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

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

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Ahenkorah, Stephen, Cassells, Irwin, Deroose, Christophe M., Cardinaels, Thomas, Burgoyne, Andrew R., Bormans, Guy, Ooms, Maarten, Cleeren, Frederik·2021·Pharmaceutics

DOI 10.3390/pharmaceutics13050599PMC PMC8143329

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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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Method
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Background
Treatment of carcinoma in situ of the urinary bladder with an alpha-emitter immunoconjugate targeting the epidermal growth factor receptor: a pilot study
Autenrieth, M. E., Seidl, C., Bruchertseifer, F., Horn, T. D., Kurtz, F., Feuerecker, B., D’Alessandria, C., Pfob, C. H., Nekolla, S. G., Apostolidis, C., et al. (2018) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-018-4003-6 · Cited by 74 · cited 11×
“The animals survived for an average of 131.8 d after fractionated treatment with 0.46 MBq 213Bi-anti-EGFR-mAb, with 30% survival for more than 300 d.”
BackgroundInfluential
Prognostic Significance of Somatostatin Receptor Heterogeneity in Progressive Neuroendocrine Tumor Treated with Lu-177 DOTATOC or Lu-177 DOTATATE
Graf, J., Pape, U., Jann, H., Denecke, T., Arsenić, R., Brenner, W., Pavel, M., & Prasad, V. (2019) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-019-04439-9 · Cited by 74
Equilibrium, 1H and 13C NMR Spectroscopy, and X-ray Diffraction Studies on the Complexes Bi(DOTA)- and Bi(DO3A-Bu)
Csajbók, É., Baranyai, Z., Bányai, I., Brücher, E., Király, R., Müller‐Fahrnow, A., Platzek, J., Radüchel, B., & Schäfer, M. (2003) · Inorganic Chemistry · doi:10.1021/ic0261272 · Cited by 73 · cited 1×
“Copyright (2003) American Chemical Society [67].”
Conventional and pretargeted radioimmunotherapy using bismuth-213 to target and treat non-Hodgkin lymphomas expressing CD20: a preclinical model toward optimal consolidation therapy to eradicate minimal residual disease
Park, S. I., Shenoi, J., Pagel, J. M., Hamlin, D. K., Wilbur, D. S., Orgun, N. N., Kenoyer, A. L., Frayo, S. L., Axtman, A., Bäck, T. A., et al. (2010) · Blood · doi:10.1182/blood-2010-05-282327 · Cited by 73
213Bi-PAI2 conjugate selectively induces apoptosis in PC3 metastatic prostate cancer cell line and shows anti-cancer activity in a xenograft animal model
Li, Y., Rizvi, S. M., Ranson, M., & Allen, B. (2002) · British Journal of Cancer · doi:10.1038/sj.bjc.6600179 · Cited by 73
Theranostic radionuclides: recent advances in production methodologies
Qaim, S. M. (2019) · Journal of Radioanalytical and Nuclear Chemistry · doi:10.1007/s10967-019-06797-y · Cited by 69 · cited 1×
“Me-DO2PA (Figure 4D), a [12] aneN4 bearing two picolinic acid arms and two methyl-capped amines, has also been reported to be stable in vivo when radiolabeled with 213Bi [60,61].”
Background
Investigation on the pharmacological profile of 2,6-diacetylpyridine bis(benzoylhydrazone) derivatives and their antimony(III) and bismuth(III) complexes
Ferraz, K. S. O., Silva, N. F., Silva, J. G. D., de Miranda, L. F., Romeiro, C. F. D., de Souza-Fagundes, E. M., Mendes, I. C., & Beraldo, H. D. O. (2012) · European Journal of Medicinal Chemistry · doi:10.1016/j.ejmech.2012.03.040 · Cited by 68
Targeted alpha therapy with bismuth‐213 and actinium‐225: Meeting future demand
Bruchertseifer, F., Kellerbauer, A., Malmbeck, R., & Morgenstern, A. (2019) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.3792 · Cited by 68
Improved safety and efficacy of 213Bi-DOTATATE-targeted alpha therapy of somatostatin receptor-expressing neuroendocrine tumors in mice pre-treated with l-lysine
Chan, H. S., Konijnenberg, M., Daniels, T., Nysus, M. V., Makvandi, M., de Blois, E., Breeman, W. A. P., Atcher, R. W., de Jong, M., & Norenberg, J. P. (2016) · EJNMMI Research · doi:10.1186/s13550-016-0240-5 · Cited by 67 · cited 5×
“The co-infusion of lysine or the plasma expander Gelofusine® with 213Bi-bioconjugates during TAT has been reported to have a threefold reduction in the kidney uptake and retention [66,132].”
BackgroundInfluential
Single-Dose Anti-CD138 Radioimmunotherapy: Bismuth-213 is More Efficient than Lutetium-177 for Treatment of Multiple Myeloma in a Preclinical Model
Fichou, N., Gouard, S., Maurel, C., Barbet, J., Ferrer, L., Morgenstern, A., Bruchertseifer, F., Faivre-Chauvet, A., Bigot‐Corbel, E., Davodeau, F., et al. (2015) · Frontiers in Medicine · doi:10.3389/fmed.2015.00076 · Cited by 64 · cited 2×
“37 days in the control group); however, the authors reported that no mice were cured with this treatment [87].”
Background
Therapeutic Applications of Pretargeting
Verhoeven, M., Seimbille, Y., & Dalm, S. U. (2019) · Pharmaceutics · doi:10.3390/pharmaceutics11090434 · Cited by 64 · cited 1×
“Pretargeted radiotherapy is another approach for combining a vector with long plasma half-life with a radionuclide with a short half-life, such as 213Bi [99].”
Background
Therapeutic Efficacy of 213Bi-labeled sdAbs in a Preclinical Model of Ovarian Cancer
Dekempeneer, Y., Caveliers, V., Ooms, M., Maertens, D., Gysemans, M., Lahoutte, T., Xavier, C., Lecocq, Q., Maes, K., Covens, P., et al. (2020) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.0c00580 · Cited by 62 · cited 18×
“Additionally, the high temperatures are unsuitable for heat-sensitive proteins of interest for TRNT, as this may cause the proteins to denature.”
BackgroundInfluential
Synthesis, crystal structures, in vitro biological evaluation of zinc(II) and bismuth(III) complexes of 2-acetylpyrazine N(4)-phenylthiosemicarbazone
Li, M., Zhang, L., Yang, M., Niu, J., & Zhou, J. (2012) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2012.02.024 · Cited by 61
Production of Ac-225 for cancer therapy by photon-induced transmutation of Ra-226
Melville, G., Meriarty, H., Metcalfe, P. E., Knittel, T., & Allen, B. (2007) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2007.03.018 · Cited by 60 · cited 1×
“226Ra(γ,n)225Ra is another reaction path for 225Ac production that has been determined experimentally [27,28].”
Background
Anti-CD45 pretargeted radioimmunotherapy using bismuth-213: high rates of complete remission and long-term survival in a mouse myeloid leukemia xenograft model
Pagel, J. M., Kenoyer, A. L., Bäck, T. A., Hamlin, D. K., Wilbur, D. S., Fisher, D. R., Park, S. I., Frayo, S. L., Axtman, A., Orgun, N. N., et al. (2011) · Blood · doi:10.1182/blood-2011-04-347039 · Cited by 59 · cited 1×
“213Bi-DOTA-biotin 80% and 20% of mice treated with antiCD45 Ab-SA conjugate followed by Myeloid leukaemia [109] Preprints (www.”
Background
Treatment of Peritoneal Carcinomatosis by Targeted Delivery of the Radio-Labeled Tumor Homing Peptide 213Bi-DTPA-[F3]2 into the Nucleus of Tumor Cells
Drecoll, E., Gaertner, F. C., Miederer, M., Blechert, B., Vallon, M., Müller, J. M., Alke, A., Seidl, C., Bruchertseifer, F., Morgenstern, A., et al. (2009) · PLoS ONE · doi:10.1371/journal.pone.0005715 · Cited by 58
Investigating the Complexation of the Pb2+/Bi3+ Pair with Dipicolinate Cyclen Ligands
Lima, L. M. P., Beyler, M., Delgado, R., Platas‐Iglesias, C., & Tripier, R. (2015) · Inorganic Chemistry · doi:10.1021/acs.inorgchem.5b01079 · Cited by 57 · cited 1×
“Me-DO2PA (Figure 4D), a [12] aneN4 bearing two picolinic acid arms and two methyl-capped amines, has also been reported to be stable in vivo when radiolabeled with 213Bi [60,61].”
Background
Breakthrough of 225Ac and its radionuclide daughters from an 225Ac/213Bi generator: development of new methods, quantitative characterization, and implications for clinical use
Ma, D., McDevitt, M. R., Finn, R. D., & Scheinberg, D. A. (2001) · Applied Radiation and Isotopes · doi:10.1016/s0969-8043(01)00062-8 · Cited by 56
The affinity of bismuth(III) for nitrogen-donor ligands
Hancock, R. D., Cukrowski, I., Baloyi, J., & Mashishi, J. (1993) · Journal of the Chemical Society Dalton Transactions · doi:10.1039/dt9930002895 · Cited by 56
In Vivo Evaluation of Bismuth-Labeled Monoclonal Antibody Comparing DTPA-Derived Bifunctional Chelates
Milenic, D. E., Roselli, M., Mirzadeh, S., Pippin, C. G., Gansow, O. A., Colcher, D. M., Brechbiel, M. W., & Schlom, J. (2001) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/108497801300189227 · Cited by 56 · cited 1×
“2 %ID/g for BF-1B4M-DTPA respectively [63].”
Efficient Bifunctional Decadentate Ligand 3p-C-DEPA for Targeted α-Radioimmunotherapy Applications
Song, H. A., Kang, C. S., Baidoo, K. E., Milenic, D. E., Chen, Y., Dai, A., Brechbiel, M. W., & Chong, H. (2011) · Bioconjugate Chemistry · doi:10.1021/bc100586y · Cited by 56 · cited 1×
“, rapid complexation (favorable formation kinetics) at ambient temperatures with radionuclides and high thermodynamic stability [62,63].”
Background
Preclinical evaluation of NETA-based bifunctional ligand for radioimmunotherapy applications using 212Bi and 213Bi: Radiolabeling, serum stability, and biodistribution and tumor uptake studies
Kang, C. S., Song, H. A., Milenic, D. E., Baidoo, K. E., Brechbiel, M. W., & Chong, H. (2013) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2013.01.012 · Cited by 54 · cited 1×
“3p-C-NETA-trastuzumab showed faster labeling of 205/206Bi compared with DOTA-trastuzumab, and an in vivo experiment on mice bearing subcutaneous tumors (LS-174T, which expresses HER-2, the target of trastuzumab) demonstrated significant tumor accumulation without increasing kidney uptake (after 24 h) [65].”
Background
In Vitro comparison of 213Bi- and 177Lu-radiation for peptide receptor radionuclide therapy
Chan, H. S., de Blois, E., Morgenstern, A., Bruchertseifer, F., de Jong, M., Breeman, W. A. P., & Konijnenberg, M. (2017) · PLoS ONE · doi:10.1371/journal.pone.0181473 · Cited by 54 · cited 1×
“2 DOTA and DOTA-derivatives The current “gold standard” BF chelator for 213Bi is the amino carboxylate macrocycle DOTA and 213Bi-DOTA bioconjugates have been reported to be stable in vitro and in vivo for at least two hours [65,66].”
Background
Improved efficacy of α‐particle–targeted radiation therapy
Milenic, D. E., Brady, E. D., Garmestani, K., Albert, P. S., Abdulla, A., & Brechbiel, M. W. (2010) · Cancer · doi:10.1002/cncr.24793 · Cited by 52 · cited 6×
“Several targets are currently being investigated for TAT with 213Bi-labeled probes, such as human epidermal growth factor receptor 2 (HER2) [69], cluster of differentiation 20 (CD20) [70], CD33 [71,72], CD45 [73], substance P [74–76], somatostatin receptors [19], prostate-specific membrane antigen (PSMA) [77], and epi…”
Influential
α- Versus β-Emitting Radionuclides for Pretargeted Radioimmunotherapy of Carcinoembryonic Antigen–Expressing Human Colon Cancer Xenografts
Heskamp, S., Hernandez, R., Molkenboer‐Kuenen, J. D. M., Essler, M., Bruchertseifer, F., Morgenstern, A., Steenbergen, E. J., Cai, W., Seidl, C., McBride, W. J., et al. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.116.187021 · Cited by 51
α-Radioimmunotherapy with 213Bi-anti-CD38 immunoconjugates is effective in a mouse model of human multiple myeloma
Teiluf, K., Seidl, C., Blechert, B., Gaertner, F. C., Gilbertz, K.-P., Fernández‐Sáiz, V., Bassermann, F. C., Endell, J., Boxhammer, R., Leclair, S., et al. (2014) · Oncotarget · doi:10.18632/oncotarget.2986 · Cited by 50
Targeting Aberrant DNA Double-Strand Break Repair in Triple-Negative Breast Cancer with Alpha-Particle Emitter Radiolabeled Anti-EGFR Antibody
Hong, S., Hedayati, M. A., Hobbs, R. F., Shao, C., Bruchertseifer, F., Morgenstern, A., DeWeese, T. L., & Sgouros, G. (2013) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-13-0108 · Cited by 50
Efficient synthesis and evaluation of bimodal ligand NETA
Chong, H., Song, H. A., Birch, N. W., Le, T., Lim, S., & Ma, X. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.03.084 · Cited by 49 · cited 2×
“55%ID/g), even though having a seemingly non-coordinatively saturated Bi3+ metal center [62,64].”
Background
Novel Bimodal Bifunctional Ligands for Radioimmunotherapy and Targeted MRI
Chong, H., Song, H. A., Ma, X., Milenic, D. E., Brady, E. D., Lim, S., Lee, H., Baidoo, K. E., Cheng, D., & Brechbiel, M. W. (2008) · Bioconjugate Chemistry · doi:10.1021/bc800050x · Cited by 46 · cited 1×
“55%ID/g), even though having a seemingly non-coordinatively saturated Bi3+ metal center [62,64].”
Background
111In-DTPA0-octreotide (Octreoscan), 131I-MIBG and other agents for radionuclide therapy of NETs
Bomanji, J. B., & Papathanasiou, N. D. (2012) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-011-2013-8 · Cited by 44
Efficient formation of inert Bi-213 chelates by tetraphosphorus acid analogues of DOTA: towards improved alpha-therapeutics
Šimeček, J., Hermann, P., Seidl, C., Bruchertseifer, F., Morgenstern, A., Wester, H., & Notni, J. (2018) · EJNMMI Research · doi:10.1186/s13550-018-0431-3 · Cited by 43 · cited 1×
“In contrast, for CHX-A’’-DTPA, a concentration of 1 μM is in general sufficient to achieve quantitative yields [68].”
Background
In vitro and in vivo evaluation of novel ligands for radioimmunotherapy
Chong, H., Milenic, D. E., Garmestani, K., Brady, E. D., Arora, H., Pfiester, C. M., & Brechbiel, M. W. (2006) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2006.03.004 · Cited by 42
Radionuclide-Based Cancer Imaging Targeting the Carcinoembryonic Antigen
Hong, H., Sun, J., & Cai, W. (2008) · Biomarker Insights · doi:10.4137/bmi.s1124 · Cited by 41 · cited 1×
“, 2008 and modified with permission from [79], SAGE Journals, 2008.”
Background
p-NO2–Bn–H4neunpa and H4neunpa–Trastuzumab: Bifunctional Chelator for Radiometalpharmaceuticals and 111In Immuno-Single Photon Emission Computed Tomography Imaging
Spreckelmeyer, S., Ramogida, C. F., Rousseau, J., Arane, K., Bratanovic, I., Colpo, N., Jermilova, U., Dias, G., Dude, I., Jaraquemada-Peláez, M. D. G., et al. (2017) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.7b00311 · Cited by 41 · cited 1×
“8) was lower than that of DOTA and DTPA; however, the pM value is the similar to that of DOTA (pM = 27), providing potential for in vivo use [68].”
Background
Intra-arterial versus standard intravenous administration of lutetium-177-DOTA-octreotate in patients with NET liver metastases: study protocol for a multicenter, randomized controlled trial (LUTIA trial)
Ebbers, S. C., Braat, A. J. A. T., Moelker, A. D., Stokkel, M. P. M., Lam, M. G. E. H., & Barentsz, M. W. (2020) · Trials · doi:10.1186/s13063-019-3888-0 · Cited by 41
Combining α-Radioimmunotherapy and Adoptive T Cell Therapy to Potentiate Tumor Destruction
Ménager, J., Gorin, J., Maurel, C., Drujont, L., Gouard, S., Louvet, C., Chérel, M., Faivre-Chauvet, A., Morgenstern, A., Bruchertseifer, F., et al. (2015) · PLoS ONE · doi:10.1371/journal.pone.0130249 · Cited by 40 · cited 1×
“213Bi-DTPA-anti-CD138mAb The combined treatment resulted in significant tumor growth suppression and improved survival in the animals MM [105]”
Background
Cross sections from proton irradiation of thorium at 800 MeV
Engle, J. W., Mashnik, S. G., Weidner, J. W., Wolfsberg, L. E., Fassbender, M. E., Jackman, K. R., Couture, A. J., Bitteker, L. J., Ullmann, J. L., Gulley, M. S., et al. (2013) · Physical Review C · doi:10.1103/physrevc.88.014604 · Cited by 38 · cited 1×
“77y) at the end of bombardment which might be a serious limitation in terms of hospital translation and waste management [29,30].”
Background
Evaluating the Combination of Radioimmunotherapy and Immunotherapy in a Melanoma Mouse Model
Jiao, R., Allen, K. J. H., Malo, M. E., Rickles, D. J., & Dadachova, E. (2020) · International Journal of Molecular Sciences · doi:10.3390/ijms21030773 · Cited by 38
Immunoliposomal Delivery of 213Bi for α-Emitter Targeting of Metastatic Breast Cancer
Lingappa, M., Hong, S., Thompson, S., Bruchertseifer, F., Morgenstern, A., & Sgouros, G. (2010) · Cancer Research · doi:10.1158/0008-5472.can-09-4548 · Cited by 37
Preferential Cleavage of a Tripeptide Linkage by Enzymes on Renal Brush Border Membrane To Reduce Renal Radioactivity Levels of Radiolabeled Antibody Fragments
Suzuki, C., Uehara, T., Kanazawa, N., Wada, S., Suzuki, H. Y., & Arano, Y. (2018) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.8b00198 · Cited by 36 · cited 1×
“These findings would allow to develop radiometal-based radiopharmaceuticals with clinically relevant lower renal radioactivity levels [134].”
Background
Targeted alpha therapy for chronic lymphocytic leukaemia and non-Hodgkin’s lymphoma with the anti-CD37 radioimmunoconjugate 212Pb-NNV003
Maaland, A. F., Saidi, A., Torgue, J. J.-C., Heyerdahl, H., Stallons, T. A. R., Kolstad, A., & Dahle, J. (2020) · PLoS ONE · doi:10.1371/journal.pone.0230526 · Cited by 36
Targeted alpha-therapy using [Bi-213]anti-CD20 as novel treatment option for radio- and chemoresistant non-Hodgkin lymphoma cells
Roscher, M., Hormann, I., Leib, O., Marx, S., Moreno, J., Miltner, E., & Friesen, C. (2013) · Oncotarget · doi:10.18632/oncotarget.817 · Cited by 34 · cited 1×
“Nonetheless, preclinical studies have shown activity against other cancer types, including non-Hodgkin’s lymphoma and multiple myeloma [92,106].”
Background
A novel selection strategy for antibody producing hybridoma cells based on a new transgenic fusion cell line
Listek, M., Hönow, A., Gossen, M., & Hanack, K. (2020) · Scientific Reports · doi:10.1038/s41598-020-58571-w · Cited by 34 · cited 1×
“1 Antibodies Monoclonal antibodies (mAbs), with their impeccable affinity for tumor antigens, have become powerful tools in the diagnosis and treatment of cancer, particularly when combined with therapeutic agents such as radionuclides and cytotoxic drugs, thanks to advances in hybridoma technology in the 1980s [90,91…”
Background
DTPA complexation of bismuth in human blood serum
Montavon, G., Du, A. L., Champion, J., Rabung, T., & Morgenstern, A. (2012) · Dalton Transactions · doi:10.1039/c2dt30230f · Cited by 33
Production of Alpha Emitters for Targeted Alpha Therapy
Morgenstern, A., Abbas, K., Bruchertseifer, F., & Apostolidis, C. (2008) · Current Radiopharmaceuticals · doi:10.2174/1874471010801030135 · Cited by 33 · cited 2×
“The advantage of this method is the widespread availability of appropriate cyclotrons worldwide, especially in Europe [22,23], and high amounts of clinical doses of 225Ac could be produced in a reliable way.”
Background
Targeted alpha and beta radiotherapy: An overview of radiopharmaceutical and clinical aspects
Lacœuille, F., Arlicot, N., & Faivre-Chauvet, A. (2018) · Médecine Nucléaire · doi:10.1016/j.mednuc.2017.12.002 · Cited by 33 · cited 1×
“The high LET of α-particles results in a high rate of double-strand and cluster DNA breaks and consequently irreparable damage, producing the high kill rate of α-emitting radioisotopes both in normoxic as well as in a hypoxic tumor cell environment, which is known to be more resistant to photon and electron-based irra…”
Background
Therapeutic Efficacy of Alpha-RIT Using a 213Bi-Anti-hCD138 Antibody in a Mouse Model of Ovarian Peritoneal Carcinomatosis
Derrien, A., Gouard, S., Maurel, C., Gaugler, M., Bruchertseifer, F., Morgenstern, A., Faivre-Chauvet, A., Classe, J., & Chérel, M. (2015) · Frontiers in Medicine · doi:10.3389/fmed.2015.00088 · Cited by 32
H2Me-do2pa: an attractive chelator with fast, stable and inert nat Bi 3+ and 213 Bi 3+ complexation for potential α-radioimmunotherapy applications
Lima, L. M. P., Beyler, M., Oukhatar, F., Saëc, P. L., Faivre-Chauvet, A., Platas‐Iglesias, C., Delgado, R., & Tripier, R. (2014) · Chemical Communications · doi:10.1039/c4cc05529b · Cited by 31 · cited 1×
“5D), a [12]aneN4 bearing two picolinic acid arms and two methylcapped amines has also been reported to be stable in vivo when radiolabeled with 213Bi [69,70].”
Background
Radioimmunotherapy with Bismuth-213 as Conditioning for Nonmyeloablative Allogeneic Hematopoietic Cell Transplantation in Dogs: A Dose Deescalation Study
Bethge, W. A., Wilbur, D. S., Storb, R. F., Hamlin, D. K., Santos, E. B., Brechbiel, M. W., & Sandmaier, B. M. (2004) · Transplantation · doi:10.1097/01.tp.0000128853.62545.b2 · Cited by 31 · cited 2×
“Several targets are currently being investigated for TAT with 213Bi-labeled probes, such as human epidermal growth factor receptor 2 (HER2) [69], cluster of differentiation 20 (CD20) [70], CD33 [71,72], CD45 [73], substance P [74–76], somatostatin receptors [19], prostate-specific membrane antigen (PSMA) [77], and epi…”
Background
Synthesis and evaluation of a macrocyclic bifunctional chelating agent for use with bismuth radionuclides
Garmestani, K., Yao, Z., Zhang, M., Wong, K. J., Park, C., Pastan, I. H., Carrasquillo, J. A., & Brechbiel, M. W. (2001) · Nuclear Medicine and Biology · doi:10.1016/s0969-8051(00)00203-1 · Cited by 30 · cited 2×
“Several papers have reported that naked 213Bi and 213Bi dissociated from its chelating ligands tend to accumulate in the kidney [5,57,58].”
Background
Structure-function analysis and therapeutic efficacy of antibodies to fungal melanin for melanoma radioimmunotherapy
Nosanchuk, J. D., Jeyakumar, A., Ray, A., Revskaya, E., Jiang, Z., Bryan, R. A., Allen, K. J. H., Jiao, R., Malo, M. E., Gómez, B. L., et al. (2018) · Scientific Reports · doi:10.1038/s41598-018-23889-z · Cited by 30
Synthesis and biological evaluation of a novel decadentate ligand DEPA
Chong, H., Lim, S., Baidoo, K. E., Milenic, D. E., Ma, X., Jia, F., Song, H. A., Brechbiel, M. W., & Lewis, M. R. (2008) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2008.09.063 · Cited by 28 · cited 1×
“The 205/206Bi-DEPA complex has also been studied to show similarly promising results with DTPA as benchmark [66,67].”
Result
Pharmacokinetics and toxicity of 213Bi-labeled PAI2 in preclinical targeted alpha therapy for cancer
Song, E. Y., Rizvi, S. M., Qu, C. F., Raja, C., Brechbiel, M. W., Morgenstern, A., Apostolidis, C., & Allen, B. (2007) · Cancer Biology & Therapy · doi:10.4161/cbt.6.6.4097 · Cited by 28 · cited 1×
“The co-infusion of lysine or the plasma expander Gelofusine® with 213Bi-bioconjugates during TAT has been reported to have a threefold reduction in the kidney uptake and retention [66,132].”
Background
Evaluation of Met-Val-Lys as a Renal Brush Border Enzyme-Cleavable Linker to Reduce Kidney Uptake of 68Ga-Labeled DOTA-Conjugated Peptides and Peptidomimetics
Bendre, S., Zhang, Z., Kuo, H., Rousseau, J., Zhang, C., Merkens, H., Roxin, Á., Bénard, F., & Lin, K. (2020) · Molecules · doi:10.3390/molecules25173854 · Cited by 28 · cited 1×
“A study has demonstrated that derivatives of [68Ga]Ga-DOTA-AmBz-MVK-OH could be cleaved specifically by neutral endopeptidase (NEP), and therefore, the amino acids linker MVK could reduce kidney uptake of radiolabeled DOTA-conjugated peptides and peptidomimetics [133].”
Background
Phase I trial of α-particle therapy with actinium-225 (225Ac)-lintuzumab (anti-CD33) and low-dose cytarabine (LDAC) in older patients with untreated acute myeloid leukemia (AML.
Jurcic, J. G., Ravandi, F., Pagel, J. M., Park, J. H., Smith, B. D., Douer, D., Levy, M. Y., Estey, E. H., Kantarjian, H. M., Earle, D. C., et al. (2015) · Journal of Clinical Oncology · doi:10.1200/jco.2015.33.15_suppl.7050 · Cited by 27
Targeted Alpha-Particle Therapy for Hematologic Malignancies
Jurcic, J. G. (2019) · Journal of medical imaging and radiation sciences · doi:10.1016/j.jmir.2019.05.008 · Cited by 27
Fractionated intravesical radioimmunotherapy with213Bi-anti-EGFR-MAb is effective without toxic side-effects in a nude mouse model of advanced human bladder carcinoma
Fazel, J., Rötzer, S., Seidl, C., Feuerecker, B., Autenrieth, M. E., Weirich, G., Bruchertseifer, F., Morgenstern, A., & Senekowitsch–Schmidtke, R. (2015) · Cancer Biology & Therapy · doi:10.1080/15384047.2015.1071735 · Cited by 26
Different ways to improve the clinical effectiveness of radioimmunotherapy in solid tumors
Chatal, J., Davodeau, F., Chérel, M., & Barbet, J. (2009) · Journal of Cancer Research and Therapeutics · doi:10.4103/0973-1482.55139 · Cited by 25 · cited 1×
“Several strategies have been explored to mitigate the toxic aspect of 213Bi-labeled radioprobes during cancer treatment [5,66,130,131] and some of these approaches have been approved for clinical applications.”
Background
Long-Term Toxicity of 213Bi-Labelled BSA in Mice
Dorso, L., Bigot‐Corbel, E., Abadie, J., Diab, M., Gouard, S., Bruchertseifer, F., Morgenstern, A., Maurel, C., Chérel, M., & Davodeau, F. (2016) · PLoS ONE · doi:10.1371/journal.pone.0151330 · Cited by 22 · cited 1×
“Several papers have reported that naked 213Bi, dissociated from its chelating ligands, tends to accumulate in the kidney [5,49,50].”
Background
Therapeutic efficacy of α-radioimmunotherapy with different activity levels of the 213Bi-labeled monoclonal antibody MX35 in an ovarian cancer model
Gustafsson-Lutz, A., Bäck, T. A., Aneheim, E., Hultborn, R., Palm, S., Jacobsson, L., Morgenstern, A., Bruchertseifer, F., Albertsson, P., & Lindegren, S. (2017) · EJNMMI Research · doi:10.1186/s13550-017-0283-2 · Cited by 22
Synthesis and evaluation of a bifunctional chelate for development of Bi(III)-labeled radioimmunoconjugates
Dadwal, M., Kang, C. S., Song, H. A., Sun, X. Y., Dai, A., Baidoo, K. E., Brechbiel, M. W., & Chong, H. (2011) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2011.06.107 · Cited by 21 · cited 2×
“However, in the case of 205/206Bi-DTPA-trastuzumab, only 77% was intact after 72 h [66].”
BackgroundResult
Measurement of the Beam Energy Distribution of a Medical Cyclotron with a Multi-Leaf Faraday Cup
Nesteruk, K. P., Ramseyer, L., Carzaniga, T. S., & Braccini, S. (2019) · Instruments · doi:10.3390/instruments3010004 · Cited by 18
Targeted Alpha Therapy Approach to the Management of Pancreatic Cancer
Allen, B., Rizvi, S. M., Qu, C. F., & Smith, R. C. (2011) · Cancers · doi:10.3390/cancers3021821 · Cited by 16
213Bi production and complexation with new picolinate containing ligands
Sinenko, I. L., Калмыкова, Т. П., Likhosherstova, D. V., Egorova, B. V., Zubenko, A. D., Vasiliev, A. N., Ermolaev, S. V., Lapshina, E. V., Ostapenko, V. S., Fedorova, O. A., et al. (2019) · Journal of Radioanalytical and Nuclear Chemistry · doi:10.1007/s10967-019-06610-w · Cited by 16
A Radiolabeled Fully Human Antibody to Human Aspartyl (Asparaginyl) β -Hydroxylase Is a Promising Agent for Imaging and Therapy of Metastatic Breast Cancer
Revskaya, E., Jiang, Z., Morgenstern, A., Bruchertseifer, F., Sesay, M. A., Walker, S., Fuller, S. A., Lebowitz, M., Gravekamp, C., Ghanbari, H. A., et al. (2017) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/cbr.2016.2141 · Cited by 13
Evaluation of novel highly specific antibodies to cancer testis antigen Centrin‐1 for radioimmunoimaging and radioimmunotherapy of pancreatic cancer
Jiao, R., Allen, K. J. H., Malo, M. E., Helal, M. H. S., Jiang, Z., Smart, K., Buhl, S., Rickles, D. J., Bryan, R. A., & Dadachova, E. (2019) · Cancer Medicine · doi:10.1002/cam4.2379 · Cited by 11 · cited 1×
“The decay of 213Bi is followed by the emission of a 435 keV-photon (98% abundance) that could potentially be used for SPECT with a gamma camera equipped with high energy collimators, permitting detailed evaluation of the biodistribution of 213Bi in vivo [15].”
Method
High-Purity Actinium-225 Production from Radium-226 using a Superconducting Electron Linac
Grimm, T., Grimm, A. K., Peters, W. A., & Zamiara, M. (2019) · Journal of medical imaging and radiation sciences · doi:10.1016/j.jmir.2019.03.040 · Cited by 9
The hydrothermal chemistry of Bismuth and the liquid Bismuth collector model.
Tooth, B. (2013) · Adelaide Research & Scholarship (AR&S) (University of Adelaide) · Cited by 9
Could Autoimmune Disease Contribute to the Abscopal Effect in Metastatic Hepatocellular Carcinoma?
Beyls, C., Haustermans, K. M., Deroose, C. M., Pans, S., Vanbeckevoort, D., Verslype, C., & Dekervel, J. (2020) · Hepatology · doi:10.1002/hep.31186 · Cited by 9 · cited 1×
“Though the exact biological mechanisms accountable for the abscopal effect are yet to be identified, the immune system is considered the major player in this significant role [1,8].”
Background
Assessment of 213Bi-anti-EGFR MAb treatment efficacy in malignant cancer cells with [1-13C]pyruvate and [18F]FDG
Feuerecker, B., Michalik, M., Hundshammer, C., Schwaiger, M., Bruchertseifer, F., Morgenstern, A., & Seidl, C. (2019) · Scientific Reports · doi:10.1038/s41598-019-44484-w · Cited by 8
Thorium-229 quantified in historical Thorium-228 capsules
Boden, S., Koen, V., Cagno, S., Maertens, D., Hecke, K. V., & Cardinaels, T. (2016) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2016.11.012 · Cited by 7 · cited 1×
“Additionally, at the Belgian Nuclear Research Centre (SCK CEN) in Mol, Belgium, very pure sources of 229Th were identified, processed, and used for pre-clinical studies [20].”
Background
Proton-induced cross sections relevant to production of 225Ac and 223Ra in natural thorium targets below 200 MeVPreprint
Weidner, J. W., Mashnik, S. G., John, K. D., et al. (2012) · arXiv (Cornell University) · doi:10.48550/arxiv.1205.3523 · Cited by 4 · cited 1×
“77y) at the end of bombardment, which might be a serious limitation in terms of clinical translation and waste management [25,26].”
Background
A pulse radiolysis study of the chloride complexes of Bi(II) and Bi(IV)
Ершов, Б. Г., Akinshin, M. A., Гордеев, А. В., & Sukhov, N. L. (1986) · International Journal of Radiation Applications and Instrumentation Part C Radiation Physics and Chemistry · doi:10.1016/1359-0197(86)90139-6 · Cited by 4 · cited 1×
“However, rare occurrences of Bi(II) and Bi(IV) have been reported [38].”
Background
The electronic theory of valency.
Sv, A. (1946) · PubMed · Cited by 3
Alpha-Particle Therapy for Acute Myeloid Leukemia
Jurcic, J. G. (2019) · Journal of medical imaging and radiation sciences · doi:10.1016/j.jmir.2019.03.058 · Cited by 3
Radium Targets for the Reactor Production of Alpha-emitting Medical Radioisotopes
Copping, R., Mirzadeh, S., Stracener, D. W., Denton, D., Murphy, K., Wright, J., Hickman, E., & Marcus, C. (2019) · Journal of medical imaging and radiation sciences · doi:10.1016/j.jmir.2019.03.049 · Cited by 3
Alpha-Particle Therapy for Acute Myeloid Leukemia
Jurcic, J. G. (2019) · Journal of medical imaging and radiation sciences · doi:10.1016/j.jmir.2019.11.063 · Cited by 3
?-Radioimmunotherapy with ²¹³Bi-anti-CD38 immunoconjugates is effective in a mouse model of human multiple myeloma.
Teiluf, K. (2015) · mediaTUM (Technical University of Munich) · Cited by 2

Flagged first, then by citations

7 of the 141 references couldn’t be matched to a known paper.

Research works printed but not linked: 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

Sorted by citations

Radiopharmaceutical Treatments for Cancer Therapy, Radionuclides Characteristics, Applications, and Challenges
Salih, S., Alkatheeri, A., Alomaim, W., & Elliyanti, A. (2022) · Molecules · doi:10.3390/molecules27165231 · Cited by 101
Dosimetry in Radiopharmaceutical Therapy
O’Donoghue, J. A., ZANZONICO, P. B., Humm, J. L., & Kesner, A. (2022) · Journal of Nuclear Medicine · doi:10.2967/jnumed.121.262305 · Cited by 100
“Alpha-particle–emitting radionuclides that have been used in clinical trials include (213)Bi (84,85), (211)At (86,87), (212)Pb (88), (223)Ra (89), (225)Ac (90,91), and (227)Th (92), listed in Table 1.”
Recent Advances in 64Cu/67Cu-Based Radiopharmaceuticals
Krasnovskaya, O. O., Abramchuk, D., Erofeev, A. S., Gorelkin, P. V., Kuznetsov, A. A., Shemukhin, A. A., & Beloglazkina, E. K. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms24119154 · Cited by 85
Alpha-Emitting Radionuclides: Current Status and Future Perspectives
Miederer, M., Benešová, M., Mamat, C., Kästner, D., Pretze, M., Michler, E., Brogsitter, C., Kotzerke, J., Kopka, K., Scheinberg, D. A., et al. (2024) · Pharmaceuticals · doi:10.3390/ph17010076 · Cited by 78
“The DOTA chelator [25] has been widely used for the alpha-emitting radionuclides actinium-225, bismuth-213, and terbium-149, frequently for thorium-227, and some trials were made for radium-223 [12,26–28].”
Method
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 all 120

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
ORCID: Ahenkorah, Stephen
Cassells, Irwin
Deroose, Christophe M.
Cardinaels, Thomas
Burgoyne, Andrew R.
Bormans, Guy
Ooms, Maarten
Cleeren, Frederik
Venue: Pharmaceutics
Publisher: MDPI AG
Published: 2021-04-21
Volume: 13
Issue: 5
Pages: 599
ISSN: 1999-4923 (ISSN-L)
DOI: 10.3390/pharmaceutics13050599
PMC: PMC8143329
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: gold
doi.org
Licence: cc-by
creativecommons.org/licenses/by/4.0/ (vor)
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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Bismuth-213 for targeted radionuclide therapy: from atom to bedside.

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