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Production, quality control, biodistribution and imaging studies of 177Lu-PSMA-617 in breast adenocarcinoma model

  • Mehdi Sharifi EMAIL logo , Amir Reza Jalilian , Hassan Yousefnia , Behrouz Alirezapour , Ali Bahrami-Samani and Samaneh Zolghadri
Published/Copyright: February 2, 2018

Abstract

177Lu-PSMA-617 therapeutic agent was prepared successfully under optimized condition of pH=4.5, molar ratio of metal to ligand 1:10, temperature of 95°C and 40 min reaction time. 177LuCl3 was obtained with specific activity of 70–80 GBq/mg by the thermal neutron irradiation (5×1013 n cm−2 s−1) of the enriched Lu2O3 (52% 176Lu) samples. The radionuclidic purity of 177LuCl3 (>99%) was checked by a HPGe detector. The radiochemical purities of 177LuCl3 solution and 177Lu-PSMA-617 compound (>98%) were checked by ITLC and HPLC techniques and stability studies were assayed in the presence of human serum. Biodistribution and imaging assessments in the breast adenocarcinoma-bearing mice showed a major accumulation of activity in the tumor and kidneys tissues, as the expression site of PSMA molecule and the main route of excretion, respectively.

  1. Author’s statement: The authors declare no conflict of interest.

References

1. Jemal, A., Bray, F., Center, M. M., Ferlay, J., Ward, E., Forman, D.: Global cancer statistics. CA Cancer J. Clin. 61(2), 69 (2011).10.3322/caac.20107Search in Google Scholar PubMed

2. Banerjee, S. R., Foss, C. A., Castanares, M., Mease, R. C., Byun, Y., Fox, J. J., Hilton, J., Lupold, S. E., Kozikowski, A. P., Pomper, M. G.: Synthesis and evaluation of technetium-99m-and rhenium-labeled inhibitors of the prostate-specific membrane antigen (PSMA). J. Med. Chem. 51(15), 4504 (2008).10.1021/jm800111uSearch in Google Scholar PubMed PubMed Central

3. Eder, M., Eisenhut, M., Babich, J., Haberkorn, U.: PSMA as a target for radiolabelled small molecules. Eur. J. Nucl. Med. Mol. Imaging 40(6), 819 (2013).10.1007/s00259-013-2374-2Search in Google Scholar PubMed PubMed Central

4. Bacich, D. J., Pinto, J. T., Tong, W. P., Heston, W. D.: Cloning, expression, genomic localization, and enzymatic activities of the mouse homolog of prostate-specific membrane antigen/NAALADase/folate hydrolase. Mamm. Genome 12(2), 117 (2001).10.1007/s003350010240Search in Google Scholar PubMed

5. Chang, S. S., Reuter, V. E., Heston, W., Bander, N. H., Grauer, L. S., Gaudin, P. B.: Five different anti-prostate-specific membrane antigen (PSMA) antibodies confirm PSMA expression in tumor-associated neovasculature. Cancer Res. 59(13), 3192 (1999).Search in Google Scholar

6. Demirci, E., Ocak, M., Kabasakal, L., Decristoforo, C., Talat, Z., Halaç, M., Kanmaz, B.: 68Ga-PSMA PET/CT imaging of metastatic clear cell renal cell carcinoma. Eur. J. Nucl. Med. Mol. Imaging 41(7), 1461 (2014).10.1007/s00259-014-2766-ySearch in Google Scholar PubMed

7. Verburg, F. A., Krohn, T., Heinzel, A., Mottaghy, F. M., Behrendt, F. F.: First evidence of PSMA expression in differentiated thyroid cancer using [68Ga] PSMA-HBED-CC PET/CT. Eur. J. Nucl. Med. Mol. Imaging 42(10), 1622 (2015).10.1007/s00259-015-3065-ySearch in Google Scholar PubMed

8. Wernicke, A. G., Varma, S., Greenwood, E. A., Christos, P. J., Chao, K., Liu, H., Bander, N. H., Shin, S. J.: Prostate-specific membrane antigen expression in tumor-associated vasculature of breast cancers. APMIS 122(6), 482 (2014).10.1111/apm.12195Search in Google Scholar PubMed

9. Kratochwil, C., Afshar-Oromieh, A., Kopka, K., Haberkorn, U., Giesel, F. L.: Current status of prostate-specific membrane antigen targeting in nuclear medicine: clinical translation of chelator containing prostate-specific membrane antigen ligands into diagnostics and therapy for prostate cancer. Semin. Nucl. Med. 46(5), 405 (2016).10.1053/j.semnuclmed.2016.04.004Search in Google Scholar PubMed

10. Benešová, M., Schäfer, M., Bauder-Wüst, U., Afshar-Oromieh, A., Kratochwil, C., Mier, W., Haberkorn, U., Kopka, K., Eder, M.: Preclinical evaluation of a tailor-made DOTA-conjugated PSMA inhibitor with optimized linker moiety for imaging and endoradiotherapy of prostate cancer. J. Nucl. Med. 56(6), 914 (2015).10.2967/jnumed.114.147413Search in Google Scholar PubMed

11. Kratochwil, C., Giesel, F. L., Eder, M., Afshar-Oromieh, A., Benesová, M., Mier, W., Kopka, K., Haberkorn, U.: [177Lu] Lutetium-labelled PSMA ligand-induced remission in a patient with metastatic prostate cancer. Eur. J. Nucl. Med. Mol. Imaging 42(6), 987 (2015).10.1007/s00259-014-2978-1Search in Google Scholar PubMed

12. Das, T., Guleria, M., Parab, A., Kale, C., Shah, H., Sarma, H. D., Lele, V. R., Banerjee, S.: Clinical translation of 177Lu-labeled PSMA-617: initial experience in prostate cancer patients. Nucl. Med. Biol. 43(5), 296 (2016).10.1016/j.nucmedbio.2016.02.002Search in Google Scholar

13. Zhu, H., Xie, Q., Li, N., Tian, H., Liu, F., Yang, Z.: Radio-synthesis and mass spectrometry analysis of 68Ga-DKFZ-PSMA-617 for non-invasive prostate cancer PET imaging. J. Radioanal. Nucl. Chem. 309(2), 575 (2016).10.1007/s10967-015-4623-2Search in Google Scholar

14. Yadav, M. P., Ballal, S., Tripathi, M., Damle, N. A., Sahoo, R. K., Seth, A., Bal, C.: 177Lu-DKFZ-PSMA-617 therapy in metastatic castration resistant prostate cancer: safety, efficacy, and quality of life assessment. Eur. J. Nucl. Med. Mol. Imaging 44(1), 81 (2017).10.1007/s00259-016-3481-7Search in Google Scholar

15. Sharifi, M., Yousefnia, H., Zolghadri, S., Bahrami-Samani, A., Naderi, M., Jalilian, A. R., Geramifar, P., Beiki, D.: Preparation and biodistribution assessment of 68Ga-DKFZ-PSMA-617 for PET prostate cancer imaging. Nucl. Sci. Tech. 27(6), 142 (2016).10.1007/s41365-016-0134-2Search in Google Scholar

16. Sharifi, M., Yousefnia, H., Bahrami-Samani, A., Jalilian, A. R., Zolghadri, S., Alirezapour, B., Geramifar, P., Maus, S., Beiki, D.: Optimized production, quality control, biological evaluation and PET/CT imaging of 68Ga-PSMA-617 in breast adenocarcinoma model. Radiochim. Acta. 105(5), 399 (2017).10.1515/ract-2016-2632Search in Google Scholar

17. Essen, M. V., Krenning, E. P., Jong, M. D., Valkema, R., Kwekkeboom, D. J.: Peptide receptor radionuclide therapy with radiolabelled somatostatin analogues in patients with somatostatin receptor positive tumours. Acta Oncol. 46(6), 723 (2007).10.1080/02841860701441848Search in Google Scholar

18. Pillai, M., Chakraborty, S., Das, T., Venkatesh, M., Ramamoorthy, N.: Production logistics of 177Lu for radionuclide therapy. Appl. Radiat. Isot. 59(2), 109 (2003).10.1016/S0969-8043(03)00158-1Search in Google Scholar

19. Das, T., Pillai, M.: Options to meet the future global demand of radionuclides for radionuclide therapy. Nucl. Med. Biol. 40(1), 23 (2013).10.1016/j.nucmedbio.2012.09.007Search in Google Scholar PubMed

20. Alirezapour, B., Rasaee, M. J., Jalilian, A. R., Rajabifar, S., Mohammadnejad, J., Paknejad, M., Maadi, E., Moradkhani, S.: Development of [64Cu]-DOTA-PR81 radioimmunoconjugate for MUC-1 positive PET imaging. Nucl. Med. Biol. 43(1), 73 (2016).10.1016/j.nucmedbio.2015.07.012Search in Google Scholar PubMed

Received: 2017-9-3
Accepted: 2017-12-1
Published Online: 2018-2-2
Published in Print: 2018-6-27

©2018 Walter de Gruyter GmbH, Berlin/Boston

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