Development of [225Ac]Ac-PSMA-I&T for Targeted Alpha Therapy According to GMP Guidelines for Treatment of mCRPC
Open accessAbstract
Recently, promising results of the antitumor effects were observed in patients with metastatic castration-resistant prostate cancer treated with 177Lu-labeled PSMA-ligands. Radionuclide therapy efficacy may even be improved by using the alpha emitter Ac-225. Higher efficacy is claimed due to high linear energy transfer specifically towards PSMA positive cells, causing more double-strand breaks. This study aims to manufacture [225Ac]Ac-PSMA-I&T according to good manufacturing practice guidelines for the translation of [225Ac]Ac-PSMA-I&T into a clinical phase 1 dose escalation study. Quencher addition during labeling was investigated. Quality control of [225Ac]Ac-PSMA-I&T was based on measurement of Fr-221 (218 keV), in equilibrium with Ac-225 in approximately six half-lives of Fr-221 (T½ = 4.8 min). Radio-(i)TLC methods were utilized for identification of the different radiochemical forms, gamma counter for concentration determination, and HPGe-detector for the detection of the radiochemical yield. Radiochemical purity was determined by HPLC. The final patient dose was prepared and diluted with an optimized concentration of quenchers as during labeling, with an activity of 8–12 MBq (±5%), pH > 5.5, 100 ± 20 μg/dose, PSMA-I&T, radiochemical yield >95%, radiochemical purity >90% (up to 3 h), endotoxin levels of <5 EU/mL, osmolarity of 2100 mOsmol, and is produced according to current guidelines. The start of the phase I dose escalation study is planned in the near future.
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
Integrity signals
Registry
Cites
Statistics
Claims the paper makes
The claims and statistics of this paper haven’t been checked yet.
Run the check — free, no account needed. It reads the open-access text and checks the sources it cites.
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?
Recent results indicated that the release of free metals from DOTA may be not as evident as expected, as shown by fractioned radio-HPLC.
“However, recent results indicated that the release of free metals from DOTA may be not as evident as expected shown by fractioned radio-HPLC (115).”
From Alpha-peptide receptor radionuclide therapy using actinium-225 labeled somatostatin receptor agonists and antagonists (2022) · cites this paper as [115]
Self-check
Percentages, sums and reported differences re-computed from the paper’s own numbers.
The self-check needs the paper’s full text.
Cites
Epidemiology of Prostate Cancer
Rawla, P. (2019) · World Journal of Oncology · doi:10.14740/wjon1191 · Cited by 2,836 · see citing works
Kratochwil, C., Bruchertseifer, F., Giesel, F. L., Weis, M., Verburg, F. A., Mottaghy, F. M., Kopka, K., Apostolidis, C., Haberkorn, U., & Morgenstern, A. (2016) · Journal of Nuclear Medicine · doi:10.2967/jnumed.116.178673 · Cited by 1,163 · see citing works
Self-citationTumor target prostate specific membrane antigen (PSMA) and its regulation in prostate cancer
Ghosh, A., & Heston, W. D. W. (2003) · Journal of Cellular Biochemistry · doi:10.1002/jcb.10661 · Cited by 883 · see citing works
Weineisen, M., Schottelius, M., Šimeček, J., Baum, R. P., Yıldız, A., Beykan, S., Kulkarni, H., Laßmann, M., Klette, I., Eiber, M. J., et al. (2015) · Journal of Nuclear Medicine · doi:10.2967/jnumed.115.158550 · Cited by 540 · see citing works
Baum, R. P., Kulkarni, H., Schuchardt, C., Singh, A., Wirtz, M., Wiessalla, S., Schottelius, M., Müeller, D., Klette, I., & Wester, H. (2016) · Journal of Nuclear Medicine · doi:10.2967/jnumed.115.168443 · Cited by 526 · see citing works
Kratochwil, C., Bruchertseifer, F., Rathke, H., Bronzel, M., Apostolidis, C., Weichert, W., Haberkorn, U., Giesel, F. L., & Morgenstern, A. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.117.191395 · Cited by 505 · see citing works
Self-citationKratochwil, C., Bruchertseifer, F., Rathke, H. G., Hohenfellner, M., Giesel, F. L., Haberkorn, U., & Morgenstern, A. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.117.203539 · Cited by 429 · see citing works
Self-citationAn Overview of Targeted Alpha Therapy with 225Actinium and 213Bismuth
Morgenstern, A., Apostolidis, C., Kratochwil, C., Sathekge, M. M., Królicki, L., & Bruchertseifer, F. (2018) · Current Radiopharmaceuticals · doi:10.2174/1874471011666180502104524 · Cited by 371 · see citing works
Self-citation225Ac-PSMA-617 in chemotherapy-naive patients with advanced prostate cancer: a pilot study
Sathekge, M. M., Bruchertseifer, F., Knoesen, O., Reyneke, F., Lawal, I. O., Lengana, T., Davis, C., Mahapane, J., Corbett, C., Vorster, M., et al. (2018) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-018-4167-0 · Cited by 361 · see citing works
Self-citationFeuerecker, B., Tauber, R., Knorr, K., Heck, M. M., Beheshti, A., Seidl, C., Bruchertseifer, F., Pickhard, A., Gafita, A., Kratochwil, C., et al. (2020) · European Urology · doi:10.1016/j.eururo.2020.11.013 · Cited by 283 · see citing works
Self-citationAn overview of targeted alpha therapy
Kim, Y., & Brechbiel, M. W. (2011) · Tumor Biology · doi:10.1007/s13277-011-0286-y · Cited by 280 · see citing works
A 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
Consensus nomenclature rules for radiopharmaceutical chemistry — Setting the record straight
Coenen, H. H., Gee, A. D., Adam, M. J., Antoni, G., Cutler, C. S., Fujibayashi, Y., Jeong, J. M., Mach, R. H., Mindt, T. L., Pike, V. W., et al. (2017) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2017.09.004 · Cited by 227 · 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
Okamoto, S., Thieme, A., Allmann, J., D’Alessandria, C., Maurer, T., Retz, M., Tauber, R., Heck, M. M., Wester, H.-J., Tamaki, N., et al. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.116.178483 · Cited by 213 · 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
Development 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
Sathekge, M. M., Bruchertseifer, F., Vorster, M., Lawal, I. O., Knoesen, O., Mahapane, J., Davis, C., Reyneke, F., Maes, A., Kratochwil, C., et al. (2019) · Journal of Nuclear Medicine · doi:10.2967/jnumed.119.229229 · Cited by 196 · see citing works
Self-citationFirst Clinical Results for PSMA-Targeted α-Therapy Using 225Ac-PSMA-I&T in Advanced-mCRPC Patients
Zacherl, M. J., Gildehaus, F. J., Mittlmeier, L. M., Böning, G., Gosewisch, A., Wenter, V., Unterrainer, M., Schmidt-Hegemann, N.-S., Belka, C., Kretschmer, A., et al. (2020) · Journal of Nuclear Medicine · doi:10.2967/jnumed.120.251017 · Cited by 192 · see citing works
Heck, M. M., Retz, M. M., D’Alessandria, C., Rauscher, I., Scheidhauer, K., Maurer, T., Storz, E., Janssen, F., Schottelius, M., Wester, H., et al. (2016) · The Journal of Urology · doi:10.1016/j.juro.2016.02.2969 · Cited by 187 · see citing works
von Eyben, F. E., Roviello, G., Kiljunen, T., Uprimny, C., Virgolini, I. J., Kairemo, K., & Joensuu, T. K. (2017) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-017-3895-x · Cited by 184 · see citing works
Actinium-225 in targeted alpha-particle therapeutic applications.
A. Scheinberg, D., & R. McDevitt, M. (2011) · Current Radiopharmaceuticalse · doi:10.2174/1874471011104040306 · Cited by 176 · see citing works
Bräuer, A., Grubert, L. S., Roll, W., Schrader, A. J., Schäfers, M. A., Bögemann, M., & Rahbar, K. (2017) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-017-3751-z · Cited by 174 · see citing works
Ahmadzadehfar, H., Wegen, S., Yordanova, A., Fimmers, R., Kürpig, S., Eppard, E., Wei, X. X., Schlenkhoff, C. D., Hauser, S., & Essler, M. (2017) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-017-3716-2 · Cited by 172 · see citing works
Alpha-particles for targeted therapy
Sgouros, G. (2008) · Advanced Drug Delivery Reviews · doi:10.1016/j.addr.2008.04.007 · Cited by 147 · see citing works
Actinium-225 for Targeted α Therapy: Coordination Chemistry and Current Chelation Approaches
Thiele, N. A., & Wilson, J. J. (2018) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/cbr.2018.2494 · Cited by 141 · see citing works
Gillings, N., Hjelstuen, O., Ballinger, J., Béhé, M. P., Decristoforo, C., Elsinga, P. H., Ferrari, V., Peitl, P. K., Koziorowski, J., Laverman, P., et al. (2021) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-021-00123-2 · Cited by 131 · see citing works
Chatalic, K. L. S., Heskamp, S., Konijnenberg, M., Molkenboer‐Kuenen, J. D. M., Franssen, G. M., Groningen, M. C. C., Schottelius, M., Wester, H., van Weerden, W. M., Boerman, O. C., et al. (2016) · Theranostics · doi:10.7150/thno.14744 · Cited by 124 · see citing works
Kozempel, J., Mokhodoeva, O. B., & Vlk, M. (2018) · Molecules · doi:10.3390/molecules23030581 · Cited by 121 · see citing works
EANM guideline on the validation of analytical methods for radiopharmaceuticals
Gillings, N., Todde, S., Béhé, M. P., Decristoforo, C., Elsinga, P. H., Ferrari, V., Hjelstuen, O., Peitl, P. K., Koziorowski, J., Laverman, P., et al. (2020) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-019-0086-z · Cited by 121 · see citing works
Accuracy and Precision of Radioactivity Quantification in Nuclear Medicine Images
Frey, E. C., Humm, J. L., & Ljungberg, M. H. (2012) · Seminars in Nuclear Medicine · doi:10.1053/j.semnuclmed.2011.11.003 · Cited by 97 · see citing works
The 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
Self-citationGuideline to regulations for radiopharmaceuticals in early phase clinical trials in the EU
Verbruggen, A., Coenen, H. H., Deverre, J.-R., Guilloteau, D., Långström, B., Salvadori, P. A., & Halldin, C. (2008) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-008-0853-7 · Cited by 91 · see citing works
Repeated 177Lu-Labeled PSMA-617 Radioligand Therapy Using Treatment Activities of Up to 9.3 GBq
Rathke, H. G., Giesel, F. L., Flechsig, P., Kopka, K., Mier, W., Hohenfellner, M., Haberkorn, U., & Kratochwil, C. (2017) · Journal of Nuclear Medicine · doi:10.2967/jnumed.117.194209 · Cited by 81 · see citing works
Begum, N. J., Thieme, A., Eberhardt, N., Tauber, R., D’Alessandria, C., Beer, A. J., Glatting, G., Eiber, M. J., & Kletting, P. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.117.203505 · Cited by 78 · see citing works
The Future of PSMA-Targeted Radionuclide Therapy: An Overview of Recent Preclinical Research
Ruigrok, E. A. M., van Weerden, W. M., Nonnekens, J., & de Jong, M. (2019) · Pharmaceutics · doi:10.3390/pharmaceutics11110560 · Cited by 75 · see citing works
225Ac-H4py4pa for Targeted Alpha Therapy
Li, L., Rousseau, J., Jaraquemada-Peláez, M. D. G., Wang, X., Robertson, A. K. H., Radchenko, V., Schaffer, P. C., Lin, K., Bénard, F., & Orvig, C. (2020) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.0c00171 · Cited by 70 · see citing works
Ascorbic Acid: Useful as a Buffer Agent and Radiolytic Stabilizer for Metalloradiopharmaceuticals
Liu, S., Ellars, C. E., & Edwards, D. S. (2003) · Bioconjugate Chemistry · doi:10.1021/bc034109i · Cited by 68 · see citing works
Modeling and Predicting Tumor Response in Radioligand Therapy
Kletting, P., Thieme, A., Eberhardt, N., Rinscheid, A., D’Alessandria, C., Allmann, J., Wester, H., Tauber, R., Beer, A. J., Glatting, G., et al. (2018) · Journal of Nuclear Medicine · doi:10.2967/jnumed.118.210377 · Cited by 67 · see citing works
Li, L., Jaraquemada-Peláez, M. D. G., Kuo, H., Merkens, H., Choudhary, N., Gitschtaler, K., Jermilova, U., Colpo, N., Uribe‐Munoz, C., Radchenko, V., et al. (2019) · Bioconjugate Chemistry · doi:10.1021/acs.bioconjchem.9b00225 · Cited by 53 · see citing works
de Blois, E., Chan, H. S., Konijnenberg, M., de Zanger, R., & Breeman, W. A. P. (2013) · Current Topics in Medicinal Chemistry · doi:10.2174/1568026611212230005 · Cited by 51 · see citing works
Half-lives of 221Fr, 217At, 213Bi, 213Po and 209Pb from the 225Ac decay series
Suliman, G., Pommé, S. G., Marouli, M., Ammel, R. V., Stroh, H., Jobbágy, V., Paepen, J., Dirican, A., Bruchertseifer, F., Apostolidis, C., et al. (2013) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2013.02.008 · Cited by 44 · see citing works
Self-citationEANM guideline for the preparation of an Investigational Medicinal Product Dossier (IMPD)
Todde, S., Windhorst, A. D., Béhé, M. P., Bormans, G. M., Decristoforo, C., Faivre-Chauvet, A., Ferrari, V., Gee, A. D., Gulyás, B. Z., Halldin, C., et al. (2014) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-014-2866-8 · Cited by 40 · see citing works
DNA damage in leukocytes after internal ex-vivo irradiation of blood with the α-emitter Ra-223
Schumann, S., Eberlein, U., Muhtadi, R., Laßmann, M., & Scherthan, H. (2018) · Scientific Reports · doi:10.1038/s41598-018-20364-7 · Cited by 40 · see citing works
Influence of various scavengers of •OH radicals on the radiation sensitivity of yeast and bacteria
Múčka, V., Bláha, P., Čuba, V., & Červenák, J. (2013) · International Journal of Radiation Biology · doi:10.3109/09553002.2013.817702 · Cited by 34 · see citing works
de Blois, E., Chan, H. S., de Zanger, R., Konijnenberg, M., & Breeman, W. A. P. (2013) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2013.10.023 · Cited by 33 · see citing works
Labriola, M., Atiq, S. O., Hirshman, N. A., & Bitting, R. L. (2020) · Prostate Cancer and Prostatic Diseases · doi:10.1038/s41391-020-00299-9 · Cited by 33 · see citing works
Kelly, J. M., Amor‐Coarasa, A., Nikolopoulou, A., Kim, D., Williams, C. M., Vallabhajosula, S., & Babich, J. W. (2017) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2017.10.001 · Cited by 32 · see citing works
Computer-Assisted Design of Macrocyclic Chelators for Actinium-225 Radiotherapeutics
Morgenstern, A., Lilley, L. M., Stein, B. W., Kozimor, S. A., Batista, E. R., & Yang, P. X. (2020) · Inorganic Chemistry · doi:10.1021/acs.inorgchem.0c02432 · Cited by 31 · see citing works
Self-citationQin, Y., Imobersteg, S., Blanc, A., Frank, S., Schibli, R., Béhé, M. P., & Grzmil, M. (2020) · Pharmaceutics · doi:10.3390/pharmaceutics12111088 · Cited by 29 · see citing works
Maintaining radiochemical purity of [177Lu]Lu-DOTA-PSMA-617 for PRRT by reducing radiolysis
de Zanger, R. M. S., Chan, H. S., Breeman, W. A. P., & de Blois, E. (2019) · Journal of Radioanalytical and Nuclear Chemistry · doi:10.1007/s10967-019-06573-y · Cited by 28 · see citing works
Medical management of metastatic prostate cancer
Body, A. L., Pranavan, G., Tan, T. H., & Slobodian, P. (2018) · Australian Prescriber · doi:10.18773/austprescr.2018.046 · Cited by 14 · see citing works
A Consensus Time for Performing Quality Control of 225Ac-Labeled Radiopharmaceuticals
Kelly, J. M., Amor-Coarasa, A., Sweeney, E., Wilson, J. J., Causey, P. W., & Babich, J. (2021) · doi:10.21203/rs.3.rs-39342/v2 · Cited by 11 · see citing works
A Consensus Time for Performing Quality Control of 225Ac-Labeled RadiopharmaceuticalsPreprint
Kelly, J. M., Amor‐Coarasa, A., Sweeney, E. M., Wilson, J. J., Causey, P. W., & Babich, J. W. (2020) · doi:10.21203/rs.3.rs-39342/v1 · Cited by 11 · see citing works
Flagged first, then by citations
2 of the 56 references couldn’t be matched to a known paper.
Cited by
Sorted by citations
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
Self-citationShi, 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
Ling, S. W., de Blois, E., Hooijman, E. L., Veldt, A. A. M. V. D., & Brabander, T. (2022) · Pharmaceutics · doi:10.3390/pharmaceutics14102166 · Cited by 63 · see citing works
Self-citationIn vitro dose effect relationships of actinium-225- and lutetium-177-labeled PSMA-I&T
Ruigrok, E. A. M., Tamborino, G., de Blois, E., Roobol, S. J., Verkaik, N. S., Saint‐Hubert, M. D., Konijnenberg, M., van Weerden, W. M., de Jong, M., & Nonnekens, J. (2022) · European Journal of Nuclear Medicine and Molecular Imaging · doi:10.1007/s00259-022-05821-w · Cited by 49 · see citing works
161Tb-PSMA Unleashed: a Promising New Player in the Theranostics of Prostate Cancer
Al‐Ibraheem, A., & Scott, A. M. (2023) · Nuclear Medicine and Molecular Imaging · doi:10.1007/s13139-023-00804-7 · Cited by 47 · see citing works
Kiss, O. C., Kopka, K., Liolios, C. C., & Afshar‐Oromieh, A. (2021) · Cancers · doi:10.3390/cancers13246255 · Cited by 46 · see citing works
Rubira, L., Deshayes, E., Santoro, L., Kotzki, P. O., & Fersing, C. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15041051 · Cited by 40 · see citing works
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
Selçuk, N. A., Beydağı, G., Demirci, E., Ocak, M., Çelik, S., Öven, B. B., Toklu, T., Karaaslan, İ. Ş., Akçay, K., Sönmez, Ö., et al. (2023) · Journal of Nuclear Medicine · doi:10.2967/jnumed.123.265546 · Cited by 36 · see citing works
Hassan, M., Bokhari, T. H., Lodhi, N. A., Khosa, M. K., & Usman, M. (2023) · Chemical Biology & Drug Design · doi:10.1111/cbdd.14311 · Cited by 33 · see citing works
Coll, R. P., Bright, S. J., Martinus, D. K. J., Georgiou, D. K., Sawakuchi, G. O., & Manning, H. C. (2023) · Molecular Imaging and Biology · doi:10.1007/s11307-023-01857-y · Cited by 29 · see citing works
Unterrainer, L. M., Beyer, L., Zacherl, M. J., Gildehaus, F. J., Todica, A. S., Kunte, S. C., Holzgreve, A., Sheikh, G. T., Herlemann, A., Casuscelli, J., et al. (2022) · Biomedicines · doi:10.3390/biomedicines10050946 · Cited by 25 · see citing works
Castillo, D., Saint‐Hubert, M. D., Ahenkorah, S., Vargas, C. S., Ooms, M., Struelens, L., & Koole, M. J. B. (2022) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-022-00174-z · Cited by 20 · see citing works
Handula, M., Beekman, S., Konijnenberg, M., Stuurman, D. C., de Ridder, C., Bruchertseifer, F., Morgenstern, A., Denkova, A. G., de Blois, E., & Seimbille, Y. (2023) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-023-00197-0 · Cited by 21 · see citing works
Self-citationActinium-225 Targeted Agents: Where Are We Now?
Mourtada, F., Tomiyoshi, K., Sims‐Mourtada, J., Mukai-Sasaki, Y., Yagihashi, T., Namiki, Y., Murai, T., Yang, D. J., & Inoue, T. (2023) · Brachytherapy · doi:10.1016/j.brachy.2023.06.228 · Cited by 21 · see citing works
Design of 225Ac-PSMA for targeted alpha therapy in prostate cancer
Kairemo, K., Kgatle, M. M., Bruchertseifer, F., Morgernstern, A., & Sathekge, M. M. (2024) · Annals of Translational Medicine · doi:10.21037/atm-23-1842 · Cited by 18 · see citing works
Self-citationAc-225 radiochemistry through the lens of [225Ac]Ac-DOTA-TATE
Hooijman, E. L., de Jong, J. R., Ntihabose, C., Bruchertseifer, F., Morgenstern, A., Seimbille, Y., Brabander, T., Koolen, S. L. W., & de Blois, E. (2025) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-025-00332-z · Cited by 18 · see citing works
Self-citationA third generation PSMA-targeted agent [211At]YF2: Synthesis and in vivo evaluation
Feng, Y., Meshaw, R. L., Finch, S. W., Zheng, Y., Minn, I., Vaidyanathan, G., Pomper, M. G., & Zalutsky, M. R. (2024) · Nuclear Medicine and Biology · doi:10.1016/j.nucmedbio.2024.108916 · Cited by 18 · see citing works
Mattana, F., Muraglia, L., Barone, A., Colandrea, M., Saker Diffalah, Y., Provera, S., Cascio, A. S., Omodeo Salè, E., & Ceci, F. (2024) · Cancers · doi:10.3390/cancers16091643 · Cited by 16 · see citing works
Deshayes, E., Fersing, C., Thibault, C., Roumiguié, M., Pourquier, P., & Houédé, N. (2023) · Cancers · doi:10.3390/cancers15123133 · Cited by 14 · see citing works
Recent Innovations and Nano-Delivery of Actinium-225: A Narrative Review
Mdanda, S., Ngema, L. M., Mdlophane, A. H., Sathekge, M. M., & Zeevaart, J. R. (2023) · Pharmaceutics · doi:10.3390/pharmaceutics15061719 · Cited by 13 · see citing works
The determination of the radiochemical purity of Actinium-225 radiopharmaceuticals: a conundrum
Kleynhans, J., & Duatti, A. (2022) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-022-00175-y · Cited by 11 · see citing works
Imaging and therapy in prostate cancer using prostate specific membrane antigen radioligands
Naik, M., Khan, S. R., Lewington, V., Challapalli, A., Eccles, A., & Barwick, T. D. (2024) · British Journal of Radiology · doi:10.1093/bjr/tqae092 · Cited by 10 · see citing works
Tomiyoshi, K., Wilson, L. J., Mourtada, F., Sims‐Mourtada, J., Namiki, Y., Kamata, W., Yang, D. J., & Inoue, T. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16111458 · Cited by 9 · see citing works
Wurzer, A. J., Sun, B., Saleh, S., Brosch-Lenz, J., Fischer, S., Kossatz, S., Hürkamp, K., Li, W. B., Eiber, M., Morgenstern, A., et al. (2025) · Journal of Nuclear Medicine · doi:10.2967/jnumed.125.269744 · Cited by 9 · see citing works
Self-citationЛаренков, А. А., Mitrofanov, Y. A., & Rakhimov, M. G. (2024) · Pharmaceutics · doi:10.3390/pharmaceutics16121535 · Cited by 8 · see citing works
Cui, X., Yao, Z., Zhao, T., Guo, J., Ding, J., Zhang, S., Liang, Z., Wei, Z., Zoa, A., Tian, Y., et al. (2022) · Frontiers in Oncology · doi:10.3389/fonc.2022.1069033 · Cited by 7 · see citing works
Ashhar, Z., Fadzil, M. F. A., Safee, Z. M., Aziz, F., Ibarhim, U. H., Afinde, N. M. F. N., Ail, N. M., Harizan, M. A. H. J., Halib, D., Amran, A. A., et al. (2023) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2023.111161 · Cited by 6 · see citing works
Prostate-specific Membrane Antigen: Alpha-labeled Radiopharmaceuticals
Ndlovu, H., Mokoala, K. M. G., Lawal, I. O., Emmett, L., & Sathekge, M. M. (2024) · PET Clinics · doi:10.1016/j.cpet.2024.03.003 · Cited by 6 · see citing works
Ding, J., Qin, S., Hou, X., Zhang, J., Yang, M., Ma, S., Zhu, H., Feng, Y., & Yu, F. (2024) · TrAC Trends in Analytical Chemistry · doi:10.1016/j.trac.2024.118053 · Cited by 5 · see citing works
Aalbersberg, E. A., Cao, T. T., Geluk–Jonker, M. M., & Hendrikx, J. J. M. A. (2022) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-022-00178-9 · Cited by 5 · see citing works
Kara, A. (2022) · Applied Radiation and Isotopes · doi:10.1016/j.apradiso.2022.110552 · Cited by 5 · see citing works
Quality control of actinium-225 and 225Ac-radiopharmaceuticals: Francium-221 to be or not to be?
Toro-González, M., Wheeless, L., Tangadanchu, V. K. R., Hawkins, C. A., Provo, S., Smith, W., Hommen, M., DeVries, D., Harvey, J., Drum, T., et al. (2026) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-025-00419-7 · Cited by 4 · 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
Maystrenko, D. N., Stanzhevskii, A. A., Важенина, Д. А., Одинцова, М. В., Попов, С. А., Номоконова, В. Б., Чипига, Л. А., Сапрыкин, К. А., Gromov, A. V., & Vasiliev, S. K. (2023) · Diagnostic radiology and radiotherapy · doi:10.22328/2079-5343-2022-13-4-86-94 · Cited by 4 · see citing works
Hu, Z., Qu, S., Liu, H., Zhang, Y., Yan, S., Hu, A., Qiu, R., Wu, Z., Zhang, H., & Li, J. (2025) · EJNMMI Physics · doi:10.1186/s40658-025-00765-0 · Cited by 4 · see citing works
Greifenstein, L., Martin, M., Stephan, S., Eismant, A., Kramer, C. S., Landvogt, C., Mueller, C., Rösch, F., & Baum, R. P. (2026) · Pharmaceuticals · doi:10.3390/ph19010172 · Cited by 2 · see citing works
Automated radiolabeling and handling of 177 Lu‐ and 225 Ac‐PSMA‐617 using a robotic pipettor
Ahn, S. H., & Belanger, A. P. (2024) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.4085 · Cited by 2 · see citing works
Wang, Z., Chen, H., Liu, Y., Zou, L., Zhang, Z., Yin, Z., Mao, S., Guo, C., Yang, B., Wu, P., et al. (2025) · Frontiers in Oncology · doi:10.3389/fonc.2024.1466190 · Cited by 2 · see citing works
Tayal, S., Gurjar, M., Shukla, V., Venkatachalam, M., Kumar, R., & Jain, Y. (2024) · Indian Journal of Nuclear Medicine · doi:10.4103/ijnm.ijnm_42_24 · Cited by 1 · see citing works
Rizvi, S. K., Javed, A., & Khan, Q. (2025) · Journal of Radioanalytical and Nuclear Chemistry · doi:10.1007/s10967-025-10346-1 · Cited by 1 · see citing works
Ling, S. W., Konijnenberg, M., Segbers, M., Hooijman, E. L., Koolen, S. L. W., de Blois, E., de Jong, L. C., van Puffelen, A. J., de Lussanet, Q. G., Bruchertseifer, F., et al. (2026) · Journal of Nuclear Medicine · doi:10.2967/jnumed.125.271880 · Cited by 2 · see citing works
Self-citationBera, A., Ragland, G., Zhang, Y., Madel, P. G., B'Lanton, J., Siriki, A., Chen, C.-T., Szmulewitz, R. Z., & Chitneni, S. K. (2026) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-026-00456-w · Cited by 1 · see citing works
Theranostic radiopharmacy for the nuclear medicine and molecular imaging
Ocak, M., & Decristoforo, C. (2022) · Elsevier eBooks · doi:10.1016/b978-0-12-822960-6.00066-1
Gronostaj, P., & Cholewiński, W. (2023) · Letters in Oncology Science · doi:10.21641/los.2023.20.1.238
Assessment of DNA/RNA Deregulation in Cancer Using 99m Tc-Labeled Thiopurine
Chiu, C., Yang, D. J., Liou, Y.-C., Chang, W.-C., Yu, T.-H., Chung, M.-C., Lee, Y., Chen, I.-J., Wang, P.-Y., Lin, C., et al. (2024) · Cancer Biotherapy and Radiopharmaceuticals · doi:10.1089/cbr.2023.0148
Dossier de médicament expérimental (DME) en RIV
Kryza, D., & Couturier, O. (2025) · Médecine Nucléaire · doi:10.1016/j.mednuc.2024.12.001
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
Тищенко, В. К., Viryasov, M. B., Ryzhikova, T. P., Степченкова, Е. Д., Ostroukhov, A. A., Shcherbakova, A. V., Dorovatovskiy, S. A., Власова, О. П., & Иванов, С. А. (2025) · Pharmaceutical Chemistry Journal · doi:10.1007/s11094-025-03397-x
Handula, M., Beekman, S., Konijnenberg, M., Stuurman, D. C., de Ridder, C., Bruchertseifer, F., Morgenstern, A., Denkova, A. G., de Blois, E., & Seimbille, Y. (2023) · Figshare · doi:10.6084/m9.figshare.23612575
Self-citationHooijman, E. L., Ntihabose, C., Koolen, S. L. W., Handula, M., Beekman, S., Stuurman, D. C., de Ridder, C., de Jong, J. R., van de Merbel, J. R. J. P., Rook, N., et al. (2025) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-025-00414-y
Self-citationMoss, C. E., Chvála, O., & Hartanto, D. (2026) · Journal of Nuclear Engineering · doi:10.3390/jne7010009
Hedefe Yönelik Alfa Tedavisi Fiziksel Prensiplerden Klinik Uygulamaya
Beytur, F. (2026) · Akademisyen Kitabevi eBooks · doi:10.37609/akya.4060
Claude, G., Balzer, M., Brenner, W., Bruchertseifer, F., Morgenstern, A., Thonon, D., & Spreckelmeyer, S. (2026) · EJNMMI Radiopharmacy and Chemistry · doi:10.1186/s41181-026-00476-6
Self-citationToward Personalized Theranostics: A Modular PET Platform for Antibody‐Based Imaging and Therapy
Vivier, D., Kple, M. G., Ariztia, J., Leroux, M., Moreau, M., Claron, M., Cheveau, M., Laouafa, A., Kownacka, A., Petitot, C., et al. (2026) · Advanced Science · doi:10.1002/advs.76940
García-Arce, D., Luna‐Gutiérrez, M., Cruz-Nova, P., Limón, A. M. V., Jiménez‐Mancilla, N., Aranda‐Lara, L., Azorin‐Vega, E. P., Morales-Ávila, E., Rodríguez-López, P., Santos‐Cuevas, C., et al. (2026) · International Journal of Molecular Sciences · doi:10.3390/ijms27177785
Wenker, S. T. M., Franssen, G. M., Molkenboer‐Kuenen, J. D. M., Konijnenberg, M., Lobeek, D., Tamborino, G., Peters, H., van Lith, S. A. M., Heskamp, S., & Bussink, J. (2026) · Molecular Imaging and Biology · doi:10.1007/s11307-026-02142-4
- Authors
- Hooijman, E. L., Chalashkan, Y., Ling, S. W., Kahyargil, F. F., Segbers, M., Bruchertseifer, F., Morgenstern, A., Seimbille, Y., Koolen, S. L. W., Brabander, T., & de Blois, E.
- Affiliations
- Erasmus MC (NL)
- Joint Research Centre (DE)
- TRIUMF (CA)
- Erasmus Medical Centre, Department of Radiology and Nuclear Medicine, 3015 CN Rotterdam, The Netherlands
- ORCID
- Venue
- Pharmaceutics
- Publisher
- MDPI AG
- Published
- 2021-05-13
- Volume
- 13
- Issue
- 5
- Pages
- 715
- ISSN
- 1999-4923 (ISSN-L)
- PMC
- PMC8153125
- OpenAlex
- W3162340133
- Cited by
- 59
- References
- 56
- Citations by year
- 2026: 11 · 2025: 9 · 2024: 13 · 2023: 14 · 2022: 11 · 2021: 1
- FWCI
- 5.15
- Type
- journal article
- Language
- en
- Open access
- gold
- doi.org
- Licence
- Locations
- Pharmaceutics (publishedVersion, cc-by)
- PubMed Central (publishedVersion, cc-by)
- PubMed (publishedVersion)
- EUR Research Repository (Erasmus University Rotterdam) (publishedVersion, cc-by)
- EUR Research Repository (Erasmus University Rotterdam) (submittedVersion, cc-by)
- DOAJ (DOAJ: Directory of Open Access Journals) (submittedVersion, cc-by-sa)
- Funders
- KWF Kankerbestrijding (11960)
- 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 › Medicine › Epidemiology › Neuroendocrine Tumor Research Advances
- Keywords
- targeted alpha therapy, metastatic castration-resistant prostate cancer, actinium-225, PSMA ligands, radionuclide therapy, radiochemical yield, radiochemical purity, endotoxin, osmolarity, good manufacturing practices
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
