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Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers


Boros, Eszter; Holland, Jason P (2018). Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers. Journal of Labelled Compounds and Radiopharmaceuticals, 61(9):652-671.

Abstract

Radiometals are becoming increasingly accessible and are utilized frequently in the design of radiotracers for imaging and therapy. Nuclear properties ranging from the emission of γ‐rays and β+‐particles (imaging) to Auger electron and β− and α‐particles (therapy) in combination with long half‐lives are ideally matched with the relatively long biological half‐life of monoclonal antibodies in vivo. Radiometal labeling of antibodies requires the incorporation of a metal chelate onto the monoclonal antibody. This chelate must coordinate the metal under mild conditions required for the handling of antibodies, as well as provide high kinetic, thermodynamic, and metabolic stability once the metal ion is coordinated to prevent release of the radionuclide before the target site is reached in vivo. Herein, we review the role of different radiometals that have found applications of the design of radiolabeled antibodies for imaging and radioimmunotherapy. Each radionuclide is described regarding its nuclear synthesis, coordinative preference, and radiolabeling properties with commonly used and novel chelates, as well as examples of their preclinical and clinical applications. An overview of recent trends in antibody‐based radiopharmaceuticals is provided to spur continued development of the chemistry and application of radiometals for imaging and therapy.

Abstract

Radiometals are becoming increasingly accessible and are utilized frequently in the design of radiotracers for imaging and therapy. Nuclear properties ranging from the emission of γ‐rays and β+‐particles (imaging) to Auger electron and β− and α‐particles (therapy) in combination with long half‐lives are ideally matched with the relatively long biological half‐life of monoclonal antibodies in vivo. Radiometal labeling of antibodies requires the incorporation of a metal chelate onto the monoclonal antibody. This chelate must coordinate the metal under mild conditions required for the handling of antibodies, as well as provide high kinetic, thermodynamic, and metabolic stability once the metal ion is coordinated to prevent release of the radionuclide before the target site is reached in vivo. Herein, we review the role of different radiometals that have found applications of the design of radiolabeled antibodies for imaging and radioimmunotherapy. Each radionuclide is described regarding its nuclear synthesis, coordinative preference, and radiolabeling properties with commonly used and novel chelates, as well as examples of their preclinical and clinical applications. An overview of recent trends in antibody‐based radiopharmaceuticals is provided to spur continued development of the chemistry and application of radiometals for imaging and therapy.

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Additional indexing

Item Type:Journal Article, refereed, further contribution
Communities & Collections:07 Faculty of Science > Department of Chemistry
Dewey Decimal Classification:540 Chemistry
Scopus Subject Areas:Physical Sciences > Analytical Chemistry
Life Sciences > Biochemistry
Health Sciences > Radiology, Nuclear Medicine and Imaging
Life Sciences > Drug Discovery
Physical Sciences > Spectroscopy
Physical Sciences > Organic Chemistry
Uncontrolled Keywords:Organic Chemistry, Analytical Chemistry, Spectroscopy, Biochemistry, Drug Discovery, Radiology Nuclear Medicine and imaging
Language:English
Date:1 July 2018
Deposited On:07 Mar 2019 08:21
Last Modified:29 Jul 2020 10:07
Publisher:Wiley-Blackwell Publishing, Inc.
ISSN:0362-4803
Additional Information:This is the peer reviewed version of the following articl Boros, Eszter; Holland, Jason P (2018). Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers. Journal of Labelled Compounds and Radiopharmaceuticals, 61(9):652-671., which has been published in final form at https://doi.org/10.1002/jlcr.3590. This article may be used for non-commercial purposes in accordance with Wiley Terms and Conditions for Use of Self-Archived Versions. (http://www.wileyauthors.com/self-archiving)
OA Status:Green
Publisher DOI:https://doi.org/10.1002/jlcr.3590
Project Information:
  • : FunderSNSF
  • : Grant IDPP00P2_163683
  • : Project TitleAdvanced radiochemical methods for multi-modal imaging with nanomedicines
  • : FunderH2020
  • : Grant ID676904
  • : Project TitleNanoSCAN - Developing multi-modality nanomedicines for targeted annotation of oncogenic signaling pathways
  • : FunderERC
  • : Grant ID
  • : Project TitleStG 2015
  • : FunderNHLBI
  • : Grant IDK99HL125728
  • : Project TitleK99 Pathway to Independence award

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