Nuclear Medicine and Biology
Volume 36, Issue 6 , Pages 671-680 , August 2009

Evaluation of an anti-p185HER2 (scFv-CH2-CH3)2 fragment following radioiodination using two different residualizing labels: SGMIB and IB-Mal-d-GEEEK

  • Ganesan Vaidyanathan

      Affiliations

    • Duke University Medical Center, Durham, NC 27710, USA
    • Corresponding Author InformationCorresponding author. Radiology, Duke University Medical Center, Box 3808, Durham, NC 27710, USA. Tel.: +1 919 684 7811; fax: +1 919 684 7122.
  • ,
  • Emmanuelle Jestin

      Affiliations

    • Duke University Medical Center, Durham, NC 27710, USA
  • ,
  • Tove Olafsen

      Affiliations

    • Department of Molecular and Medical Pharmacology, Crump Institute for Molecular Imaging, David Geffen School of Medicine at University of California Los Angeles, Los Angeles, CA 90095, USA
  • ,
  • Anna M. Wu

      Affiliations

    • Department of Molecular and Medical Pharmacology, Crump Institute for Molecular Imaging, David Geffen School of Medicine at University of California Los Angeles, Los Angeles, CA 90095, USA
    • AMW is a member of the UCLA Johnson Comprehensive Cancer Center (CA16042).
  • ,
  • Michael R. Zalutsky

      Affiliations

    • Duke University Medical Center, Durham, NC 27710, USA

Received 29 October 2008 ,Revised 31 March 2009 ,Accepted 2 April 2009.

References 

  1. Ferretti G, Felici A, Papaldo P, Fabi A, Cognetti F. HER2/neu role in breast cancer: from a prognostic foe to a predictive friend. Curr Opin Obstet Gynecol. 2007;19:56–62
  2. Morris SR, Carey LA. Trastuzumab and beyond: new possibilities for the treatment of HER2-positive breast cancer. Oncology (Huntingt). 2006;20:1763–1771
  3. Nahta R, Esteva FJ. Trastuzumab: triumphs and tribulations. Oncogene. 2007;26:3637–3643
  4. Carter P, Presta L, Gorman CM, Ridgway JB, Henner D, Wong WL, et al. Humanization of an anti-p185HER2 antibody for human cancer therapy. Proc Natl Acad Sci USA. 1992;89:4285–4289
  5. Hudis CA. Trastuzumab—mechanism of action and use in clinical practice. N Engl J Med. 2007;357:39–51
  6. Torigian DA, Huang SS, Houseni M, Alavi A. Functional imaging of cancer with emphasis on molecular techniques. CA Cancer J Clin. 2007;57:206–224
  7. da Silva FA, Corte-Real S, Goncalves J. Recombinant antibodies as therapeutic agents — Pathways for modeling new biodrugs. Biodrugs. 2008;22:301–314
  8. Demarest SJ, Glaser SM. Antibody therapeutics, antibody engineering, and the merits of protein stability. Curr Opin Drug Discov Dev. 2008;11:675–687
  9. Hu S, Shively L, Raubitschek A, Sherman M, Williams LE, Wong JY, et al. Minibody: a novel engineered anti-carcinoembryonic antigen antibody fragment (single-chain Fv-CH3) which exhibits rapid, high-level targeting of xenografts. Cancer Res. 1996;56:3055–3061
  10. Yazaki PJ, Wu AM, Tsai SW, Williams LE, Ikler DN, Wong JY, et al. Tumor targeting of radiometal labeled anti-CEA recombinant T84.66 diabody and t84.66 minibody: comparison to radioiodinated fragments. Bioconjug Chem. 2001;12:220–228
  11. Olafsen T, Kenanova VE, Sundaresan G, Anderson AL, Crow D, Yazaki PJ, et al. Optimizing radiolabeled engineered anti-p185HER2 antibody fragments for in vivo imaging. Cancer Res. 2005;65:5907–5916
  12. Kenanova V, Olafsen T, Crow DM, Sundaresan G, Subbarayan M, Carter NH, et al. Tailoring the pharmacokinetics and positron emission tomography imaging properties of anti-carcinoembryonic antigen single-chain Fv-Fc antibody fragments. Cancer Res. 2005;65:622–631
  13. Brambell FW. The transmission of immunity from mother to young and the catabolism of immunoglobulins. Lancet. 1966;2:1087–1093
  14. Junghans RP, Anderson CL. The protection receptor for IgG catabolism is the β2-microglobulin-containing neonatal intestinal transport receptor. Proc Natl Acad Sci USA. 1996;93:5512–5516
  15. Kim JK, Firan M, Radu CG, Kim CH, Ghetie V, Ward ES. Mapping the site on human IgG for binding of the MHC class I-related receptor, FcRn. Eur J Immunol. 1999;29:2819–2825
  16. Austin CD, Wen X, Gazzard L, Nelson C, Scheller RH, Scales SJ. Oxidizing potential of endosomes and lysosomes limits intracellular cleavage of disulfide-based antibody-drug conjugates. Proc Natl Acad Sci USA. 2005;102:17987–17992
  17. Mittendorf EA, Storrer CE, Shriver CD, Ponniah S, Peoples GE. Investigating the combination of trastuzumab and HER2/neu peptide vaccines for the treatment of breast cancer. Ann Surg Oncol. 2006;13:1085–1098
  18. 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
  19. Borchardt PE, Yuan RR, Miederer M, McDevitt MR, Scheinberg DA. Targeted actinium-225 in vivo generators for therapy of ovarian cancer. Cancer Res. 2003;63:5084–5090
  20. Kobayashi H, Shirakawa K, Kawamoto S, Saga T, Sato N, Hiraga A, et al. Rapid accumulation and internalization of radiolabeled Herceptin in an inflammatory breast cancer xenograft with vasculogenic mimicry predicted by the contrast-enhanced dynamic MRI with the macromolecular contrast agent G6-(1B4M-Gd)(256). Cancer Res. 2002;62:860–866
  21. Costantini DL, Chan C, Cai Z, Vallis KA, Reilly RM. 111In-Labeled trastuzumab (Herceptin) modified with nuclear localization sequences (NLS): an Auger electron-emitting radiotherapeutic agent for HER2/neu-amplified breast cancer. J Nucl Med. 2007;48:1357–1368
  22. Olafsen T, Cheung CW, Yazaki PJ, Li L, Sundaresan G, Gambhir SS, et al. Covalent disulfide-linked anti-CEA diabody allows site-specific conjugation and radiolabeling for tumor targeting applications. Protein Eng Des Sel. 2004;17:21–27
  23. Govindan SV, Griffiths GL, Stein R, Andrews P, Sharkey RM, Hansen HJ, et al. Clinical-scale radiolabeling of a humanized anticarcinoembryonic antigen monoclonal antibody, hMN-14, with residualizing 131I for use in radioimmunotherapy. J Nucl Med. 2005;46:153–159
  24. Stein R, Govindan SV, Hayes M, Griffiths GL, Hansen HJ, Horak ID, et al. Advantage of a residualizing iodine radiolabel in the therapy of a colon cancer xenograft targeted with an anticarcinoembryonic antigen monoclonal antibody. Clin Cancer Res. 2005;11:2727–2734
  25. Vaidyanathan G, Affleck DJ, Bigner DD, Zalutsky MR. Improved xenograft targeting of tumor-specific anti-epidermal growth factor receptor variant III antibody labeled using N-succinimidyl 4-guanidinomethyl-3-iodobenzoate. Nucl Med Biol. 2002;29:1–11
  26. 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
  27. Vaidyanathan G, Alston KL, Bigner DD, Zalutsky MR. Nɛ-(3-[*I]Iodobenzoyl)-Lys5-Nα-maleimido-Gly1-GEEEK ([*I]IB-Mal-d-GEEEK): a radioiodinated prosthetic group containing negatively charged d-glutamates for labeling internalizing monoclonal antibodies. Bioconjug Chem. 2006;17:1085–1092
  28. Vaidyanathan G, Zalutsky MR. Synthesis of N-succinimidyl 4-guanidinomethyl-3-[*I]iodobenzoate: a radio-iodination agent for labeling internalizing proteins and peptides. Nat Protoc. 2007;2:282–286
  29. Benz CC, Scott GK, Sarup JC, Johnson RM, Tripathy D, Coronado E, et al. Estrogen-dependent, tamoxifen-resistant tumorigenic growth of MCF-7 cells transfected with HER2/neu. Breast Cancer Res Treat. 1992;24:85–95
  30. Vaidyanathan G, Affleck DJ, Li J, Welsh P, Zalutsky MR. A polar substituent-containing acylation agent for the radioiodination of internalizing monoclonal antibodies: N-succinimidyl 4-guanidinomethyl-3-[131I]iodobenzoate ([131I]SGMIB). Bioconjug Chem. 2001;12:428–438
  31. Brooks SC, Hansen ER, Saunders DE, Battelli MG, Shafie SM. Effect of growth on the estrogen receptor levels in MCF-7 cells. Cancer Res. 1984;44:3724–3729
  32. DeNardo GL, DeNardo SJ, Peterson JJ, Miers LA, Lam KS, Hartmann-Siantar C, et al. Preclinical evaluation of cathepsin-degradable peptide linkers for radioimmunoconjugates. Clin Cancer Res. 2003;9:3865S–3872S
  33. DeNardo GL, Kukis DL, Shen S, DeNardo DA, Meares CF, DeNardo SJ. 67Cu-versus 131I-labeled Lym-1 antibody: comparative pharmacokinetics and dosimetry in patients with non-Hodgkin's lymphoma. Clin Cancer Res. 1999;5:533–541
  34. Kukis DL, DeNardo GL, DeNardo SJ, Mirick GR, Miers LA, Greiner DP, et al. Effect of the extent of chelate substitution on the immunoreactivity and biodistribution of 2IT-BAT-Lym-1 immunoconjugates. Cancer Res. 1995;55:878–884
  35. Lewis MR, Boswell CA, Laforest R, Buettner TL, Ye D, Connett JM, et al. Conjugation of monoclonal antibodies with TETA using activated esters: biological comparison of 64Cu-TETA-1A3 with 64Cu-BAT-2IT-1A3. Cancer Biother Radiopharm. 2001;16:483–494
  36. Foulon CF, Reist CJ, Bigner DD, Zalutsky MR. Radioiodination via d-amino acid peptide enhances cellular retention and tumor xenograft targeting of an internalizing anti-epidermal growth factor receptor variant III monoclonal antibody. Cancer Res. 2000;60:4453–4460
  37. Maack T, Park CH, Camargo MJ. Filtration, transport, and metabolism of proteins. In:  Seldin DW,  Giebisch G editor. Physiology and Pathophysiology. New York: Raven Press; 1992;p. 3005–3038
  38. Miao Y, Fisher DR, Quinn TP. Reducing renal uptake of 90Y- and 177Lu-labeled α-melanocyte stimulating hormone peptide analogues. Nucl Med Biol. 2006;33:723–733
  39. Dijkgraaf I, Liu S, Kruijtzer JA, Soede AC, Oyen WJ, Liskamp RM, et al. Effects of linker variation on the in vitro and in vivo characteristics of an 111In-labeled RGD peptide. Nucl Med Biol. 2007;34:29–35
  40. von Guggenberg E, Behe M, Behr TM, Saurer M, Seppi T, Decristoforo C. 99mTc-labeling and in vitro and in vivo evaluation of HYNIC- and (N-His)acetic acid-modified [d-Glu1]-minigastrin. Bioconjug Chem. 2004;15:864–871
  41. Wen X, Jackson EF, Price RE, Kim EE, Wu Q, Wallace S, et al. Synthesis and characterization of poly(l-glutamic acid) gadolinium chelate: a new biodegradable MRI contrast agent. Bioconjug Chem. 2004;15:1408–1415
  42. Behe M, Kluge G, Becker W, Gotthardt M, Behr TM. Use of polyglutamic acids to reduce uptake of radiometal-labeled minigastrin in the kidneys. J Nucl Med. 2005;46:1012–1015
  43. Gotthardt M, van Eerd-Vismale J, Oyen WJ, de Jong M, Zhang H, Rolleman E, et al. Indication for different mechanisms of kidney uptake of radiolabeled peptides. J Nucl Med. 2007;48:596–601
  44. Rexhepaj R, Grahammer F, Volkl H, Remy C, Wagner CA, Sandulache D, et al. Reduced intestinal and renal amino acid transport in PDK1 hypomorphic mice. FASEB J. 2006;20:2214–2222
  45. Verrey F, Ristic Z, Romeo E, Ramadan T, Makrides V, Dave MH, et al. Novel renal amino acid transporters. Annu Rev Physiol. 2005;67:557–572
  46. Kenanova V, Olafsen T, Williams LE, Ruel NH, Longmate J, Yazaki PJ, et al. Radioiodinated versus radiometal-labeled anti-carcinoembryonic antigen single-chain Fv-Fc antibody fragments: optimal pharmacokinetics for therapy. Cancer Res. 2007;67:718–726

 This work was supported by Grants CA42324, CA14236, CA43904 and CA86306 from the National Institutes of Health.

PII: S0969-8051(09)00089-4

doi: 10.1016/j.nucmedbio.2009.04.002

Nuclear Medicine and Biology
Volume 36, Issue 6 , Pages 671-680 , August 2009