A Cursory Gaze at Solitary Radiopharmaceutical Chelators Incorporating Macrocyclic and Acyclic Moieties

Radiopharmaceutical development usually requires chelators to route radiometals to specific cancer targets. However, there is no universal chelator. To reduce off-target side effects, new chelators are needed as the radiometal toolset grows. DOTA is the most often used chelator for radiometals in radiopharmaceutical development, however DOTA's extreme conditions make it unsuitable for labeling heat sensitive biological vectors. The ideal chelator should be thermodynamically and kinetically stable, allowing labeling under mild conditions (~37 °C). In recent years, new hybrid chelators with enhanced characteristics have emerged, warranting further investigation for medical applications. This paper aims to discuss some of these promising chelators.

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Publication Details

Journal
Pharmaceutics
Published
2025-11-22
DOI
https://doi.org/10.3390/pharmaceutics17121508
Primary Topic
Radiopharmaceutical Chemistry and Applications
Type
article
Field-Weighted Citation Impact
0.00
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article

A Cursory Gaze at Solitary Radiopharmaceutical Chelators Incorporating Macrocyclic and Acyclic Moieties

Danni Ramdhani, Stephen Ahenkorah
Pharmaceutics
Radiopharmaceutical Chemistry and Applications
article

A Cursory Gaze at Solitary Radiopharmaceutical Chelators Incorporating Macrocyclic and Acyclic Moieties

Danni Ramdhani, Stephen Ahenkorah
article en

Abstract

Radiopharmaceutical development usually requires chelators to route radiometals to specific cancer targets. However, there is no universal chelator. To reduce off-target side effects, new chelators are needed as the radiometal toolset grows. DOTA is the most often used chelator for radiometals in radiopharmaceutical development, however DOTA's extreme conditions make it unsuitable for labeling heat sensitive biological vectors. The ideal chelator should be thermodynamically and kinetically stable, allowing labeling under mild conditions (~37 °C). In recent years, new hybrid chelators with enhanced characteristics have emerged, warranting further investigation for medical applications. This paper aims to discuss some of these promising chelators.

PharmaceuticsVol. 17(12)
University of Iowa (US), University of Iowa Health Care (US), Padjadjaran University (ID)
Openalex Percentile: Top 49%
Radiopharmaceutical Chemistry and Applications
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