Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside
In contrast to external high energy photon or proton therapy, targeted radionuclide therapy (TRNT) is a systemic cancer treatment allowing targeted irradiation of a primary tumor and all its metastases, resulting in less collateral damage to normal tissues. The α-emitting radionuclide bismuth-213 (&...
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| Format: | Article |
| Language: | English |
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MDPI AG
2021-04-01
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| Series: | Pharmaceutics |
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| Online Access: | https://www.mdpi.com/1999-4923/13/5/599 |
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| author | Stephen Ahenkorah Irwin Cassells Christophe M. Deroose Thomas Cardinaels Andrew R. Burgoyne Guy Bormans Maarten Ooms Frederik Cleeren |
| author_facet | Stephen Ahenkorah Irwin Cassells Christophe M. Deroose Thomas Cardinaels Andrew R. Burgoyne Guy Bormans Maarten Ooms Frederik Cleeren |
| author_sort | Stephen Ahenkorah |
| collection | DOAJ |
| description | In contrast to external high energy photon or proton therapy, targeted radionuclide therapy (TRNT) is a systemic cancer treatment allowing targeted irradiation of a primary tumor and all its metastases, resulting in less collateral damage to normal tissues. The α-emitting radionuclide bismuth-213 (<sup>213</sup>Bi) has interesting properties and can be considered as a magic bullet for TRNT. The benefits and drawbacks of targeted alpha therapy with <sup>213</sup>Bi are discussed in this review, covering the entire chain from radionuclide production to bedside. First, the radionuclide properties and production of <sup>225</sup>Ac and its daughter <sup>213</sup>Bi 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 <sup>213</sup>Bi-radiopharmaceutical are provided. Finally, we provide an overview of preclinical and clinical studies involving <sup>213</sup>Bi-radiopharmaceuticals, as well as the future perspectives of this promising cancer treatment option. |
| first_indexed | 2024-03-10T12:06:38Z |
| format | Article |
| id | doaj.art-53fe69a71bb745bdbf24088894bf1111 |
| institution | Directory Open Access Journal |
| issn | 1999-4923 |
| language | English |
| last_indexed | 2024-03-10T12:06:38Z |
| publishDate | 2021-04-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Pharmaceutics |
| spelling | doaj.art-53fe69a71bb745bdbf24088894bf11112023-11-21T16:33:22ZengMDPI AGPharmaceutics1999-49232021-04-0113559910.3390/pharmaceutics13050599Bismuth-213 for Targeted Radionuclide Therapy: From Atom to BedsideStephen Ahenkorah0Irwin Cassells1Christophe M. Deroose2Thomas Cardinaels3Andrew R. Burgoyne4Guy Bormans5Maarten Ooms6Frederik Cleeren7Institute for Nuclear Materials Science, Belgian Nuclear Research Center (SCK CEN), 2400 Mol, BelgiumInstitute for Nuclear Materials Science, Belgian Nuclear Research Center (SCK CEN), 2400 Mol, BelgiumNuclear Medicine Unit, University Hospitals Leuven, 3000 Leuven, BelgiumInstitute for Nuclear Materials Science, Belgian Nuclear Research Center (SCK CEN), 2400 Mol, BelgiumInstitute for Nuclear Materials Science, Belgian Nuclear Research Center (SCK CEN), 2400 Mol, BelgiumRadiopharmaceutical Research, Department of Pharmacy and Pharmacology, University of Leuven, 3000 Leuven, BelgiumInstitute for Nuclear Materials Science, Belgian Nuclear Research Center (SCK CEN), 2400 Mol, BelgiumRadiopharmaceutical Research, Department of Pharmacy and Pharmacology, University of Leuven, 3000 Leuven, BelgiumIn contrast to external high energy photon or proton therapy, targeted radionuclide therapy (TRNT) is a systemic cancer treatment allowing targeted irradiation of a primary tumor and all its metastases, resulting in less collateral damage to normal tissues. The α-emitting radionuclide bismuth-213 (<sup>213</sup>Bi) has interesting properties and can be considered as a magic bullet for TRNT. The benefits and drawbacks of targeted alpha therapy with <sup>213</sup>Bi are discussed in this review, covering the entire chain from radionuclide production to bedside. First, the radionuclide properties and production of <sup>225</sup>Ac and its daughter <sup>213</sup>Bi 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 <sup>213</sup>Bi-radiopharmaceutical are provided. Finally, we provide an overview of preclinical and clinical studies involving <sup>213</sup>Bi-radiopharmaceuticals, as well as the future perspectives of this promising cancer treatment option.https://www.mdpi.com/1999-4923/13/5/599bismuth-213targeted radionuclide therapytargeted alpha therapyradiopharmaceuticalbifunctional chelatorvector molecule |
| spellingShingle | Stephen Ahenkorah Irwin Cassells Christophe M. Deroose Thomas Cardinaels Andrew R. Burgoyne Guy Bormans Maarten Ooms Frederik Cleeren Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside Pharmaceutics bismuth-213 targeted radionuclide therapy targeted alpha therapy radiopharmaceutical bifunctional chelator vector molecule |
| title | Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside |
| title_full | Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside |
| title_fullStr | Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside |
| title_full_unstemmed | Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside |
| title_short | Bismuth-213 for Targeted Radionuclide Therapy: From Atom to Bedside |
| title_sort | bismuth 213 for targeted radionuclide therapy from atom to bedside |
| topic | bismuth-213 targeted radionuclide therapy targeted alpha therapy radiopharmaceutical bifunctional chelator vector molecule |
| url | https://www.mdpi.com/1999-4923/13/5/599 |
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