The Evolving Coordination Chemistry of Radiometals for Targeted Alpha Therapy

Melyssa L. Grieve; Brett M. Paterson

doi:10.1071/CH21184

REVIEW (Open Access)

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The Evolving Coordination Chemistry of Radiometals for Targeted Alpha Therapy

Melyssa L. Grieve

^A and Brett M. Paterson

^A ^B ^C

+ Author Affiliations

- Author Affiliations

^A School of Chemistry, Monash University, Clayton, Vic. 3800, Australia.

^B Monash Biomedical Imaging, Monash University, Clayton, Vic. 3800, Australia.

^C Corresponding author. Email: brett.paterson@monash.edu

Melyssa Grieve graduated from Monash University in 2019 with a Bachelor of Science – Advanced Research (Honours) majoring in genetics and chemistry. In 2020 she joined the group of Dr Brett Paterson at Monash University as a Ph.D. student working on developing chelators for use in radiopharmaceuticals.

Dr Brett Paterson is a graduate of the University of Melbourne where Professor Paul Donnelly supervised his Ph.D. studies. This was followed by post-doctoral research with Professor Donnelly and a Victorian Post-Doctoral Fellowship at King's College London with Professor Phil Blower. Dr Paterson returned to Australia and received a Discovery Early Career Research Award from the Australian Research Council, which he undertook at Monash University. Dr Paterson was a National Imaging Facility Fellow at Monash Biomedical Imaging and is currently Head of Radiochemistry at the Centre for Advanced Imaging, University of Queensland.

Australian Journal of Chemistry 75(2) 65-88 https://doi.org/10.1071/CH21184
Submitted: 2 August 2021 Accepted: 29 October 2021 Published: 7 December 2021

Journal Compilation © CSIRO 2022 Open Access CC BY

Abstract

Several radiometals are of interest in the development of new α-emitting radiopharmaceuticals. This review highlights the role of coordination chemistry in the design of ²²⁵Ac, ^212/213Bi, ²¹²Pb, ¹⁴⁹Tb, ²²⁷Th, and ^223/224Ra radiopharmaceuticals to treat cancer. Several chelators have recently been developed that are addressing the specific requirements of each radiometal to provide outstanding radiolabelling and in vivo properties. These advances are supporting the momentum that is building around radiopharmaceuticals for targeted α therapy.

Keywords: radiometals, targeted alpha therapy, coordination chemistry, radiopharmaceuticals, radiolabelling, chelators, inorganic chemistry, nuclear medicine.

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