Preprint Review Version 1 Preserved in Portico This version is not peer-reviewed

Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside

Stephen Ahenkorah
ORCID logo ,
Irwin Cassells
,
Christophe M Deroose
,
Thomas Cardinaels
,
Andrew R Burgoyne
,
Guy Bormans
,
Maarten Ooms
* ORCID logo ,
Frederik Cleeren
*
Version 1 : Received: 27 March 2021 / Approved: 29 March 2021 / Online: 29 March 2021 (14:43:57 CEST)

A peer-reviewed article of this Preprint also exists.

Ahenkorah, S.; Cassells, I.; Deroose, C.M.; Cardinaels, T.; Burgoyne, A.R.; Bormans, G.; Ooms, M.; Cleeren, F. Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside. Pharmaceutics 2021, 13, 599. Ahenkorah, S.; Cassells, I.; Deroose, C.M.; Cardinaels, T.; Burgoyne, A.R.; Bormans, G.; Ooms, M.; Cleeren, F. Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside. Pharmaceutics 2021, 13, 599.

Abstract

Besides external high-energy photon or proton beam therapy, targeted radionuclide therapy (TRNT) is an alternative approach to deliver radiation to cancer cells. TRNT is distributed within the body by the vascular system and allows targeted irradiation of a primary tumor and all its metastases, resulting in substantially less collateral damage to normal tissues as compared to ex-ternal beam radiotherapy (EBRT). It is a systemic cancer therapy, tackling systemic spread of the disease, which is the cause of death in most cancer patients. The α-emitting radionuclide bis-muth-213 (213Bi) has interesting properties and can be considered as a magic bullet for TRNT. The benefits and drawbacks of targeted alpha therapy with 213Bi are discussed in this review, covering the entire chain from radionuclide production to bedside. First, the radionuclide properties and production of 225Ac and its daughter 213Bi are discussed, followed by the fundamental chemical properties of bismuth. Next, an overview of available acyclic and macrocyclic bifunctional chelators for bismuth, and general considerations for designing a 213Bi-radiopharmaceutical are provided. Finally, we will provide an overview of preclinical and clinical studies involving 213Bi-radiopharmaceuticals, as well as the future perspectives of this promising cancer treatment option.

Keywords

Bismuth-213; Targeted Radionuclide Therapy; Targeted alpha Therapy; radiopharmaceutical; bifunctional chelator; vector molecule

Subject

Medicine and Pharmacology, Immunology and Allergy

Copyright: This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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