Efforts to Control the Errant Products of a Targeted In vivo Generator
Abstract
Alpha-particle immunotherapy by targeted alpha-emitters or alpha-emitting isotope generators is a novel form of extraordinarily potent cancer therapy. A major impediment to the clinical use of targeted actinium-225 (225Ac) in vivo generators may be the radiotoxicity of the systemically released daughter radionuclides. The daughters, especially bismuth-213 (213Bi), tend to accumulate in the kidneys. We tested the efficacy of various pharmacologic agents and the effect of tumor burden in altering the pharmacokinetics of the 225Ac daughters to modify their renal uptake. Pharmacologic treatments in animals were started before i.v. administration of the HuM195-225Ac generator. 225Ac, francium-221 (221Fr), and 213Bi biodistributions were calculated in each animal at different time points after 225Ac generator injection. Oral metal chelation with 2,3-dimercapto-1-propanesulfonic acid (DMPS) or meso-2,3-dimercaptosuccinic acid (DMSA) caused a significant reduction (P < 0.0001) in the renal 213Bi uptake; however, DMPS was more effective than DMSA (P < 0.001). The results with DMPS were also confirmed in a monkey model. The renal 213Bi and 221Fr activities were significantly reduced by furosemide and chlorothiazide treatment (P < 0.0001). The effect on renal 213Bi activity was further enhanced by the combination of DMPS with either chlorothiazide or furosemide (P < 0.0001). Competitive antagonism by bismuth subnitrate moderately reduced the renal uptake of 213Bi. The presence of a higher target-tumor burden significantly prevented the renal 213Bi accumulation (P = 0.003), which was further reduced by DMPS treatment (P < 0.0001). Metal chelation, diuresis with furosemide or chlorothiazide, and competitive metal blockade may be used as adjuvant therapies to modify the renal accumulation of 225Ac daughters.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
Claims other papers make about this one
Each is checked against this paper’s own text: does it say what the citing paper says it does?
Renal toxicity induced by 213Bi in small animals is considered a critical constraint to clinical use of 225Ac.
“For example, the renal toxicity induced by 213Bi (in small animals) is considered a critical constraint to clinical use of 225Ac (114).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [114]
Cites
Immunotherapy: past, present and future
Waldmann, T. A. (2003) · Nature Medicine · doi:10.1038/nm0303-269 · Cited by 623 · see citing works
Tumor therapy with targeted atomic nanogenerators.
McDevitt, M. R., Ma, D., Lai, L. T., Simon, J., Borchardt, P., Frank, R. K., Wu, K., Pellegrini, V., Curcio, M. J., Miederer, M., et al. (2001) · Science · doi:10.1126/science.1064126 · Cited by 501 · see citing works
Self-citationTargeted α particle immunotherapy for myeloid leukemia
Jurcic, J. G., Larson, S. M., Sgouros, G., McDevitt, M. R., Finn, R. D., Divgi, C. R., Ballangrud, Å., Hamacher, K. A., Ma, D., Humm, J. L., et al. (2002) · Blood · doi:10.1182/blood.v100.4.1233.h81602001233_1233_1239 · Cited by 472 · see citing works
Self-citationAntibody-targeted radiation cancer therapy
Milenic, D. E., Brady, E. D., & Brechbiel, M. W. (2004) · Nature Reviews Drug Discovery · doi:10.1038/nrd1413 · Cited by 380 · see citing works
Pharmacokinetics and Toxicity of Bismuth Compounds
Slikkerveer, A., & Wolff, F. A. (1989) · Drug Safety · doi:10.1007/bf03259915 · Cited by 247 · see citing works
Design and synthesis of 225Ac radioimmunopharmaceuticals.
McDevitt, M. R., Ma, D., Simon, J., Frank, R. K., & Scheinberg, D. A. (2002) · Applied Radiation and Isotopes · doi:10.1016/s0969-8043(02)00167-7 · Cited by 225 · see citing works
Self-citationCohen, E. P., & Robbins, M. E. C. (2003) · Seminars in Nephrology · doi:10.1016/s0270-9295(03)00093-7 · Cited by 214 · see citing works
Astatine-211-Labeled Radiotherapeutics An Emerging Approach to Targeted Alpha-Particle Radiotherapy
Zalutsky, M. R., & Vaidyanathan, G. (2000) · Current Pharmaceutical Design · doi:10.2174/1381612003399275 · Cited by 203 · see citing works
Kozak, R. W., Atcher, R. W., Gansow, O. A., Friedman, A. M., Hines, J. J., Jr., & Waldmann, T. A. (1986) · Proceedings of the National Academy of Sciences · doi:10.1073/pnas.83.2.474 · Cited by 197 · see citing works
Nikula, T. K., McDevitt, M. R., Finn, R. D., Wu, C., Kozak, R. W., Garmestani, K., Brechbiel, M. W., Curcio, M. J., Pippin, C. G., Tiffany-Jones, L., et al. (1999) · PubMed · Cited by 176 · see citing works
Self-citationRadiobiology of α Particles: III. Cell Inactivation by α-Particle Traversals of the Cell Nucleus
Raju, M. R., Eisen, Y., Carpenter, S. G., & Inkret, W. C. T. (1991) · Radiation Research · doi:10.2307/3578139 · Cited by 167 · see citing works
The Chemical Fate of 212Bi-DOTA Formed by β- Decay of 212Pb(DOTA)2-***
Mirzadeh, S., Kumar, K., & Gansow, O. A. (1993) · Radiochimica Acta · doi:10.1524/ract.1993.60.1.1 · Cited by 155 · see citing works
Targeted actinium-225 in vivo generators for therapy of ovarian cancer.
Borchardt, P. E., Yuan, R., Miederer, M., McDevitt, M. R., & Scheinberg, D. A. (2003) · PubMed · Cited by 150 · see citing works
Self-citationHassfjell, S. P., & Brechbiel, M. W. (2001) · Chemical Reviews · doi:10.1021/cr000118y · Cited by 133 · see citing works
Molecular advances in pretargeting radioimunotherapy with bispecific antibodies.
Chang, C., Sharkey, R. M., Rossi, E. A., Karacay, H., McBride, W., Hansen, H. J., Chatal, J., Barbet, J., & Goldenberg, D. M. (2002) · PubMed · Cited by 129 · see citing works
Comparison of 225actinium chelates: tissue distribution and radiotoxicity
Davis, I. A., Glowienka, K. A., Boll, R. A., Deal, K. A., Brechbiel, M. W., Stabin, M. G., Bochsler, P. N., Mirzadeh, S., & Kennel, S. J. (1999) · Nuclear Medicine and Biology · doi:10.1016/s0969-8051(99)00024-4 · Cited by 105 · see citing works
Mazumder, D. N. G., Ghoshal, U. C., Saha, J. K., Santra, A. K., De, B. K., Chatterjee, A., Dutta, S. K., Angle, C. R., & Centeno, J. A. (1998) · Journal of Toxicology Clinical Toxicology · doi:10.3109/15563659809162616 · Cited by 96 · see citing works
Mazumder, D. G., De, B. K., Santra, A. K., Ghosh, N., Das, S., Lahiri, S., & Das, T. (2001) · Journal of Toxicology Clinical Toxicology · doi:10.1081/clt-100108507 · Cited by 92 · see citing works
Ghetie, M., Picker, L. J., Richardson, J. A., Tucker, K., Uhr, J., & Vitetta, E. S. (1994) · Blood · doi:10.1182/blood.v83.5.1329.bloodjournal8351329 · Cited by 91 · see citing works
Scheinberg, D. A., Straus, D. J., Yeh, S.-D., Divgi, C. R., Garin‐Chesa, P., Graham, M. C., Pentlow, K. S., Coit, D. G., Oettgen, H. F., & Old, L. J. (1990) · Journal of Clinical Oncology · doi:10.1200/jco.1990.8.5.792 · Cited by 89 · see citing works
Self-citationDetermination and metabolism of dithiol chelating agents
Rivera, M., Zheng, W., Aposhian, H. V., & Fernaǹdo, Q. (1989) · Toxicology and Applied Pharmacology · doi:10.1016/0041-008x(89)90094-x · Cited by 86 · see citing works
Binding of bismuth to serum proteins: implication for targets of Bi(III) in blood plasma
Sun, H., & Szeto, K.-Y. (2003) · Journal of Inorganic Biochemistry · doi:10.1016/s0162-0134(02)00649-9 · Cited by 79 · see citing works
Are certain diuretics also anticonvulsants?
Hesdorffer, D. C., Stables, J. P., Hauser, W. A., Annegers, J. F., & Cascino, G. D. (2001) · Annals of Neurology · doi:10.1002/ana.1136 · Cited by 64 · see citing works
Bethge, W. A., Wilbur, D. S., Storb, R. F., Hamlin, D. K., Santos, E. B., Brechbiel, M. W., Fisher, D. R., & Sandmaier, B. M. (2003) · Blood · doi:10.1182/blood-2002-12-3867 · Cited by 63 · see citing works
Competitive Binding of Bismuth to Transferrin and Albumin in Aqueous Solution and in Blood Plasma
Sun, H., Li, H., Mason, A. B., Woodworth, R. C., & Sadler, P. J. (2001) · Journal of Biological Chemistry · doi:10.1074/jbc.m004779200 · Cited by 61 · see citing works
Yao, Z., Garmestani, K., Wong, K. J., Park, L. S., Dadachova, E., Yordanov, A. T., Waldmann, T. A., Eckelman, W. C., Paik, C. H., & Carrasquillo, J. A. (2001) · PubMed · Cited by 51 · see citing works
Aposhian, H. V., Mershon, M. M., Brinkley, F. B., Hsu, C.-A., & Hackley, B. E. (1982) · Life Sciences · doi:10.1016/0024-3205(82)90108-4 · Cited by 49 · see citing works
Metabolic Studies with Radiobismuth: I. Retention and Distribution of 206 Bi in the Normal Rat
Russ, G. A., Bigler, R. E., Tilbury, R. S., WOODARD, H. Q., & Laughlin, J. S. (1975) · Radiation Research · doi:10.2307/3574096 · Cited by 47 · see citing works
Modeling and dosimetry of monoclonal antibody M195 (anti-CD33) in acute myelogenous leukemia.
Sgouros, G., Graham, M. C., Divgi, C. R., Larson, S. M., & Scheinberg, D. A. (1993) · PubMed · Cited by 43 · see citing works
Self-citationPharmacological Classification and Renal Actions of Diuretics
Puschett, J. B. (2008) · Cardiology · doi:10.1159/000176450 · Cited by 42 · see citing works
Binding of bismuth in the kidneys of the rate: The role of metallothionein-like proteins
Szymańska, J. A., Mogilnicka, E. M., & Kaszper, B. W. (1977) · Biochemical Pharmacology · doi:10.1016/0006-2952(77)90314-8 · Cited by 41 · see citing works
Ac-225 and her daughters: the many faces of Shiva
McDevitt, M. R., & Scheinberg, D. A. (2002) · Cell Death and Differentiation · doi:10.1038/sj.cdd.4401047 · Cited by 36 · see citing works
Self-citationDiuretics in Cardiovascular Therapy: The New Clinicopharmacological Bases That Matter
Reyes, A. J., & Taylor, S. H. (1999) · Cardiovascular Drugs and Therapy · doi:10.1023/a:1007835821228 · Cited by 33 · see citing works
Determination and metabolism of dithiol chelating agents
Maiorino, R. M., & Aposhian, H. V. (1989) · Biochemical Pharmacology · doi:10.1016/0006-2952(89)90261-x · Cited by 32 · see citing works
Maiorino, R. M., Xu, Z., & Aposhian, H. V. (1996) · Journal of Pharmacology and Experimental Therapeutics · doi:10.1016/s0022-3565(25)12833-4 · Cited by 24 · see citing works
Antibody-based treatment of acute myeloid leukaemia
Mulford, D. A., & Jurcic, J. G. (2004) · Expert Opinion on Biological Therapy · doi:10.1517/14712598.4.1.95 · Cited by 21 · see citing works
Antidotes for Acute Bismuth Intoxication
Basinger, M. A., Jones, M. M., & McCroskey, S. A. (1983) · Journal of Toxicology Clinical Toxicology · doi:10.3109/15563658308990060 · Cited by 19 · see citing works
Development of a therapeutic procedure for bismuth intoxication with chelating agents.
Slikkerveer, A., Jong, H. B., Helmich, R. B., & de Wolff, F. A. (1992) · PubMed · Cited by 17 · see citing works
Slikkerveer, A., van der Voet, G. B., de Wolff, F. A., Noach, L. A., & Tytgat, G. N. J. (1998) · The Analyst · doi:10.1039/a704945e · Cited by 16 · see citing works
Jones, S. B., Tiffany, L. J., Garmestani, K., Gansow, O. A., & Kozak, R. W. (1996) · Nuclear Medicine and Biology · doi:10.1016/0969-8051(95)02006-3 · Cited by 14 · see citing works
Effectiveness of DTPA Treatments Following the Injection of Particulate Plutonium
Bruenger, F. W., Taylor, D. M., Taylor, G. N., & Lloyd, R. D. (1991) · International Journal of Radiation Biology · doi:10.1080/09553009114552611 · Cited by 14 · see citing works
Flagged first, then by citations
Cited by
Sorted by citations
Sgouros, G., Roeske, J. C., McDevitt, M. R., Palm, S., Allen, B. J., Fisher, D. R., Brill, A. B., Song, H., Howell, R. W., & Akabani, G. (2010) · Journal of Nuclear Medicine · doi:10.2967/jnumed.108.058651 · Cited by 552 · see citing works
Self-citationα-Emitters for Radiotherapy: From Basic Radiochemistry to Clinical Studies—Part 1
Poty, S., Francesconi, L. C., McDevitt, M. R., Morris, M. J., & Lewis, J. S. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.116.186338 · Cited by 262 · see citing works
Self-citationA Critical Review of Alpha Radionuclide Therapy—How to Deal with Recoiling Daughters?
de Kruijff, R. M., Wolterbeek, H. T., & Denkova, A. G. (2015) · Pharmaceuticals · doi:10.3390/ph8020321 · Cited by 254 · see citing works
Miederer, M., Scheinberg, D. A., & McDevitt, M. R. (2008) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2008.04.009 · Cited by 210 · see citing works
Self-citationDevelopment of <sup>225</sup>Ac Radiopharmaceuticals: TRIUMF Perspectives and Experiences
Robertson, A. K. H., Ramogida, C. F., Schaffer, P., & Radchenko, V. (2018) · Current Radiopharmaceuticals · doi:10.2174/1874471011666180416161908 · Cited by 202 · see citing works
Overview of the Most Promising Radionuclides for Targeted Alpha Therapy: The “Hopeful Eight”
Eychenne, R., Chérel, M., Haddad, F., Guérard, F., & Gestin, J. (2021) · Pharmaceutics · doi:10.3390/pharmaceutics13060906 · Cited by 201 · see citing works
Targeted alpha therapy: progress in radionuclide production, radiochemistry, and applications.
Nelson, B. J. B., Andersson, J. D., & Wuest, F. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics13010049 · Cited by 194 · see citing works
Aghevlian, S., Boyle, A. J., & Reilly, R. M. (2015) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2015.12.003 · Cited by 194 · see citing works
Alpha-Emitters and Targeted Alpha Therapy in Oncology: from Basic Science to Clinical Investigations
Makvandi, M., Dupis, E., Engle, J. W., Nortier, F. M., Fassbender, M. E., Simon, S., Birnbaum, E. R., Atcher, R. W., John, K. D., Rixe, O., et al. (2018) · Targeted Oncology · doi:10.1007/s11523-018-0550-9 · Cited by 169 · see citing works
Shen, G., Xu, C., Hu, R., Jain, M. R., Nair, S., Lin, W., Yang, C. S., Chan, J. Y., & Kong, A.-N. T. (2005) · Pharmaceutical Research · doi:10.1007/s11095-005-7546-8 · Cited by 159 · see citing works
Hong, S., Hobbs, R. F., Vajravelu, R. K., Huso, D. L., Esaias, C. E., Apostolidis, C., Morgenstern, A., & Sgouros, G. (2009) · Cancer Research · doi:10.1158/0008-5472.can-09-1828 · Cited by 158 · see citing works
Self-citationDevelopment of targeted alpha particle therapy for solid tumors.
Tafreshi, N. K., Doligalski, M. L., Tichacek, C. J., Pandya, D. N., Budzevich, M. M., El-Haddad, G., Khushalani, N. I., Moros, E. G., McLaughlin, M. L., Wadas, T. J., et al. (2019) · Molecules · doi:10.3390/molecules24234314 · Cited by 157 · see citing works
Miederer, M., Henriksen, G., Alke, A., Mossbrugger, I., Quintanilla-Martinez, L., Senekowitsch-Schmidtke, R., & Essler, M. (2008) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-07-4647 · Cited by 155 · see citing works
Targeted α-therapy–past, present, future?
Brechbiel, M. W. (2007) · Dalton Transactions · doi:10.1039/b704726f · Cited by 151 · see citing works
225Ac-PSMA-617 for Therapy of Prostate Cancer
Kratochwil, C., Haberkorn, U., & Giesel, F. L. (2020) · Seminars in Nuclear Medicine · doi:10.1053/j.semnuclmed.2020.02.004 · Cited by 139 · see citing works
Gold Coated Lanthanide Phosphate Nanoparticles for Targeted Alpha Generator Radiotherapy
McLaughlin, M. F., Woodward, J. D., Boll, R. A., Wall, J. S., Rondinone, A. J., Kennel, S. J., Mirzadeh, S., & Robertson, J. D. (2013) · PLoS ONE · doi:10.1371/journal.pone.0054531 · Cited by 123 · see citing works
Kozempel, J., Mokhodoeva, O. B., & Vlk, M. (2018) · Molecules · doi:10.3390/molecules23030581 · Cited by 121 · see citing works
Evaluation of an Anti-HER2 Nanobody Labeled with 225Ac for Targeted α-Particle Therapy of Cancer
Pruszyński, M., D’Huyvetter, M., Bruchertseifer, F., Morgenstern, A., & Lahoutte, T. (2018) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.7b00985 · Cited by 116 · see citing works
Radionuclide carriers for targeting of cancer
Sofou, S. (2008) · International Journal of Nanomedicine · doi:10.2147/ijn.s2736 · Cited by 106 · see citing works
Poty, S., Carter, L. M., Mandleywala, K., Membreno, R., Abdel-Atti, D., Ragupathi, A., Scholz, W. W., Zeglis, B. M., & Lewis, J. S. (2018) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-18-1650 · Cited by 105 · see citing works
Chen, P. L., Wang, J., Hope, K. J., Jin, L., Dick, J. E., Cameron, R., Brandwein, J. M., Minden, M. D., & Reilly, R. M. (2006) · PubMed · Cited by 105 · see citing works
Enhanced Retention of the α-Particle-Emitting Daughters of Actinium-225 by Liposome Carriers
Sofou, S., Kappel, B. J., Jaggi, J. S., McDevitt, M. R., Scheinberg, D. A., & Sgouros, G. (2007) · Bioconjugate Chemistry · doi:10.1021/bc070075t · Cited by 94 · see citing works
Self-citationThe in vivo fate of 225Ac daughter nuclides using polymersomes as a model carrier
de Kruijff, R. M., Raavé, R., Kip, A., Molkenboer‐Kuenen, J. D. M., Morgenstern, A., Bruchertseifer, F., Heskamp, S., & Denkova, A. G. (2019) · Scientific Reports · doi:10.1038/s41598-019-48298-8 · Cited by 93 · see citing works
Kratochwil, C., Apostolidis, L., Rathke, H. G., Apostolidis, C., Bicu, F., Bruchertseifer, F., Choyke, P. L., Haberkorn, U., Giesel, F. L., & Morgenstern, A. (2021) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-021-05474-1 · Cited by 91 · see citing works
Jaggi, J. S., Seshan, S. V., McDevitt, M. R., LaPerle, K., Sgouros, G., & Scheinberg, D. A. (2005) · Journal of the American Society of Nephrology · doi:10.1681/asn.2004110945 · Cited by 89 · see citing works
Self-citationWilliams, L. E., DeNardo, G. L., & Meredith, R. F. (2008) · Medical Physics · doi:10.1118/1.2938520 · Cited by 80 · see citing works
Mitigation of radiation nephropathy after internal α-particle irradiation of kidneys
Jaggi, J. S., Seshan, S. V., McDevitt, M. R., Sgouros, G., Hyjek, E. M., & Scheinberg, D. A. (2006) · International Journal of Radiation Oncology*Biology*Physics · doi:10.1016/j.ijrobp.2005.11.036 · Cited by 78 · see citing works
Self-citationPandya, D. N., Hantgan, R. R., Budzevich, M. M., Kock, N. D., Morse, D. L., Batista, I., Mintz, A., Li, K. C., & Wadas, T. J. (2016) · Theranostics · doi:10.7150/thno.14338 · Cited by 76 · see citing works
Essler, M., Gärtner, F. C., Neff, F., Blechert, B., Senekowitsch–Schmidtke, R., Bruchertseifer, F., Morgenstern, A., & Seidl, C. (2012) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-011-2023-6 · Cited by 75 · see citing works
Recent Research Trends on Bismuth Compounds in Cancer Chemoand Radiotherapy
Kowalik, M., Masternak, J., & Barszcz, B. (2017) · Current Medicinal Chemistry · doi:10.2174/0929867324666171003113540 · Cited by 73 · see citing works
Targeted Alpha-Particle Immunotherapy for Acute Myeloid Leukemia
Jurcic, J. G., & Rosenblat, T. L. (2014) · American Society of Clinical Oncology Educational Book · doi:10.14694/edbook_am.2014.34.e126 · Cited by 72 · see citing works
Peptide-targeted radionuclide therapy for melanoma
Miao, Y., & Quinn, T. P. (2008) · Critical Reviews in Oncology/Hematology · doi:10.1016/j.critrevonc.2008.02.006 · Cited by 69 · see citing works
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
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
A nephron-based model of the kidneys for macro-to-micro α-particle dosimetry
Hobbs, R. F., Song, H., Huso, D. L., H Sundel, M., & Sgouros, G. (2012) · Physics in Medicine and Biology · doi:10.1088/0031-9155/57/13/4403 · Cited by 61 · see citing works
Self-citationRetention studies of recoiling daughter nuclides of 225Ac in polymer vesicles
Wang, G., de Kruijff, R. M., Rol, M. A., Thijssen, L., Mendes, E., Morgenstern, A., Bruchertseifer, F., Stuart, M. C. A., Wolterbeek, H. T., & Denkova, A. G. (2013) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2013.12.008 · Cited by 61 · see citing works
Radiochemical aspects of alpha emitting radionuclides for medical application
Ferrier, M. G., Radchenko, V., & Wilbur, D. S. (2019) · Radiochimica Acta · doi:10.1515/ract-2019-0005 · Cited by 61 · see citing works
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 · see citing works
Robinson, M. K., Shaller, C. C., Garmestani, K., Plascjak, P. S., Hodge, K. M., Yuan, Q., Marks, J. D., Waldmann, T. A., Brechbiel, M. W., & Adams, G. P. (2008) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-07-1250 · Cited by 59 · see citing works
Functionalized TiO2 nanoparticles labelled with 225Ac for targeted alpha radionuclide therapy
Cędrowska, E., Pruszyński, M., Majkowska‐Pilip, A., Męczyńska‐Wielgosz, S., Bruchertseifer, F., Morgenstern, A., & Bilewicz, A. (2018) · Journal of Nanoparticle Research · doi:10.1007/s11051-018-4181-y · Cited by 58 · see citing works
Treatment of Prostate Cancer with CD46-targeted 225Ac Alpha Particle Radioimmunotherapy
Bidkar, A. P., Wang, S., Bobba, K. N., Chan, E., Bidlingmaier, S. M., Egusa, E. A., Peter, R., Ali, U., Meher, N., Wadhwa, A., et al. (2023) · Clinical Cancer Research · doi:10.1158/1078-0432.ccr-22-3291 · Cited by 56 · see citing works
Wilson, J. J., Ferrier, M. G., Radchenko, V., Maassen, J. R., Engle, J. W., Batista, E. R., Martin, R. L., Nortier, F. M., Fassbender, M. E., John, K. D., et al. (2014) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2014.12.007 · Cited by 51 · see citing works
Radionuclide Antibody-Conjugates, a Targeted Therapy Towards Cancer
Kitson, S. L., Cuccurullo, V., Moody, T. S., & Mansi, L. (2013) · Current Radiopharmaceuticals · doi:10.2174/1874471011306020001 · Cited by 50 · see citing works
Targeted Alpha-Particle Therapy for Hematologic Malignancies
Jurcic, J. G. (2019) · Seminars in Nuclear Medicine · doi:10.1053/j.semnuclmed.2019.09.002 · Cited by 50 · see citing works
Syed, V., Mak, P., Du, C., & Balaji, K. C. (2007) · Journal of Cellular Biochemistry · doi:10.1002/jcb.21603 · Cited by 49 · see citing works
Selective Alpha-Particle Mediated Depletion of Tumor Vasculature with Vascular Normalization
Jaggi, J. S., Henke, E., Seshan, S. V., Kappel, B. J., Chattopadhyay, D., May, C., McDevitt, M. R., Nolan, D., Mittal, V., Benezra, R., et al. (2007) · PLoS ONE · doi:10.1371/journal.pone.0000267 · Cited by 49 · see citing works
Self-citationNanoparticles in Targeted Alpha Therapy
Majkowska‐Pilip, A., Gawęda, W., Żelechowska-Matysiak, K., Wawrowicz, K., & Bilewicz, A. (2020) · Nanomaterials · doi:10.3390/nano10071366 · Cited by 48 · see citing works
LnPO 4 Nanoparticles Doped with Ac-225 and Sequestered Daughters for Targeted Alpha Therapy
McLaughlin, M. F., Robertson, D., Pevsner, P. H., Wall, J. S., Mirzadeh, S., & Kennel, S. J. (2013) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/cbr.2013.1546 · Cited by 47 · see citing works
Atomic Nanogenerators in Targeted Alpha Therapies: Curie’s Legacy in Modern Cancer Management
Roscher, M., Bakos, G., & Benešová, M. (2020) · Pharmaceuticals · doi:10.3390/ph13040076 · Cited by 47 · see citing works
Modelling and Dosimetry for Alpha-Particle Therapy
Sgouros, G., Hobbs, R. F., & Hong, S. (2011) · Current Radiopharmaceuticals · doi:10.2174/1874471011104030261 · Cited by 43 · see citing works
Self-citationRubira, L., Deshayes, E., Santoro, L., Kotzki, P. O., & Fersing, C. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15041051 · Cited by 40 · see citing works
Carter, L. M., Poty, S., Sharma, S. K., & Lewis, J. S. (2018) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.3612 · Cited by 36 · see citing works
Alpha-particle radiotherapy: For large solid tumors diffusion trumps targeting
Zhu, C., Sempkowski, M., Holleran, T. J., Linz, T., Thomas, B., Josefsson, A., Bruchertseifer, F., Morgenstern, A., & Sofou, S. (2017) · Biomaterials · doi:10.1016/j.biomaterials.2017.03.035 · Cited by 34 · see citing works
Lakes, A. L., An, D. D., Gauny, S. S., Ansoborlo, C., Liang, B. H., Rees, J. A., McKnight, K. D., Karsunky, H., & Abergel, R. J. (2020) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.0c00703 · Cited by 34 · see citing works
Preclinical Evaluation of 225Ac-Labeled Single-Domain Antibody for the Treatment of HER2pos Cancer
Rodak, M., Dekempeneer, Y., Wojewódzka, M., Caveliers, V., Covens, P., Miller, B. W., Sevenois, M. B., Bruchertseifer, F., Morgenstern, A., Lahoutte, T., et al. (2022) · Molecular Cancer Therapeutics · doi:10.1158/1535-7163.mct-21-1021 · Cited by 35 · see citing works
Jaggi, J. S., Carrasquillo, J. A., Seshan, S. V., ZANZONICO, P. B., Henke, E., Nagel, A., Schwartz, J., Beattie, B., Kappel, B. J., Chattopadhyay, D., et al. (2007) · Journal of Clinical Investigation · doi:10.1172/jci32226 · Cited by 32 · see citing works
Self-citation212Pb in targeted radionuclide therapy: a review
Scaffidi-Muta, J. M., & Abell, A. D. (2025) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-025-00362-7 · Cited by 30 · see citing works
213Bi‐radioimmunotherapy defeats early‐stage disseminated gastric cancer in nude mice
Beck, R., Seidl, C., Pfost, B., Morgenstern, A., Bruchertseifer, F., Baum, H. H. E., Schwaiger, M., & Senekowitsch–Schmidtke, R. (2007) · Cancer Science · doi:10.1111/j.1349-7006.2007.00525.x · Cited by 30 · see citing works
Максимилианович, Т. В., Wållberg, H., Andersson, K., Wennborg, A., Lundqvist, H., & Orlova, A. (2009) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-009-1134-9 · Cited by 30 · see citing works
Targeted Alpha Therapy and Nanocarrier Approach
Silindir‐Gunay, M., Karpuz, M., & Özer, A. Y. (2020) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/cbr.2019.3213 · Cited by 29 · see citing works
CKD After 225Ac-PSMA617 Therapy in Patients With Metastatic Prostate Cancer
Pelletier, K., Côté, G., Fallah‐Rad, N., John, R., & Kitchlu, A. (2020) · Kidney International Reports · doi:10.1016/j.ekir.2020.12.006 · Cited by 27 · see citing works
Holzwarth, U., Ojea‐Jiménez, I., & Calzolai, L. (2018) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-018-0042-3 · Cited by 26 · see citing works
Challenges and opportunities in developing Actinium-225 radiopharmaceuticals
Dhiman, D., Vatsa, R., & Sood, A. K. (2022) · Nuclear Medicine Communications · doi:10.1097/mnm.0000000000001594 · Cited by 25 · see citing works
Amicis, F. D., Lanzino, M., Kisslinger, A., Calı̀, G., Chieffi, P., Andò, S., Mancini, F. P., & Tramontano, D. (2006) · Journal of Cellular Physiology · doi:10.1002/jcp.20709 · Cited by 24 · see citing works
A GATE simulation study for dosimetry in cancer cell and micrometastasis from the 225Ac decay chain
Koniar, H., Miller, C., Rahmim, A., Schaffer, P. C., & Uribe, C. (2023) · EJNMMI Physics · doi:10.1186/s40658-023-00564-5 · Cited by 22 · see citing works
Alpha‐emitters and targeted alpha therapy in cancer treatment
Zhang, J., Qin, S., Yang, M., Zhang, X., Zhang, S., & Yu, F. (2023) · iRadiology · doi:10.1002/ird3.30 · Cited by 22 · see citing works
Ali, A. M., Dehdashti, F., DiPersio, J. F., & Cashen, A. F. (2016) · Blood Reviews · doi:10.1016/j.blre.2016.04.007 · Cited by 17 · see citing works
Current landscape and future directions of targeted-alpha-therapy for glioblastoma treatment
Roncali, L., Hindré, F., Samarut, É., Lacœuille, F., Rousseau, A., D, J.-M. L. M., Garcion, E., & Chérel, M. (2025) · Theranostics · doi:10.7150/thno.106081 · Cited by 16 · see citing works
Kondo, M., Cai, Z., Chan, C., Brown, M. K., & Reilly, R. M. (2024) · Molecular Pharmaceutics · doi:10.1021/acs.molpharmaceut.4c01071 · Cited by 15 · see citing works
Winter, R., Amghar, M., Wacker, A. S., Bakos, G., Taş, H., Roscher, M., Kelly, J. M., & Benešová, M. (2024) · Pharmaceuticals · doi:10.3390/ph17081031 · Cited by 15 · see citing works
Radioimmunotherapy for Hematopoietic Cell Transplantation
Jurcic, J. G. (2013) · Immunotherapy · doi:10.2217/imt.13.11 · Cited by 15 · see citing works
Castillo, D., Saint‐Hubert, M. D., Crabbé, M., Struelens, L., & Koole, M. J. B. (2020) · The Quarterly Journal of Nuclear Medicine and Molecular Imaging · doi:10.23736/s1824-4785.20.03266-5 · Cited by 15 · see citing works
Approaches to Reducing Normal Tissue Radiation from Radiolabeled Antibodies
Suzuki, H. Y., Kannaka, K., & Uehara, T. (2024) · Pharmaceuticals · doi:10.3390/ph17040508 · Cited by 14 · see citing works
Salerno, D., Howe, A. K., Bhatavdekar, O., Josefsson, A., Pacheco‐Torres, J., Bhujwalla, Z. M., Gabrielson, K. L., & Sofou, S. (2021) · Bioengineering & Translational Medicine · doi:10.1002/btm2.10266 · Cited by 13 · see citing works
Nawar, M. F., Selim, A. A., Essa, B. M., El-Daoushy, A. F., Swidan, M. M., Chambers, C., Al-Qahtani, M. H., Smith, C. J., & Sakr, T. M. (2025) · Cancers · doi:10.3390/cancers17183055 · Cited by 12 · see citing works
Cure of Disseminated Human Lymphoma with [225Ac]Ac-Ofatumumab in a Preclinical Model
Longtine, M. S., Shim, K., Hoegger, M. J., Benabdallah, N., Abou, D. S., Thorek, D. L. J., & Wahl, R. L. (2023) · Journal of Nuclear Medicine · doi:10.2967/jnumed.122.265167 · Cited by 11 · see citing works
A High-Throughput Screen for Alpha Particle Radiation Protectants
Seideman, J. H., Shum, D., Djaballah, H., & Scheinberg, D. A. (2010) · Assay and Drug Development Technologies · doi:10.1089/adt.2010.0291 · Cited by 11 · see citing works
Self-citationScalability study on [133La]LaCl3 production with a focus on potential clinical applications
Brühlmann, S. A., Walther, M., Blei, M., Mamat, C., Kopka, K., Freudenberg, R., & Kreller, M. (2024) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-024-00292-w · Cited by 10 · see citing works
Iorio, V. D., Sarnelli, A., Boschi, S., Sansovini, M., Genovese, R. M., Ştefănescu, C., Ghizdovăţ, V., Jalloul, W., Young, J. D., Sosabowski, J. K., et al. (2025) · Pharmaceuticals · doi:10.3390/ph18101578 · Cited by 9 · see citing works
Jurcic, J. G., Wong, J. Y. C., Knox, S. J., Wahl, D. R., Rosenblat, T. L., & Meredith, R. F. (2015) · Elsevier eBooks · doi:10.1016/b978-0-323-24098-7.00022-8 · Cited by 7 · see citing works
Nair, R. R., Prasad, A. G., Bhatavdekar, O., Sarkar, A., Gabrielson, K. L., & Sofou, S. (2024) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-024-06710-0 · Cited by 6 · see citing works
Recent Achievements about Targeted Alpha Therapy-Based Targeting Vectors and Chelating Agents
Alvandi, M., Farzipour, S., Shaghaghi, Z., Abbasi, S., & Albooyeh, H. (2021) · Anti-Cancer Agents in Medicinal Chemistry · doi:10.2174/1871520621666210727120308 · Cited by 6 · see citing works
Evaluation of the Effect of Chelating Arms and Carrier Agents on t he Radiotoxicity of TAT Agents
Alvandi, M., Farzipour, S., Shaghaghi, Z., Raeispour, M., Jalali-Zefrei, F., & Ahmadieh-Yazdi, A. (2022) · Current Radiopharmaceuticals · doi:10.2174/1874471015666220510161047 · Cited by 6 · see citing works
EANM recommendations for dosimetry in targeted radionuclide therapy with alpha-emitters
Gabiña, P. M., Gleisner, K. S., Chouin, N., Tran‐Gia, J., Koole, M., Cremonesi, M., Denis-Bacelar, A. M., Cassano, B., Verburg, F. A., Brosch-Lenz, J., et al. (2026) · EANM Innovation · doi:10.1016/j.eanmi.2025.100018 · Cited by 5 · see citing works
Development of a prelabeling approach for a targeted nanochelator
Fitzsimmons, J., Atcher, R. W., & Cutler, C. S. (2015) · Journal of Radioanalytical and Nuclear Chemistry · doi:10.1007/s10967-015-3976-x · Cited by 5 · see citing works
Radiation Biology of Radiopharmaceuticals: Beyond External Beam Radiation Therapy
Olson, A. P., Engle, J. W., & Pandey, M. K. (2026) · Pharmaceuticals · doi:10.3390/ph19040591 · Cited by 4 · see citing works
EXPERIMENTAL IN VITRO DOSIMETRY OF 223RA AND 177LU
Ondrák, L., Sommer, M., Štěpán, V., Davídková, M., Vlk, M., Kundrát, P., & Kozempel, J. (2022) · Radiation Protection Dosimetry · doi:10.1093/rpd/ncac090 · Cited by 2 · see citing works
Developing a dedicated comprehensive α-radionuclide therapy program
Basu, S. K., & Banerjee, S. (2016) · Nuclear Medicine Communications · doi:10.1097/mnm.0000000000000626 · Cited by 2 · see citing works
Radionuclide‑drug conjugates in lung cancer: advances in precision therapy and clinical translation
Liu, J., Zuo, X., Yang, X., Wang, X., Gan, L., & Xue, J. (2026) · Molecular Cancer · doi:10.1186/s12943-026-02695-6 · Cited by 1 · see citing works
Cyclotron production of 206Bi for SPECT tracing of bismuth radioisotopes’ redistribution in vivo
Aluicio‐Sarduy, E., Wehner, L. E., Jeffery, J. J., Levitt, N. P., Mixdorf, J. C., Barnhart, T. E., Hernandez, R. T., & Engle, J. W. (2026) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2026.112822 · Cited by 1 · see citing works
Martellini, M., Leung, K. N., Gherardi, G., & Falzone, L. (2023) · Medical Research Archives · doi:10.18103/mra.v11i9.4409 · Cited by 1 · see citing works
Leukemic Stem Cell-targeting Auger Electron Radioimmunotherapeutic Agent for Acute Myeloid Leukemia
Bergstrom, D. (2015) · TSpace (University of Toronto) · Cited by 1 · see citing works
Radionuclide Therapy of Leukemias
Abi‐Ghanem, A. S. (2012) · Springer eBooks · doi:10.1007/978-1-4614-4021-5_2
Radioimmunotherapy of Acute Myeloid Leukemia
Rosenblat, T. L., & Jurcic, J. G. (2010) · Wiley eBooks · doi:10.1002/9780470613214.ch7
Cyclotron-Based Radiopharmaceuticals for Nuclear Medicine Therapy
Barbet, J., Bourgeois, M., & Chatal, J. (2012) · Medical radiology · doi:10.1007/174_2012_668
Current Status of alpha emitters useful for targeted radionuclide therapy
Washiyama, K. (2020) · Drug Delivery System · doi:10.2745/dds.35.102
Status of Development of Short-Range Radionuclide Therapeutic Agents
(公社)日本アイソトープ協会理工・ライフサイエンス部会放射線照射標的分子探索専門委員会 (2024) · RADIOISOTOPES · doi:10.3769/radioisotopes.73.271
Olaosun, A. M., Aborisade, C. A., Shian, D. E., Osuolale, P. T., Oloyede, O. O., & Balogun, F. A. (2025) · Radiation effects and defects in solids · doi:10.1080/10420150.2025.2519986
- Authors
- Singh Jaggi, J., Kappel, B. J., McDevitt, M. R., Sgouros, G., Flombaum, C. D., Cabassa, C., & Scheinberg, D. A.
- Affiliations
- 1Molecular Pharmacology and Chemistry Program;
- Memorial Sloan Kettering Cancer Center (US)
- Johns Hopkins University (US)
- Venue
- Cancer Research
- Published
- 2005-06-01
- Volume
- 65
- Issue
- 11
- Pages
- 4888-4895
- ISSN
- 0008-5472 (ISSN-L)
- 1538-7445
- OpenAlex
- W2135368140
- Cited by
- 98
- References
- 41
- Citations by year
- 2026: 4 · 2025: 5 · 2024: 6 · 2023: 6 · 2022: 6 · 2021: 4 · 2020: 9 · 2019: 4 · 2018: 9 · 2017: 2 · 2016: 3 · 2015: 5 · 2014: 2 · 2013: 5 · 2012: 4
- FWCI
- 4.34
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Cancer Research (publishedVersion)
- PubMed (publishedVersion)
- Funders
- U.S. Public Health Service (P01 33049)
- National Cancer Institute (R01CA055349, R01-CA 55349)
- Topics
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Radiopharmaceutical Chemistry and Applications
- Health Sciences › Health Professions › Radiological and Ultrasound Technology › Radioactivity and Radon Measurements
- Health Sciences › Medicine › Radiology, Nuclear Medicine and Imaging › Effects of Radiation Exposure
- Keywords
- targeted alpha therapy, actinium-225, bismuth-213, francium-221, metal chelation, DMPS, DMSA, furosemide, chlorothiazide, diuresis, bismuth subnitrate, tumor burden
- MeSH terms
- Actinium, Alpha Particles, Animals, Antibodies, Monoclonal, Immunotoxins, Bismuth, Chelating Agents, Succimer, Female, Francium, Kidney, Lymphoma, Macaca fascicularis, Male, Mice, Inbred BALB C, Unithiol, Radioimmunotherapy, Mice, SCID, Mice
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
Are you an author, or do you see a problem with this page? Request a review