Targeted alpha therapy: progress in radionuclide production, radiochemistry, and applications.

Nelson, Bryce J. B.; Andersson, Jan D.; Wuest, Frank

doi:10.3390/pharmaceutics13010049

Cited by 194Radiopharmaceutical Chemistry and ApplicationsChemical Reactions and IsotopesRadioactivity and Radon Measurements

Targeted alpha therapy: progress in radionuclide production, radiochemistry, and applications.

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Nelson, Bryce J. B., Andersson, Jan D., Wuest, Frank·2020·Pharmaceutics

DOI 10.3390/pharmaceutics13010049PMC PMC7824049

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Abstract

This review outlines the accomplishments and potential developments of targeted alpha (α) particle therapy (TAT). It discusses the therapeutic advantages of the short and highly ionizing path of α-particle emissions; the ability of TAT to complement and provide superior efficacy over existing forms of radiotherapy; the physical decay properties and radiochemistry of common α-emitters, including 225Ac, 213Bi, 224Ra, 212Pb, 227Th, 223Ra, 211At, and 149Tb; the production techniques and proper handling of α-emitters in a radiopharmacy; recent preclinical developments; ongoing and completed clinical trials; and an outlook on the future of TAT.

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The isomeric gamma emissions with energy suitable for SPECT imaging grant 225Ac the theranostic possibility.
“Moreover, the isomeric γ emissions with energy suitable for SPECT imaging grants 225Ac the theranostic possibility (68, 69).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [68]

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Significant systemic therapeutic effects of high-LET immunoradiation by 212Pb-trastuzumab against prostatic tumors of androgen-independent human prostate cancer in mice
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The α-emitter astatine-211 targeted to CD38 can eradicate multiple myeloma in a disseminated disease model
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First in vivo evaluation of liposome-encapsulated 223Ra as a potential alpha-particle-emitting cancer therapeutic agent.
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In Vitro comparison of 213Bi- and 177Lu-radiation for peptide receptor radionuclide therapy
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Vascular Targeted Radioimmunotherapy for the Treatment of Glioblastoma
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Ra‐224 labeling of calcium carbonate microparticles for internal α‐therapy: Preparation, stability, and biodistribution in mice
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An Appendix of Radionuclides Used in Targeted Alpha Therapy
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Intratumoral 224Ra-loaded wires spread alpha-emitters inside solid human tumors in athymic mice achieving tumor control.
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Pharmacokinetics, microscale distribution, and dosimetry of alpha-emitter-labeled anti-PD-L1 antibodies in an immune competent transgenic breast cancer model
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Assessment of long-term radiotoxicity after treatment with the low-dose-rate alpha-particle-emitting radioimmunoconjugate 227Th-rituximab
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Alpha Particle Detection Using Alpha-Induced Air Radioluminescence: A Review and Future Prospects for Preliminary Radiological Characterisation for Nuclear Facilities Decommissioning
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α‐particle therapy for synovial sarcoma in the mouse using an astatine‐211‐labeled antibody against frizzled homolog 10
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Peptide Receptor Radionuclide Therapy Using 225Ac-DOTATOC Achieves Partial Remission in a Patient With Progressive Neuroendocrine Liver Metastases After Repeated β-Emitter Peptide Receptor Radionuclide Therapy
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cGMP production of astatine-211-labeled anti-CD45 antibodies for use in allogeneic hematopoietic cell transplantation for treatment of advanced hematopoietic malignancies
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Cross section measurements of 151Eu(3He,5n) reaction: new opportunities for medical alpha emitter 149Tb production
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212Pb-Labeled Antibody 225.28 Targeted to Chondroitin Sulfate Proteoglycan 4 for Triple-Negative Breast Cancer Therapy in Mouse Models
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Antitumor Activity of Novel Bone-seeking, α-emitting 224Ra-solution in a Breast Cancer Skeletal Metastases Model
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Radium-224 Retention, Distribution, and Dosimetry in Beagles
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Evaluation of astatine-211-labeled octreotide as a potential radiotherapeutic agent for NSCLC treatment
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The five “W”s and “How” of Targeted Alpha Therapy: Why? Who? What? Where? When? and How?
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Actinium
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Remote Optical Detection of Alpha Radiation
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Cherenkov light production from the α-emitting decay chains of 223Ra, 212Pb, and 149Tb for Cherenkov Luminescence Imaging
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Preclinical Development of an Actinium-225-Labeled Antibody Radio-Conjugate Directed Against CD45 for Targeted Conditioning and Radioimmunotherapy
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Development of 211At Production via Continuous Extraction of 211Rn
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Targeted α -Emitter Therapy with 212 Pb-DOTAMTATE for the Treatment of Metastatic SSTR-Expressing Neuroendocrine Tumors: First-in-Humans Dose-Escalation Clinical Trial
Delpassand, E. S., Tworowska, I., Esfandiari, R., Torgue, J., Hurt, J., Shafie, A., & Núñez, R. (2022) · Journal of Nuclear Medicine · doi:10.2967/jnumed.121.263230 · Cited by 199 · see citing works
Targeted Alpha-Particle Therapy: A Review of Current Trials
Jang, A., Kendi, A. T., Johnson, G. B., Halfdanarson, T. R., & Sartor, O. A. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms241411626 · Cited by 121 · see citing works
Uranium: The Nuclear Fuel Cycle and Beyond
Peluzo, B. M. T. C., & Kraka, E. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23094655 · Cited by 109 · see citing works
Radionuclides for Targeted Therapy: Physical Properties
Stokke, C., Kvassheim, M., & Blakkisrud, J. (2022) · Molecules · doi:10.3390/molecules27175429 · Cited by 105 · see citing works
PSMA-Targeting Imaging and Theranostic Agents—Current Status and Future Perspective
Debnath, S., Zhou, N., McLaughlin, M. F., Rice, S. L., Pillai, A. K., Hao, G., & Sun, X. (2022) · International Journal of Molecular Sciences · doi:10.3390/ijms23031158 · Cited by 92 · see citing works
Recent advances and impending challenges for the radiopharmaceutical sciences in oncology
Lapi, S. E., Scott, P. J. H., Scott, A. M., Windhorst, A. D., Zeglis, B. M., Abdel–Wahab, M., Baum, R. P., Buatti, J. M., Giammarile, F., Kiess, A. P., et al. (2024) · The Lancet Oncology · doi:10.1016/s1470-2045(24)00030-5 · Cited by 90 · see citing works
Preclinical and Clinical Status of PSMA-Targeted Alpha Therapy for Metastatic Castration-Resistant Prostate Cancer
Juzeniene, A., Stenberg, V. Y., Bruland, Ø. S., & Larsen, R. H. (2021) · Cancers · doi:10.3390/cancers13040779 · Cited by 89 · see citing works
Implementing Ac-225 labelled radiopharmaceuticals: practical considerations and (pre-)clinical perspectives
Hooijman, E. L., Radchenko, V., Ling, S. W., Konijnenberg, M., Brabander, T., Koolen, S. L. W., & de Blois, E. (2024) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-024-00239-1 · Cited by 88 · see citing works
Radioimmunotherapy in Oncology: Overview of the Last Decade Clinical Trials
Rondon, A., Rouanet, J., & Degoul, F. (2021) · Cancers · doi:10.3390/cancers13215570 · Cited by 74 · see citing works
Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists
Shi, M., Jakobsson, V., Greifenstein, L., Khong, P.-L., Chen, X., Baum, R. P., & Zhang, J. (2022) · Frontiers in Medicine · doi:10.3389/fmed.2022.1034315 · Cited by 68 · see citing works
H 2 BZmacropa-NCS: A Bifunctional Chelator for Actinium-225 Targeted Alpha Therapy
Kadassery, K. J., King, A., Fayn, S., Baidoo, K. E., MacMillan, S. N., Escorcia, F. E., & Wilson, J. J. (2022) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.2c00190 · Cited by 64 · see citing works
Development of radiopharmaceuticals for targeted alpha therapy: Where do we stand?
Pallares, R. M., & Abergel, R. J. (2022) · Frontiers in Medicine · doi:10.3389/fmed.2022.1020188 · Cited by 64 · see citing works
Peptide Binder to Glypican-3 as a Theranostic Agent for Hepatocellular Carcinoma
Lin, F., Clift, R., Ehara, T., Yanagida, H., Horton, S., Noncovich, A., Guest, M., Kim, D., Salvador, K., Richardson, S., et al. (2024) · Journal of Nuclear Medicine · doi:10.2967/jnumed.123.266766 · Cited by 58 · see citing works
Modulating the pharmacokinetic profile of Actinium-225-labeled macropa-derived radioconjugates by dual targeting of PSMA and albumin
Reissig, F., Zarschler, K., Nový, Z., Petřík, M., Bendová, K. D., Kurfürstová, D., Bouchal, J., Ludik, M.-C., Brandt, F., Kopka, K., et al. (2022) · Theranostics · doi:10.7150/thno.78043 · Cited by 53 · see citing works
Chromatin and the Cellular Response to Particle Radiation-Induced Oxidative and Clustered DNA Damage
Danforth, J. M., Provencher, L., & Goodarzi, A. A. (2022) · Frontiers in Cell and Developmental Biology · doi:10.3389/fcell.2022.910440 · Cited by 52 · see citing works
Recent progress of astatine-211 in endoradiotherapy: Great advances from fundamental properties to targeted radiopharmaceuticals
Li, F., Yang, Y., Liao, J., & Liu, N. (2022) · Chinese Chemical Letters · doi:10.1016/j.cclet.2022.03.025 · Cited by 45 · see citing works
In vitro and in vivo evaluation of 211At-labeled fibroblast activation protein inhibitor for glioma treatment
Ma, H., Li, F., Shen, G., Pan, L., Liu, W., Liang, R., Lan, T., Yang, Y., Yang, J., Liao, J., et al. (2022) · Bioorganic & Medicinal Chemistry · doi:10.1016/j.bmc.2021.116600 · Cited by 44 · see citing works
PSMA Theranostics: Science and Practice
Mokoala, K. M. G., Lawal, I. O., Lengana, T., Kgatle, M., Giesel, F. L., Vorster, M., & Sathekge, M. M. (2021) · Cancers · doi:10.3390/cancers13153904 · Cited by 43 · see citing works
First In Vivo and Phantom Imaging of Cyclotron-Produced 133La as a Theranostic Radionuclide for 225Ac and 135La
Nelson, B. J. B., Ferguson, S., Wuest, M., Wilson, J., Duke, M. J. M., Richter, S., Soenke-Jans, H., Andersson, J. D., Juengling, F. D., & Wuest, F. R. (2021) · Journal of Nuclear Medicine · doi:10.2967/jnumed.121.262459 · Cited by 43 · see citing works
Theranostic Imaging Surrogates for Targeted Alpha Therapy: Progress in Production, Purification, and Applications
Nelson, B. J. B., Wilson, J. S., Andersson, J. D., & Wuest, F. R. (2023) · Pharmaceuticals · doi:10.3390/ph16111622 · Cited by 40 · see citing works
68Ga- and 211At-Labeled RGD Peptides for Radiotheranostics with Multiradionuclides
Ogawa, K., Echigo, H., Mishiro, K., Hirata, S., Washiyama, K., Kitamura, Y., Takahashi, K., Shiba, K., & Kinuya, S. (2021) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.1c00460 · Cited by 39 · see citing works
Radiometals in Imaging and Therapy: Highlighting Two Decades of Research
Sharma, S., & Pandey, M. K. (2023) · Pharmaceuticals · doi:10.3390/ph16101460 · Cited by 39 · see citing works
Targeted Alpha Therapy: All We Need to Know about 225Ac’s Physical Characteristics and Production as a Potential Theranostic Radionuclide
Jalloul, W., Ghizdovăţ, V., Stolniceanu, C. R., Ionescu, T. M., Grierosu, I. C., Păvăleanu, I., Moscalu, M., & Ştefănescu, C. (2023) · Pharmaceuticals · doi:10.3390/ph16121679 · Cited by 40 · see citing works
Alpha Atlas: Mapping global production of α-emitting radionuclides for targeted alpha therapy
Tosato, M., Favaretto, C., Kleynhans, J., Burgoyne, A. R., Gestin, J., van der Meulen, N. P., Jalilian, A. R., Köster, U., Asti, M., & Radchenko, V. (2024) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2024.108990 · Cited by 38 · see citing works
The Potentiation of Anti-Tumor Immunity by Tumor Abolition with Alpha Particles, Protons, or Carbon Ion Radiation and Its Enforcement by Combination with Immunoadjuvants or Inhibitors of Immune Suppressor Cells and Checkpoint Molecules
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Dying of Stress: Chemotherapy, Radiotherapy, and Small-Molecule Inhibitors in Immunogenic Cell Death and Immunogenic Modulation
Fabian, K. P., Kowalczyk, J. T., Reynolds, S. T., & Hodge, J. W. (2022) · Cells · doi:10.3390/cells11233826 · Cited by 36 · see citing works
Development of probes for radiotheranostics with albumin binding moiety to increase the therapeutic effects of astatine-211 (211At)
Echigo, H., Mishiro, K., Munekane, M., Fuchigami, T., Washiyama, K., Takahashi, K., Kitamura, Y., Wakabayashi, H., Kinuya, S., & Ogawa, K. (2023) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-023-06457-0 · Cited by 35 · see citing works
Commercial and business aspects of alpha radioligand therapeutics
Ostuni, E., & Taylor, M. R. G. (2023) · Frontiers in Medicine · doi:10.3389/fmed.2022.1070497 · Cited by 35 · see citing works
Revolutionizing cancer treatment: The role of radiopharmaceuticals in modern cancer therapy
Varghese, T. P., John, A., & Mathew, J. (2024) · Precision Radiation Oncology · doi:10.1002/pro6.1239 · Cited by 34 · see citing works
A Radioluminescent Metal–Organic Framework for Monitoring 225 Ac in Vivo
Zhang, Y., Li, F., Cui, Z., Li, K., Guan, J., Tian, L., Wang, Y., Liu, N., Wu, W., Chai, Z., et al. (2023) · Journal of the American Chemical Society · doi:10.1021/jacs.3c02325 · Cited by 35 · see citing works
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Authors: Nelson, B. J. B., Andersson, J. D., & Wuest, F.
Affiliations: University of Alberta (CA)
Alberta Health Services (CA)
Corresponding author: Wuest, Frank
ORCID: Nelson, Bryce J. B.
Andersson, Jan D.
Wuest, Frank
Venue: Pharmaceutics
Publisher: MDPI AG
Published: 2020-12-31
Volume: 13
Issue: 1
Pages: 49
ISSN: 1999-4923 (ISSN-L)
DOI: 10.3390/pharmaceutics13010049
PMC: PMC7824049
OpenAlex: W3115246370
Cited by: 194
References: 123
Citations by year: 2026: 33 · 2025: 35 · 2024: 45 · 2023: 29 · 2022: 35 · 2021: 17
FWCI: 2.99
Type: journal article
Language: en
Open access: gold
doi.org
Licence: cc-by
creativecommons.org/licenses/by/4.0/ (vor)
Locations: Pharmaceutics (publishedVersion, cc-by)
Europe PMC (PubMed Central) (publishedVersion, other-oa)
PubMed Central (publishedVersion, cc-by)
PubMed (publishedVersion)
DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
Topics: Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Chemical Reactions and Isotopes
Health Sciences › Health Professions › Radiological and Ultrasound Technology › Radioactivity and Radon Measurements
Keywords: targeted alpha therapy, alpha-emitting radionuclides, radioisotope production, radiopharmacy, actinium-225, bismuth-213, radium-224, lead-212, thorium-227, radium-223, astatine-211, clinical trials, preclinical drug development

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Targeted alpha therapy: progress in radionuclide production, radiochemistry, and applications.

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