
- Discussion of physical determinants of Auger radiotoxicity (e.g., Auger electrons, ionization density).
- Application of cellular S values to demonstrate dose variation with localization (nucleus, cytoplasm, membrane).
- Analysis of specific radionuclides (e.g., Iodine-125, Iodine-123, Terbium-161) and diagnostic emitters (e.g., Technetium-99m, Indium-111, Gallium-67).
Main Results:
- Auger radiotoxicity is highly dependent on the source-target geometry within the cell.
- The DNA-incorporated Iodine-125 model is not universally applicable to receptor-targeted agents.
- Alternative localizations (nuclear, perinuclear, vesicular) yield distinct radiobiological effects.
- Terbium-161 acts as a hybrid emitter, and diagnostic emitters have overlooked radiobiological relevance.
Conclusions:
- Auger-emitter radiopharmaceuticals require integrated assessment of decay physics, dosimetry, and cellular behavior.
- Ranking by electron yield alone is insufficient; therapeutic relevance depends on complex interactions.
- Intracellular trafficking, retention, and dose delivery timing are critical for efficacy and toxicity.
Keywords:
Auger electronsCoster–Kronig electronsCoulomb explosionDNA damagecellular dosimetryinternal conversion electronsradiopharmaceutical therapysubcellular localizationtechnetium-99mterbium-161More Related Videos
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