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Approaches to Radiolabeling of Antibodies for Diagnosis and Therapy of Cancer

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The development of monoclonal antibodies of high affinity and selectivity for tumor antigens has supported the development of radiolabeled antibodies for diagnostic localization and targeted delivery of therapeutic radionuclides. Several radionuclide chelating agent systems have been developed for indium-111 and technetium-99m that have shown good sensitivity and specificity for tumor detection in patients. Feasibility for therapy has been shown in animal models and a few patient studies with iodine-131 and yttrium-90. This review covers selection of radionuclides and chemistry of antibody radiolabeling.

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REFERENCES

  1. G. Kohler and C. Milstein. Nature 256:495–497 (1975).

    Google Scholar 

  2. F. Otsuka and M. J. Welch. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 14:243–249 (1987).

    Google Scholar 

  3. D. E. Troutner. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 14:171–176 (1987).

    Google Scholar 

  4. W. C. Eckelman and C. H. Paik. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B. 14:335–343 (1986).

    Google Scholar 

  5. L. W. Brady, D. V. Woo, N. D. Heindel, A. M. Markoe, and H. Koprowski. Int. J. Radiat. Oncol. Biol. Phys. 13:1535–1544 (1987).

    Google Scholar 

  6. S. M. Larsen, J. A. Carrasquillo, and J. C. Reynolds. Cancer Invest. 2:363–381 (1984).

    Google Scholar 

  7. R. H. J. Begent. Biochim. Biophys. Acta 780:151–166 (1985).

    Google Scholar 

  8. P. G. Abrams, J. A. Carrasquillo, R. W. Schroff, J. F. Eary, A. R. Fritzberg, A. C. Morgan, D. S. Wilbur, P. L. Beaumier, S. M. Larson, and W. B. Nelp. In R. K. Oldham (ed.), Principles of Cancer Biotherapy, Raven Press, New York, 1987, pp. 337–354.

    Google Scholar 

  9. K. E. Britton and M. Granowska. Cancer Surveys 6:247–267 (1987).

    Google Scholar 

  10. S. D. Rockoff, D. J. Goodenough, and K. R. McIntire. Cancer Res. 40:3054–3058 (1980).

    Google Scholar 

  11. G. L. Buraggi, A. Turrin, N. Cascinelli, A. Attili, G. Terno, E. Bombardieri, M. Gasparini, and E. Seregni. In L. Donatto and K. Britton (eds.), Immunoscintigraphy, Gordon and Breach, New York, 1984, pp. 215–245.

    Google Scholar 

  12. J. Eary, R. Schroff, P. Abrams, S. Kasina, A. Srinivasan, J. Reno, C. Woodhouse, and W. Nelp. J. Nucl. Med. 28:650–651 (1987) (abstr.).

    Google Scholar 

  13. L. A. Osterman. In Methods of Protein and Nucleic Acid Research, Springer-Verlag, New York, 1984, Chap. 3, pp. 131–143.

    Google Scholar 

  14. R. H. Seevers and R. E. Counsell. Chem. Rev. 82:575–590 (1982).

    Google Scholar 

  15. D. Engler and A. G. Burger. Endocrine Rev. 5:151–184 (1984).

    Google Scholar 

  16. D. S. Wilbur, D. S. Jones, A. R. Fritzberg, and A. C. Morgan. J. Nucl. Med. 27:959 (1986).

    Google Scholar 

  17. M. R. Zalutsky and A. S. Narula. Appl. Radiat. Isot. 38:1051–1055 (1987).

    Google Scholar 

  18. L. Knight, K. A. Krohn, M. J. Welch, B. Spomer, and J. P. Hagar. In B. A. Rhodes (ed.), Radiopharmaceuticals, Society of Nuclear Medicine, New York, 1975, pp. 149–154.

    Google Scholar 

  19. K. D. McElvany, J. W. Barnes, and M. J. Welch. Int. J. Appl. Radiat. Isot. 31:679–688 (1980).

    Google Scholar 

  20. K. D. McElvany and M. J. Welch. J. Nucl. Med. 21:953–960 (1980).

    Google Scholar 

  21. M. R. Kilbourn, C. S. Dence, M. J. Welch, and C. J. Mathias. J. Nucl. Med. 28:462–470 (1987).

    Google Scholar 

  22. E. Krejcarek and K. L. Tucker. Biochem. Biophys. Res. Commun. 77:581–585 (1977).

    Google Scholar 

  23. A. Scheinberg, M. Strand, and O. A. Gansow. Science 215:1511–1513 (1982).

    Google Scholar 

  24. W. W. Layne, D. J. Hnatowich, P. W. Doherty, R. L. Childs, D. Lanteigne, and J. Ansell. J. Nucl. Med. 23:627–630 (1982).

    Google Scholar 

  25. D. J. Hnatowich, W. W. Layne, and R. L. Childs. Int. J. Appl. Radiat. Isot. 33:327–332 (1982).

    Google Scholar 

  26. C. H. Paik, M. A. Ebbert, P. R. Murphy, C. R. Lassman, R. C. Reba, W. C. Eckelman, K. Y. Pak, J. Powe, Z. Steplewski, and H. Koprowski. J. Nucl. Med. 24:1158–1163 (1983).

    Google Scholar 

  27. D. J. Hnatowich, W. W. Layne, R. L. Childs, D. Lanteigne, M. A. Davis, T. W. Griffin, and P. W. Doherty. Science 220:613–615 (1983).

    Google Scholar 

  28. D. J. Hnatowich, R. L. Childs, D. Lanteigne, and A. Najafi. J. Immunol. Meth. 35:554–557 (1984).

    Google Scholar 

  29. C. H. Paik, P. R. Murphy, W. C. Eckelman, W. A. Volkert, and R. C. Reba. J. Nucl. Med. 24:932–936 (1983).

    Google Scholar 

  30. R. G. Buckley and F. Searles. FEBS Lett. 166:202–204 (1984).

    Google Scholar 

  31. R. J. Paxton, J. G. Jakowatz, J. D. Beatty, B. G. Beatty, W. G. Vlahos, L. E. Williams, B. R. Clark, and J. G. Shively. Cancer Res. 45:5694–5699 (1985).

    Google Scholar 

  32. A. Najafi, R. L. Childs, and D. J. Hnatowich. Int. J. Appl. Radiat. Isot. 35:554–557 (1984).

    Google Scholar 

  33. J. M. Estaban, J. Schlom, O. A. Gansow, R. W. Atcher, M. W. Brechbiel, D. E. Simpson, and D. Colcher. J. Nucl. Med. 28:861–870 (1987).

    Google Scholar 

  34. M. W. Brechbiel, O. A. Gansow, R. W. Atcher, J. Schlom, J. Esteban, D. E. Simpson, and D. Colcher. Inorg. Chem. 25:2773–2781 (1986).

    Google Scholar 

  35. M. W. Sundberg, C. F. Meares, D. A. Goodwin, and C. I. Diamanti. J. Med. Chem. 17:1304–1307 (1974).

    Google Scholar 

  36. C. F. Meares, D. A. Goodwin, C. S.-H. Leung, A. Y. Girgis, D. J. Silvester, A. D. Nunn, and P. J. Lavender. Proc. Natl. Acad. Sci. USA 73:3803–3806 (1976).

    Google Scholar 

  37. C. S.-H. Leung, C. F. Meares, and D. A. Goodwin. Int. J. Appl. Radiat. Isot. 29:687–692 (1978).

    Google Scholar 

  38. C. F. Meares, M. J. McCall, D. T. Reardon, D. A. Goodwin, C. I. Diamanti, and M. McTigue. Anal. Biochem. 142:68–78 (1984).

    Google Scholar 

  39. J. D. Rodwell, V. L. Alvarez, C. Lee, A. D. Lopes, J. W. F. Goers, H. D. King, H. J. Powsner, and T. J. McKearn. Proc. Natl. Acad. Sci. USA 83:2632–2636 (1986).

    Google Scholar 

  40. M. K. Haseman, D. A. Goodwin, C. F. Meares, M. S. Kaminski, T. G. Wensel, J. J. McCall, and R. Levy. Eur. J. Nucl. Med. 12:455–460 (1986).

    Google Scholar 

  41. S. M. Quadri, C. K. Paik, K. Yokoyama, and R. C. Reba. J. Nucl. Med. 27:959 (1986) (abstr).

    Google Scholar 

  42. K. Yokoyama, C. H. Paik, S. M. Quadri, J. C. Reynolds, C. Y. Mui, S. Y. Shin, P. J. Maloney, S. M. Larson, and R. C. Reba. J. Nucl. Med. 28:572 (1987) (abstr.).

    Google Scholar 

  43. C. H. Paik, S. M. Quadri, and R. C. Reba. J. Nucl. Med. 28:572 (1987) (abstr.).

    Google Scholar 

  44. W. T. Anderson and M. Strand. Cancer Res. 45:2154–2158 (1985).

    Google Scholar 

  45. A. Yokoyama, Y. Ohmomo, K. Horiuchi, H. Saji, H. Tanaka, K. Yamamoto, Y. Ishii, and K. Torizuka. J. Nucl. Med. 23:909–914 (1982).

    Google Scholar 

  46. G. A. Janoki, J. F. Harwig, W. Chanachai, and W. Wolf. Int. J. Appl. Radiat. Isot. 34:871–877 (1983).

    Google Scholar 

  47. M. C. Ward, K. R. Roberts, J. W. Babich, M. A. Bukhari, G. Cohlan, J. H. Westwood, V. R. McCready, and R. J. Ott. Nucl. Med. Biol. Int. J. Appl. Radiat. Instrum. Part B 13:505–507 (1986).

    Google Scholar 

  48. W. A. Pettit, F. H. Deland, S. J. Bennett, and D. M. Goldenberg. J. Nucl. Med. 21:59–62 (1980).

    Google Scholar 

  49. C. H. Paik, W. C. Eckelman, and R. C. Reba. Nucl. Med. Biol. Int. J. Appl. Radiat. Instrum. Part B 13:359–362 (1986).

    Google Scholar 

  50. B. A. Rhodes, P. O. Zamora, K. D. Newell, and E. F. Valdez. J. Nucl. Med. 27:685–693 (1986).

    Google Scholar 

  51. S. W. Burchiel, R. Knight, J. H. Christie, R. R. Pollock, and M. D. Scharff. J. Nucl. Med. 26:112 (1985) (abstr.).

    Google Scholar 

  52. E. Sundrehagen. Eur. J. Nucl. Med. 7:549–552 (1982).

    Google Scholar 

  53. J. Kanellos, G. A. Pietersz, I. F. C. McKenzie, J. Bonnyman, and J. Baldas. J. Natl. Cancer Inst. 77:431–439 (1986).

    Google Scholar 

  54. B. A. Khaw, W. Strauss, A. Carvalho, E. Locke, H. Gold, and E. Haber. J. Nucl. Med. 23:1011–1019 (1982).

    Google Scholar 

  55. R. L. Childs and D. J. Hnatowich. J. Nucl. Med. 26:293–299 (1985).

    Google Scholar 

  56. Y. Arano, A. Yokoyama, T. Furukawa, K. Horiuchi, M. Koizumi, K. Endo, and K. Torizuka. J. Nucl. Med. 28:1027–1033 (1987).

    Google Scholar 

  57. G. L. Tolman, R. J. Hadjian, M. M. Morelock, P. L. Jones, W. Neacy, F. A. Liberatore, H. Sands, and B. Gallagher. J. Nucl. Med. 25:24 (1984) (abstr.).

    Google Scholar 

  58. S. W. Burchiel, R. A. Hadjian, W. B. Hladik, S. N. Gregorio, G. L. Tolman, C. A. Drozynski, D. Covell, P. A. Day, J. H. Christie, and B. M. Gallagher. J. Nucl. Med. 27:896 (1986) (abstr.).

    Google Scholar 

  59. A. R. Fritzberg. Nukl. Med. 26:7–12 (1987).

    Google Scholar 

  60. A. R. Fritzberg, P. G. Abrams, P. L. Beaumier, S. Kasina, A. C. Morgan, T. N. Rao, J. M. Reno, J. A. Sanderson, A. Srinivasan, D. S. Wilbur, and J.-L. Vanderheyden. Proc. Natl. Acad. Sci. 85 (June 1988).

  61. W. F. Bale and I. L. Spar. Adv. Biol. Med. Phys. 5:285–356 (1957).

    Google Scholar 

  62. D. E. Troutner. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 14:171–176 (1987).

    Google Scholar 

  63. B. W. Wessels and R. D. Rogus. Med. Phys. 11:638–645 (1984).

    Google Scholar 

  64. J. A. Jungerman, K.-H. P. Yu, and C. Zanelli. Int. J. Appl. Radiat. Isot. 35:883–888 (1984).

    Google Scholar 

  65. S. J. Adelstein and A. I. Kassis. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 14:165–169 (1987).

    Google Scholar 

  66. J. L. Humm. J. Nucl. Med. 27:1490–1497 (1986).

    Google Scholar 

  67. D. J. Hnatowich, F. Virzi, and P. W. Doherty. J. Nucl. Med. 26:503–509 (1985).

    Google Scholar 

  68. A. T. M. Vaughan, A. Keeling, and S. C. S. Yankuba. Int. J. Appl. Radiat. Isot. 36:803–806 (1985).

    Google Scholar 

  69. L. C. Washburn, T. T. Hwa Sun, J. E. Crook, B. L. Byrd, J. E. Carlton, X.-W. Hung, and S. Steplewski. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 13:453–456 (1986).

    Google Scholar 

  70. W. T. Andersen-Berg, R. A. Squire, and M. Strand. Cancer Res. 47:1905–1912 (1987).

    Google Scholar 

  71. J.-L. Vanderheyden, A. R. Fritzberg, T. N. Rao, S. Kasina, A. Srinivasan, J. M. Reno, and A. C. Morgan. J. Nucl. Med. 28:656 (1987) (abstr.).

    Google Scholar 

  72. W. C. Cole, S. J. DeNardo, C. F. Meares, M. J. McCall, G. DeNardo, A. L. Epstein, H. A. O'Brien, and M. K. Moi. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 14:363–368 (1986).

    Google Scholar 

  73. M. K. Moi, C. F. Meares, M. J. McCall, W. C. Cole, and S. J. DeNardo. Anal. Biochem. 148:249–253 (1985).

    Google Scholar 

  74. W. C. Cole, S. J. DeNardo, C. F. Meares, M. J. McCall, G. L. DeNardo, A. L. Epstein, H. A. O'Brien, and M. K. Moi. J. Nucl. Med. 28:83–90 (1983).

    Google Scholar 

  75. J. Franz, G. M. Freeman, E. K. Barefield, W. A. Volkert, G. J. Ehrhardt, and R. A. Holmes. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 14:479–484 (1987).

    Google Scholar 

  76. J. A. Mercer-Smith, S. D. Figard, D. K. LaVallee, and Z. V. Svitra. J. Nucl. Med. 26:437 (1985) (abstr.).

    Google Scholar 

  77. R. A. Fawwaz, T. S. T. Wang, S. C. Srivastava, J. M. Rosen, S. Ferrone, M. A. Hardy, and P. O. Alderson. J. Nucl. Med. 25:796–799 (1984).

    Google Scholar 

  78. F.-M. Chen and C. E. Troutner. Nucl. Med. Biol. Int. J. Radiat. Appl. Instrum. Part B 13:369–372 (1986).

    Google Scholar 

  79. O. A. Gansow, R. W. Atcher, D. C. Link, A. M. Friedman, R. H. Seevers, W. Anderson, D. A. Scheinberg, and M. Strand. Am. Chem. Soc. Symp. Ser. 241:215–227 (1984).

    Google Scholar 

  80. R. W. Kozak, R. W. Atcher, O. A. Gansow, A. M. Friedman, J. J. Hines, and T. A. Waldmann. Proc. Natl. Acad. Sci. 83:474–478 (1986).

    Google Scholar 

  81. F. P. Stuart, G. Perdrizet, B. Steranka, M. Buckingham, D. Lopes, V. Alvarez, J. Rodwell, T. McKearn, J. Hines, R. Atcher, and A. M. Friedman. Transplant. Proc. XIX:605–606 (1987).

    Google Scholar 

  82. J. D. Rodwell, V. L. Alvarez, C. Lee, A. D. Lopes, J. W. F. Goers, H. D. King, H. J. Powsner, and T. J. McKearn. Proc. Natl. Acad. Sci. 83:2632–2636 (1986).

    Google Scholar 

  83. G. W. M. Visser, E. L. Diemer, and F. M. Kaspersen. Int. J. Appl. Radiat. Isot. 32:905–912 (1981).

    Google Scholar 

  84. A. M. Friedman, M. R. Zalutsky, W. Wung, F. Buckingham, P. V. Harper, G. H. Scherr, B. Wainer, R. L. Hunter, E. H. Appleman, R. M. Rothberg, F. W. Fitch, F. P. Stuart, and J. J. Simonian. Inst. J. Nucl. Med. Biol. 4:219–224 (1977).

    Google Scholar 

  85. C. C. Badger, K. A. Krohn, A. V. Peterson, H. Shulman, and I. D. Bernstein. Cancer Res. 45:1536–1544 (1985).

    Google Scholar 

  86. N.-K. V. Cheung, B. Landmeier, J. Neely, A. D. Nelsen, C. Abramowsky, S. Ellery, R. B. Adams, and F. Miraldi. J. Natl. Cancer Inst. 77:739–745 (1986).

    Google Scholar 

  87. S. E. Order, G. B. Stillwagon, J. L. Klein, P. K. Leichner, S. S. Siegelman, E. K. Fishman, D. S. Ettinger, T. Haulk, K. Kopher, K. Finney, M. Surdyke, S. Self, and S. Leibel. J. Clin. Oncol. 3:1573–1582 (1985).

    Google Scholar 

  88. S. E. Order, J. L. Klein, P. K. Leichner, J. Frincke, C. Lollo, and D. J. Carlo. Int. J. Radiat. Oncol. Biol. Phys. 12:277–281 (1986).

    Google Scholar 

  89. Hammersmith Oncology Group. Lancet 1:1441–1443 (1984).

    Google Scholar 

  90. D. Pectasides, S. Stewart, N. Courtenay-Luck, R. Rampling, A. J. Munro, T. Krausz, B. Dhokia, D. Snook, G. Hooker, H. Durbin, J. Taylor-Papadimitriou, and A. A. Epenetos. Br. J. Cancer 53:727–732 (1986).

    Google Scholar 

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Fritzberg, A.R., Berninger, R.W., Hadley, S.W. et al. Approaches to Radiolabeling of Antibodies for Diagnosis and Therapy of Cancer. Pharm Res 5, 325–334 (1988). https://doi.org/10.1023/A:1015995208444

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