Cited by 120Radiopharmaceutical Chemistry and ApplicationsRadioactivity and Radon MeasurementsChemical Reactions and Isotopes

The DOI matches its Crossref record; 134 of the 141 references it cites were found in a registry or an index.

Bismuth-213 for targeted radionuclide therapy: from atom to bedside.

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Published version of a preprint

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.

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Crossref · 10.3390/pharmaceutics13050599

Cites

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Figures

Figure 1 General concept of TRNT. ROS = reactive oxygen species, SSB = single strand break, DSB = double strand break, APC = antigen presenting cells, CD6 = cluster of differentiation 6. The DNA structure was reproduced from Gill and Vallis 2019, with permission from the Royal Society of Chemistry [9], Royal Society of Chemistry, 2019.
Figure 1 General concept of TRNT. ROS = reactive oxygen species, SSB = single strand break, DSB = double strand break, APC = antigen presenting cells, CD6 = cluster of differentiation 6. The DNA structure was reproduced from Gill and Vallis 2019, with permission from the Royal Society of Chemistry [9], Royal Society of Chemistry, 2019.CC BY · PubMed Central
Figure 2 Decay chain of thorium-229 to 225Ac and 213Bi.
Figure 2 Decay chain of thorium-229 to 225Ac and 213Bi.CC BY · PubMed Central
Figure 3 (A) Production routes for 225Ac and (B) the 225Ac/213Bi generator.
Figure 3 (A) Production routes for 225Ac and (B) the 225Ac/213Bi generator.CC BY · PubMed Central
Figure 4 Some structures of bifunctional chelators currently used for 213Bi (A) DTPA and 1B4M-DTPA (B) CHX-A’’-DTPA, (C) DOTA, (D) Me-DO2PA, (E) PEPA, (F) H4neunpa, (G) 3p-C-NETA (H) 3p-C-DEPA and (I) C-NE3TA.
Figure 4 Some structures of bifunctional chelators currently used for 213Bi (A) DTPA and 1B4M-DTPA (B) CHX-A’’-DTPA, (C) DOTA, (D) Me-DO2PA, (E) PEPA, (F) H4neunpa, (G) 3p-C-NETA (H) 3p-C-DEPA and (I) C-NE3TA.CC BY · PubMed Central
Figure 5 Crystal structure of NaBiDOTA·H2O. Reprinted (adapted) from E. Brücher et al., 2003, with permission from [58]; American Chemical Society, 2003.
Figure 5 Crystal structure of NaBiDOTA·H2O. Reprinted (adapted) from E. Brücher et al., 2003, with permission from [58]; American Chemical Society, 2003.CC BY · PubMed Central
Figure 6 The size of the vector molecule determines the residence time of blood, tumor accumulation, radiotoxicity, target-to-blood ratio, and imaging contrast of the radiopharmaceutical. Image was adapted from Hong H. et al., 2008 and modified with permission from [79], SAGE Journals, 2008.
Figure 6 The size of the vector molecule determines the residence time of blood, tumor accumulation, radiotoxicity, target-to-blood ratio, and imaging contrast of the radiopharmaceutical. Image was adapted from Hong H. et al., 2008 and modified with permission from [79], SAGE Journals, 2008.CC BY · PubMed Central

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Research works printed but not linked: 1

  1. Finn, 2017, A Phase 2 Study of Actinium-225 (225Ac)-Lintuzumab in Older Patients with Previously Untreated Acute Myeloid Leukemia (AML) Unfit for Intensive Chemotherapy, Blood, 130, 2638

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Metadata

Authors
Ahenkorah, S., Cassells, I., Deroose, C. M., Cardinaels, T., Burgoyne, A. R., Bormans, G., Ooms, M., & Cleeren, F.
Affiliations
  • Belgian Nuclear Research Centre (BE)
  • Universitair Ziekenhuis Leuven (BE)
  • KU Leuven (BE)
Corresponding author
  • Ooms, Maarten
  • Cleeren, Frederik
Venue
Pharmaceutics
Publisher
MDPI AG
Published
2021-04-21
Volume
13
Issue
5
Pages
599
ISSN
1999-4923 (ISSN-L)
OpenAlex
W3145208530
Cited by
120
References
141
Citations by year
2026: 21 · 2025: 26 · 2024: 24 · 2023: 24 · 2022: 19 · 2021: 6
FWCI
2.98
Type
journal article
Language
en
Open access
Locations
  • Pharmaceutics (publishedVersion, cc-by)
  • Preprints.org (acceptedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
  • Lirias (submittedVersion, other-oa)
  • DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Funders
Fonds Wetenschappelijk Onderzoek (12R3119N)
Topics
  • Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
  • Physical Sciences › Physics and Astronomy › Radiation › Radioactivity and Radon Measurements
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Chemical Reactions and Isotopes
Keywords
bismuth-213, targeted radionuclide therapy, targeted alpha therapy, actinium-225, radioisotope production, bifunctional chelators, macrocyclic chelators, radiopharmaceutical design, bismuth chemistry, alpha-emitting radionuclides, cancer therapy

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