Nuclear Medicine and Biology
Volume 34, Issue 7 , Pages 779-785 , October 2007

Targeted α-particle radiotherapy with 211At-labeled monoclonal antibodies

  • Michael R. Zalutsky

      Affiliations

    • Department of Radiology, Duke University Medical Center, Durham, NC 27710, USA
    • Corresponding Author InformationCorresponding author. Tel.: +1 919 684 7708; fax: +1 919 684 7121.
  • ,
  • David A. Reardon

      Affiliations

    • Department of Medicine, Duke University Medical Center, Durham, NC 27710, USA
  • ,
  • Oscar R. Pozzi

      Affiliations

    • Department of Radiology, Duke University Medical Center, Durham, NC 27710, USA
  • ,
  • Ganesan Vaidyanathan

      Affiliations

    • Department of Radiology, Duke University Medical Center, Durham, NC 27710, USA
  • ,
  • Darell D. Bigner

      Affiliations

    • Department of Pathology, Duke University Medical Center, Durham, NC 27710, USA

Received 22 February 2007 ,Accepted 20 March 2007.

References 

  1. Mulford DA, Scheinberg DA, Jurcic JG. The promise of targeted α-particle therapy. J Nucl Med. 2005;46:199S–204S
  2. Zalutsky MR, Vaidyanathan G. Astatine-211-labeled radiotherapeutics: an emerging approach to targeted alpha particle therapy. Curr Pharm Des. 2000;6:1433–1455
  3. Allen BJ, Raja C, Rizvi S, Li Y, Tsui W, Zhang D, et al. Targeted alpha therapy for cancer. Phys Med Biol. 2004;49:3703–3712
  4. Akabani G, Carlin S, Welsh P, Zalutsky MR. In vitro cytotoxicity of 211At-labeled trastuzumab in human breast cancer cell lines: effect of specific activity and HER2 receptor heterogeneity on survival fraction. Nucl Med Biol. 2006;33:333–347
  5. Boyd M, Ross SC, Dorrens J, Fullerton NE, Tan KW, Zalutsky MR, et al. Radiation induced biological bystander effect elicited in vitro by targeted radiopharmaceuticals labeled with α-, β- and Auger electron emitting radionuclides. J Nucl Med. 2006;47:1007–1015
  6. Zalutsky MR. Radionuclide therapy. In:  Roesch F editors. Handbook of nuclear chemistry: Vol. 4. Radiochemistry and radiopharmaceutical chemistry in life sciences. Dordrecht, The Netherlands: Kluwer Academic; 2003;p. 315–348
  7. Zalutsky MR, Pozzi OR. Radioimmunotherapy with α-particle emitting radionuclides. Q J Nucl Med Mol Imaging. 2004;48:289–296
  8. Kotzerke J, Bunjes D, Scheinberg DA. Radioimmunoconjugates in acute leukemia treatment: the future is radiant. Bone Marrow Transplantation. 2005;36:1021–1026
  9. Couturier O, Supiot S, Degraef-Mougin M, Faivre-Chauvet A, Carlier T, Chatal J-F, et al. Cancer radioimmunotherapy with alpha-emitting nuclides. Eur J Nucl Med Mol Imaging. 2005;32:601–614
  10. Larsen RH, Murud KM, Hoff P, Bruland ØS, Zalutsky MR. 211At- and 131I-labeled bisphosphonates with high in vivo stability and bone accumulation. J Nucl Med. 1999;40:1197–1203
  11. Johnson EL, Turkington TG, Jaszczak RJ, Vaidyanathan G, Green KL, Coleman RE, et al. Quantitation of 211At in small volumes for evaluation of targeted radiotherapy in animal models. Nucl Med Biol. 1995;22:45–54
  12. Larsen RH, Wieland BW, Zalutsky MR. Evaluation of an internal cyclotron target for the production of astatine-211 via the 209Bi(α,2n)211At reaction. Appl Radiat Isot. 1996;47:135–143
  13. Lindegren S, Bäck T, Jensen HJ. Dry-distillation of astatine-211 from irradiated bismuth targets: a time-saving procedure with high recovery yields. Appl Radiat Isot. 2001;55:157–160
  14. Zalutsky MR, Garg PK, Friedman HS, Bigner DD. Labeling monoclonal antibodies and F(ab′)2 fragments with the alpha particle emitting nuclide astatine-211: preservation of immunoreactivity and in vivo localizing capacity. Proc Natl Acad Sci U S A. 1989;86:7149–7153
  15. Wilbur DS, Vessella RL, Stray JE, Goffe DK, Blouke KA, Atcher RW. Preparation and evaluation of para-[211At]astatobenzoyl labeled anti-renal cell carcinoma antibody A6H F(ab′)2. In vivo distribution comparison with para-[125I]iodobenzoyl labeled A6H F(ab′)2. Nucl Med Biol. 1993;20:917–927
  16. Zalutsky MR, Stabin M, Larsen RH, Bigner DD. Tissue distribution and radiation dosimetry of astatine-211-labeled chimeric 81C6, an α-particle emitting immunoconjugate. Nucl Med Biol. 1997;24:255–262
  17. Aurlien E, Larsen RH, Kvalheim G, Bruland ØS. Demonstration of highly specific toxicity of the alpha-emitting radioimmunoconjugate 211At-rituximab against non-Hodgkin's lymphoma cells. Br J Cancer. 2000;83:1375–1379
  18. Demartis S, Tarli L, Borsi L, Zardi L, Neri D. Selective targeting of tumour neovasculature by a radiohalogenated human antibody fragment specific for the ED-B domain of fibronectin. Eur J Nucl Med. 2001;28:534–539
  19. Palm S, Back T, Claesson I, Delle U, Hultborn R, Lindegren S, et al. Single-cell irradiation from [211At]astatine-labeled C215 monoclonal antibody: improved estimates of radiosensitivity from measurements on cellular uptake and retention. Anticancer Res. 2003;23:1219–1221
  20. Henriksen G, Bruland ØS, Larsen RH. Preparation and preclinical assessment of folate-conjugated, radiolabelled antibodies. Anticancer Res. 2005;25:9–15
  21. Almqvist Y, Orlova A, Sjostrom A, Jensen HJ, Lundqvist H, Sundin A, et al. In vitro characterization of 211At-labeled antibody A33 — a potential therapeutic agent against metastatic colorectal carcinoma. Cancer Biother Radiopharm. 2005;20:514–523
  22. Nestor M, Persson M, van Dongen GA, Jensen HJ, Lundqvist H, Anniko M, et al. In vitro evaluation of the astatinated chimeric monoclonal antibody U36, a potential candidate for treatment of head and neck squamous cell carcinoma. Eur J Nucl Med Mol Imaging. 2005;32:1296–1304
  23. Zhang Z, Zhang M, Garmestani K, Talanov VS, Plascjak PS, Beck B, et al. Effective treatment of a murine model of adult T-cell leukemia using 211At-7G7/B6 and its combination with unmodified anti-Tac (daclizumab) directed toward CD25. Blood. 2006;108:1007–1012
  24. Andersson H, Palm S, Lindegren S, Back T, Jacobsson L, Leser G, et al. Comparison of the therapeutic efficacy of 211At- and 131I-labelled monoclonal antibody MOv18 in nude mice with intraperitoneal growth of human ovarian cancer. Anticancer Res. 2001;21:409–412
  25. Elgqvist J, Andersson H, Back T, Claesson I, Hultborn R, Jensen H, et al. Alpha-radioimmunotherapy of intraperitoneally growing OVCAR-3 tumors of variable dimensions: outcome related to measured tumor size and mean absorbed dose. J Nucl Med. 2006;47:1342–1350
  26. J.N. Wesley, E.C. McGee, K. Garmestani, M.W. Brechbiel, A.T. Yordanov, C. Wu, et al. Systemic radioimmunotherapy using a monoclonal antibody, anti-Tac directed toward the alpha subunit of the IL-2 receptor armed with the α-emitting radionuclides 212Bi or 211At. Nucl Med Biol 2004;31–357–64.
  27. Vaidyanathan G, Affleck DJ, Bigner DD, Zalutsky MR. N-succinimidyl 3-[211At]astato-4-guanidinomethylbenzoate: an acylation agent for labeling internalizing antibodies with α-particle emitting 211At. Nucl Med Biol. 2003;30:351–359
  28. Talanov VS, Yordanov AT, Garmestani K, Milenic DE, Arora HC, Plascjak PS, et al. Preparation and in vivo evaluation of novel linkers for 211At labeling of proteins. Nucl Med Biol. 2004;31:1061–1071
  29. Talanov VS, Garmestani K, Regino CA, Milenic DE, Plascjak PS, Waldmann TA, et al. Preparation and in vivo evaluation of a novel stabilized linker for 211At labeling of protein. Nucl Med Biol. 2006;33:469–480
  30. Welch MJ. Potentials and pitfalls with α-particles. J Nucl Med. 2005;46:1254–1255
  31. Zalutsky MR, Zhao X-G, Alston KL, Bigner DD. High-level production of α-particle-emitting 211At and preparation of 211At-labeled antibodies for clinical use. J Nucl Med. 2001;42:1508–1515
  32. Pozzi OR, Zalutsky MR. Radiopharmaceutical chemistry of targeted radiotherapeutics: I. Effects of solvent on the degradation of radiohalogenation precursors by astatine-211 α-particles. J Nucl Med. 2005;46:700–706
  33. Pozzi OR, Zalutsky MR. Radiopharmaceutical chemistry of targeted radiotherapeutics: II. Radiolytic effects of astatine-211 α-particles influence N-succinimidyl 3-[211At]astatobenzoate synthesis. J Nucl Med. 2005;46:1393–1400
  34. Zalutsky MR. Current status of treatment of solid tumors: brain tumor therapy. J Nucl Med. 2005;46:151S–156S
  35. Reist CJ, Bigner DD, Zalutsky MR. Human IgG2 constant region enhances in vivo stability of anti-tenascin antibody 81C6 compared with its murine parent. Clinical Cancer Res. 1998;4:2495–2502
  36. McLendon RE, Archer GE, Garg PK, Bigner DD, Zalutsky MR. Radiotoxicity of systemically administered [211At]astatide in B6C3F1 and BALB/c (nu/nu) mice: a long term survival study with histologic analysis. Int J Radiat Oncol Biol Phys. 1996;35:69–80
  37. McLendon RE, Archer GE, Larsen RH, Akabani G, Bigner DD, Zalutsky MR. Radiotoxicity of systemically administered 211At-labeled human/mouse chimeric monoclonal antibody: a long-term survival study with histological analysis. Int J Radiat Oncol Biol Phys. 1999;45:491–499
  38. Zalutsky M, Reardon D, Akabani G, Friedman A, Friedman H, Herndon J, et al. Astatine-211 labeled human/mouse chimeric anti-tenascin monoclonal antibody via surgically created resection cavities for patients with recurrent glioma: Phase I study. Neuro-oncol. 2002;4:S103
  39. Stupp R, Mason W, van den Bent MJ, Weller M, Fisher B, Taphoorn MJB, et al. Radiotherapy plus concomitant and adjuvant temozolomide for glioblastoma. N Engl J Med. 2005;352:987–996
  40. Mirimanoff R-O, Gorlia T, Mason W, van den Bent MJ, Kortmann R-D, Fisher B, et al. Radiotherapy and temozolomide for newly diagnosed glioblastoma: recursive partitioning analysis of the EORTC 26981/22981-NCIC CE3 phase III randomized trial. J Clin Oncol. 2006;24:2563–2569

PII: S0969-8051(07)00091-1

doi: 10.1016/j.nucmedbio.2007.03.007

Nuclear Medicine and Biology
Volume 34, Issue 7 , Pages 779-785 , October 2007