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Compartmental and dosimetric studies of anti-CD20 labeled with 188Re

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Abstract

Radioimmunotherapy has the potential to deliver lethal radiation energy directly to malignant cells via targeting of radioisotope-conjugated monoclonal antibodies (MAbs) to specific antigens. Rituximab (RTX) is specifically targeted against CD20, a surface antigen expressed by B-lymphocytes. The use of 188Re from a 188W/188Re generator system represents an alternative radionuclide for therapy. Rhenium has chemical properties similar to technetium and both can be conjugated to antibodies using similar chemistry methods. The objective of this work is to prove the usefulness of this radiopharmaceutical based on dosimetric and pharmacokinetic studies that are also required by the Brazilian Regulatory Agency.

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References

  1. Das T, Pillai MRA (2014) Options to meet the future global demand of radionuclides for radionuclide therapy. Nucl Med Biol 40(1):23–32

    Article  Google Scholar 

  2. Davis TA, Kaminski MS, Leonard JP, Hsu FJ, Wilkinson M, Zelenetz A, Wahl RL, Kroll S, Coleman M, Goris M, Levy R, Knox SJ (2004) The radioisotope contributes significantly to the activity of radioimmunotherapy. Clin Cancer Res 10:7792–7798

    Article  CAS  Google Scholar 

  3. Kaminski MS (2005) 131I-Tositumomab therapy as initial treatment for follicular lymphoma. N Engl J Med 352:441–450

    Article  CAS  Google Scholar 

  4. Witzig TE, Flinn IW, Gordon LI, Emmanouilides C, Czuczman MS, Saleh MN, Cripe L, Wiseman G, Olejnik T, Multani PS, White CA (2002) Treatment with ibritumomab tiuxetan radioimmunotherapy in patients with rituximab-refractory follicular non-Hodgkin’s lymphoma. J Clin Oncol 20(15):3262–3269

    Article  CAS  Google Scholar 

  5. Audicio PF, Castellano G, Tassano MR, Rezzano ME, Fernandez M, Riva E, Robles A, Cabral P, Balter H, Olivier P (2011) [177Lu]DOTA-anti-CD20: labeling and pre-clinical studies. Appl Radiat Isot 69:924–928

    Article  CAS  Google Scholar 

  6. Ferro-Flores G, de Murphy CA (2008) Pharmacokinetics and dosimetry of 188Re-pharmaceuticals. Adv Drug Deliv Rev 60:1389–1401

    Article  CAS  Google Scholar 

  7. Dias CRBR, Jeger S, Osso JA Jr, Müller C, Pasquale CD, Hohn A, Waibel R, Schibli R (2011) Radiolabeling of rituximab with 188Re and 99mTc using the tricarbonyl Technology. Nucl Med Biol 38:19–28

    Article  CAS  Google Scholar 

  8. Buchsbaum DJ (2000) Experimental radioimmunotherapy. Sem Radiat Oncol 10:156–167

    Article  CAS  Google Scholar 

  9. Liu A, Williams L, Lopatin G, Yamauchi D, Wong J, Raubitschek A (1999) A radionuclide therapy treatment planning and dose estimation system. J Nucl Med 40:1151–1153

    CAS  Google Scholar 

  10. Volkert WA, Hoffman TJ (1999) Therapeutic raiopharmaceuticals. Chem Rev 99:2269–2292

    Article  CAS  Google Scholar 

  11. Volkert WA, Goeckler WF, Ehrhardt GJ, Ketring AR (1991) Therapeutic radionuclides: production and decay property considerations. J Nucl Med 32:174–185

    CAS  Google Scholar 

  12. Srivastava SC (1996) Therapeutic radionuclides: making the right choice. In: Mather SJ (ed) Current direction in radiopharmaceutical research and development. Kluver Academic Publishers, Dordrecht, pp 63–79

    Chapter  Google Scholar 

  13. Srivastava SC (1999) Traditional and new isotopes for radioimmunotherapy. In: Riva P (ed) Therapy of malignancies with radioconjugates monoclonal antibodies: present possibilities and future perspectives. Harwood Academic Publishers, Chur. Switzerland, pp 11–26

    Google Scholar 

  14. Neves M, Kling A, Oliveira A (2005) Radionuclides for therapy and suggestion of new candidates. J Radioanal Nucl Chem 266:377–384

    Article  CAS  Google Scholar 

  15. Hall DA (2011) Trivalent metals and thallium. Sampson’s Textbook of Radiopharmacy. 4o Ed. 125-139

  16. Cooper M (2011) Radiohalogenation. Sampson’s Textbook of Radiopharmacy. 4o Ed. 141-155

  17. Osso J, Knapp R (2011) Principles and Operation of Radionuclide Generators. Sampson’s Textbook of Radiopharmacy. 4o Ed

  18. Silverman DH, Delpassand ES, Torabi F, Goy A, Mclaughlin P, Murray JL (2004) Radiollabeled antibody therapy in non-Hodgkin’s lymphoma: radiation protection, isotope comparisons and quality of life issues. Cancer Treat Rev 30:165–172

    Article  CAS  Google Scholar 

  19. Milenic DE, Brechbiel MW (2004) Targeting of radio-isotopoes for cancer therapy. Can Biol Ther 3:361–370

    Article  CAS  Google Scholar 

  20. Iznaga-Escobar N (1998) 188Re-directed labeling of monoclonal antibodies for radioimmunotherapy of solid tumors: biodistribution, normal organ dosimetry and toxicology. Nucl Med Biol 25:441–447

    Article  CAS  Google Scholar 

  21. Akanji AG (2006) Estudo de marcação com iodo-131 de anticorpo monoclonal anti-CD20 usado na terapia de linfoma não-Hodgkin’s. (Master Dissertation)

  22. Aurlien E, Larsen RH, Kvalheim G, Bruland OS (2000) Demonstration of highly specific toxicity of the α-emitting radioimmunoconjugate 211At-rituximab against non-Hodgkin’s lymphoma cells. Br J Cancer 83(10):1375–1379

    Article  CAS  Google Scholar 

  23. Keith M, Norwich KH, Wong W, Jeejeebhoy KN (2000) The tissue distribution of tumor necrosis factor-a in rats: a compartmental model. Metabolism 49(10):1309–1317

    Article  CAS  Google Scholar 

  24. Resigno A (2001) The rise and fall of compartmental analysis. Pharmacol Res 44(4):335–340

    Google Scholar 

  25. Wenger Y, Schneider RJ II, Reddy GR, Kopelman R, Jolliet O, Philbert MA (2011) Tissue distribution and pharmacokinetics of stable polyacrylamide nanoparticles following intravenous injection in the rat. Toxicol App Pharmacol 251(3):181–190

    Article  CAS  Google Scholar 

  26. Wastney ME, House WA (2008) Development of a compartmental model of zinc kinetics in mice. J Nutr 138(11):2148–2155

    Article  CAS  Google Scholar 

  27. MONOLIX Version 4.2.2 (2013) User Guide. Lixoft

  28. Chan PLS, Jacqmin P, Lavielle M, McFadyen L, Weatherley B (2011) The use of the SAEM algorithm in MONOLIX software for estimation of population pharmacokinetic-pharmacodynamic-viral dynamics parameters of maraviroc in asymptomatic HIV subjects. J Pharmacokinet Pharmacodyn 38:41–61

    Article  Google Scholar 

  29. Lavielle M, Mentré F (2007) Estimation of population pharmacokinetic parameters of saquinavir in HIV patients with the MONOLIX Software. J Pharmacokinet Pharmacodyn 34(2):229–249

    Article  CAS  Google Scholar 

  30. Plan EL, Maloney A, Mentré F, Karlsson MO, Bertrand J (2012) Performance comparison of various maximum likelihood nonlinear mixed-effects estimation methods for dose–response Models. AAPS J 14(3):420–432

    Article  Google Scholar 

  31. Savic RM, Mentré F, Lavielle M (2011) Implementation and evaluation of the SAEM algorithm for longitudinal ordered categorical data with an illustration in pharmacokinetics-pharmacodynamics. AAPS J 13(1):44–53

    Article  Google Scholar 

  32. Hindorf C, Jungberg M, Strand SE (2004) Evaluation of parameters influencing S values in mouse dosimetry. J Nucl Med 45:1960–1965

    CAS  Google Scholar 

  33. Loevinger R (1954) The dosimetry of β radiations. Radiology 62:74

    Article  CAS  Google Scholar 

  34. Loevinger R, Japha EM, Brownell GL (1956) Discrete radioisotope sources. I. Beta-radiation. In: Hine GJ, Brownell GL (eds) Radiation dosimetry. Academic, New York, pp 694–754

    Google Scholar 

Download references

Acknowledgments

The authors would like to thank CNEN (Comissão Nacional Energia Nuclear–CNEN/Brazil) for granting a fellowship for this work.

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Authors and Affiliations

  1. Radiopharmacy Center, Instituto de Pesquisas Energeticas e Nucleares, Av. Professor Lineu Prestes, 2242, Cidade Universitaria, Sao Paulo, SP, 05508-000, Brazil

    Barrio Kuramoto Graciela, Mie Nakamura Matsuda Margareth & Alberto Osso João Jr.

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  1. Barrio Kuramoto Graciela
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  2. Mie Nakamura Matsuda Margareth
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  3. Alberto Osso João Jr.
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Correspondence to Barrio Kuramoto Graciela.

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Graciela, B.K., Margareth, M.N.M. & João, A.O. Compartmental and dosimetric studies of anti-CD20 labeled with 188Re. J Radioanal Nucl Chem 309, 1029–1035 (2016). https://doi.org/10.1007/s10967-016-4703-y

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  • DOI: https://doi.org/10.1007/s10967-016-4703-y

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