Humanization of an anti-vascular endothelial growth factor monoclonal antibody for the therapy of solid tumors and other disorders

Cancer Research

Volumn 57, Issue 20, 1997, Pages 4593-4599

  Presta, Leonard G ^a   Chen, Helen ^a   O'Connor, Shane J ^a   Chisholm, Vanessa ^a   Meng, Y Gloria ^a   Krummen, Lynne ^a   Winkler, Marjorie ^a   Ferrara, Napoleone ^a  

^a GENENTECH INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

MONOCLONAL ANTIBODY; VASCULOTROPIN;

ANGIOGENESIS; ANIMAL CELL; ARTICLE; CELL PROLIFERATION; DRUG EFFICACY; DRUG POTENCY; ENDOTHELIUM CELL; HUMAN; HUMAN CELL; NEOVASCULARIZATION (PATHOLOGY); NONHUMAN; PRIORITY JOURNAL; RETINA ISCHEMIA; SITE DIRECTED MUTAGENESIS; SOLID TUMOR;

ADRENAL CORTEX; AMINO ACID SEQUENCE; ANIMALS; ANTIBODIES, MONOCLONAL; CAPILLARIES; CATTLE; CELLS, CULTURED; CLONING, MOLECULAR; CONSENSUS SEQUENCE; ENDOTHELIAL GROWTH FACTORS; ENDOTHELIUM, VASCULAR; FEMALE; HUMANS; IMMUNOGLOBULIN FAB FRAGMENTS; IMMUNOGLOBULIN G; IMMUNOGLOBULIN HEAVY CHAINS; IMMUNOGLOBULIN LIGHT CHAINS; IMMUNOGLOBULIN VARIABLE REGION; LYMPHOKINES; MICE; MICE, NUDE; MODELS, STRUCTURAL; MOLECULAR SEQUENCE DATA; NEOVASCULARIZATION, PATHOLOGIC; PROTEIN CONFORMATION; RATS; RECOMBINANT FUSION PROTEINS; RHABDOMYOSARCOMA; SEQUENCE ALIGNMENT; TRANSPLANTATION, HETEROLOGOUS; TUMOR CELLS, CULTURED; VASCULAR ENDOTHELIAL GROWTH FACTOR A; VASCULAR ENDOTHELIAL GROWTH FACTORS;

EID: 0030856731     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (53)

1. Folkman, J., and Shing, Y. Angiogenesis. J. Biol. Chem., 267, 10931-10934, 1992.
2. Klagsbrun, M., and D'Amore, P. A. Regulators of angiogenesis. Annu. Rev. Physiol., 53: 217-239, 1991.
3. Gamer, A. Vascular diseases. In: A. Garner and G. K. Klintwonh (eds.), Pathobiology of Ocular Disease. A Dynamic Approach, Ed. 2, pp. 1625-1710. New York: Marcel Dekker, 1994.
4. Weidner, N., Semple, P., Welch, W., and Folkman, J. Tumor angiogenesis and metastasis. Correlation in invasive breast carcinoma. N. Engl. J. Med., 324: 1-6. 1991.
5. Horak, E. R., Leek, R., Klenk, N., Lejeune, S., Smith, K., Stuart, M., Greenall, M., and Harris, A. Quantitative angiogenesis assessed by anti-PECAM antibodies: correlation with node metastasis and survival in breast cancer. Lancet, 340: 1120-1124, 1992.
6. Macchiarini, P., Fontanini, G., Hardin, M. J., Squartini, F., and Angeletti, C. A. Relation of neovascularization to metastasis of non-small cell lung carcinoma. Lancet, 340: 145-146, 1992.
7. Good, D., Polverini, P., Rastinejad, F., Beau, M., Lemons, R., Frazier, W., and Bouck, N. A tumor suppressor-dependent inhibitor of angiogenesis is immunologically and functionally indistinguishable from a fragment of thrombospondin. Proc. Natl. Acad. Sci. USA, 87: 6624-6628, 1990.
8. Clapp, C., Martial, J. A., Guzman, R. C., Rentier-Delrue, F., and Weiner, R. I. The 16-kilodalton N-terminal fragment of human prolactin is a potent inhibitor of angiogenesis. Endocrinology, 133: 1292-1299, 1993.
9. O'Reilly, M. S., Holmgren, L., Shing, Y., Chen, C. Rosenthal, R. A., Mosem, M., Lane, W. S., Cao, Y., Sage, E. H., and Folkman, J. Angiostatin. A novel angiogenesis inhibitor that mediates the suppression of metastasis by a Lewis lung carcinoma. Cell, 79: 315-328, 1994.
10. O'Reilly, M. S., Boehm, T., Shing, Y., Fukai, N., Vasios, G., Lane, W. S., Flynn, E., Birkhead, J. R., Olsen, B. R., and Folkman, J. Endostatin. An endogenous inhibitor of angiogenesis and tumor growth. Cell, 88: 277-285, 1996.
11. Ferrara, N., and Davis Smyth, T. The biology of vascular endothelial growth factor. Endocr. Rev., 18: 4-25, 1997.
12. Berkman, R. A., Merrill, M. J., Reinhold, W. C., Monacci, W. T., Saxena, A., Clark, W. C., Robertson, J. T., Ali, I. U., and Oldfield, E. H. Expression of the vascular permeability/vascular endothelial growth factor gene in central nervous system neoplasms. J. Clin. Invest., 91: 153-159, 1993.
13. Brown, L. F., Berse, B., Jackman, R. W., Guidi, A. J., Dvorak, H. F., Senger, D. R., Connolly, J. L., and Schnitt, S. J. Expression of vascular permeability factor (vascular endothelial growth factor) and its receptors in breast cancer. Hum. Pathol., 26: 86-91, 1995.
14. Brown, L. F., Berse, B., Jackman, R. W., Tognazzi, K., Manseau, E. J., Senger, D. R., and Dvorak, H. F. Expression of vascular permeability factor (vascular endothelial growth factor) and its receptors in adenocarcinomas of the gastrointestinal tract. Cancer Res., 53: 4727-4735, 1993.
15. Mattern, J., Koomagi, R., and Volm, M. Association of vascular endothelial growth factor expression with intratumoral microvessel density and tumour cell proliferation in human epidermoid lung carcinoma. Br. J. Cancer, 73: 931-934, 1996.
16. Dvorak, H. F., Brown, L. F., Detmar, M., and Dvorak, A. M. Vascular permeability factor/vascular endothelial growth factor, microvascular permeability and angiogenesis. Am. J. Pathol., 146: 1029-1039, 1995.
17. Aiello, L. P., Avery, R., Arrigg, R., Keyt, B., Jampel, H., Shah, S., Pasquale, L., Thieme, H., Iwamoto, M., Park, J. E., Nguyen, H., Aiello, L. M., Ferrara, N., and King, G. L. Vascular endothelial growth factor in ocular fluid of patients with diabetic retinopathy and other retinal disorders. N. Engl. J. Med., 331: 1480-1487, 1994.
18. Lopez, P. F., Sippy, B. D., Lambert, H. M., Thach, A. B., and Hinton, D. R. Transdifferentiated retinal pigment epithelial cells are immunoreactive for vascular endothelial growth factor in surgically excised age-related macular degeneration-related choroidal neovascular membranes. Invest. Ophthalmol. Visual Sci., 37: 855-868, 1996.
19. Kim, K. J., Li, B., Houck, K., Winer, J., and Ferrara, N. The vascular endothelial growth factor proteins: identification of biologically relevant regions by neutralizing monoclonal antibodies. Growth Factors, 7: 53-64, 1992.
20. Kim, K. J., Li, B., Winer, J., Armanini, M., Gillett, N., Phillips, H. S., and Ferrara, N. Inhibition of vascular endothelial growth factor-induced angiogenesis suppresses tumour growth in vivo. Nature (Lond.), 362: 841-844, 1993.
21. Warren, R. S., Yuan, H., Matli, M. R., Gillett, N. A., and Ferrara, N. Regulation by vascular endothelial growth factor of human colon cancer tumorigenesis in a mouse model of experimental liver metastasis. J. Clin. Invest., 95: 1789-1797, 1995.
22. Borgström, P., Hillan, K. J., Sriramarao, P., and Ferrara, N. Complete inhibition of angiogenesis and growth of microtumors by anti-vascular endothelial growth factor neutralizing antibodies. Novel concepts of angiostatic therapy from intravital video-microscopy. Cancer Res., 56: 4032-4039, 1996.
23. Melnyk, O., Schuman, M. A., and Kim, K. J. Vascular endothelial growth factor promotes tumor dissemination by a mechanism distinct from its effect on primary tumor growth. Cancer Res., 56: 921-924, 1996.
24. Adamis, A. P., Shima, D. T., Tolentino, M., Gragoudas, E., Ferrara, N., Folkman, J., D'Amore, P. A., and Miller, J. W. Inhibition of VEGF prevents retinal ischemia-associated iris neovascularization in a primate. Arch. Ophthalmol., 114: 66-71, 1996.
25. Miller, R. A., Oseroff, A. R., Stratte, P. T., and Levy, R. Monoclonal antibody therapeutic trials in seven patients with T-cell lymphoma. Blood, 62: 988-995, 1983.
26. Schroff, R. W., Foon, K. A., Beatty, S. M., Odham, R. K., and Morgan, A. C., Jr. Human anti-murine immunoglobulin response in patients receiving monoclonal antibody therapy. Cancer Res., 45: 879-885, 1985.
27. Neuberger, M. S., Williams, G. T., Mitchell, E. B., Jouhal, S. S., Flanagan, J. G., and Rabbits, T. H. A hapten-specific chimaeric IgE antibody with human physiological effector function. Nature (Lond.), 314: 268-270, 1985.
28. Jones, P. T., Dear, P. H., Foote, J., Neuberger, M. S., and Winter, G. Replacing the complementarity-determining regions in a human antibody with those from a mouse. Nature (Lond.), 321: 522-525, 1986.
29. Riechman, L., Clark, M., Waldmann, H., and Winter, G. Reshaping human antibodies for therapy. Nature (Lond.), 332: 323-327, 1988.
30. Kabat, E. A., Wu, T. T., Perry, H. M., Gottesmann, K. S., and Foeller, C. Sequences of proteins of immunological interest. Ed. 5. Public Health Service, National Institutes of Health, Bethesda, MD, 1991.
31. Werther, W. A., Gonzalez, T. N., O'Connor, S. J., McCabe, S., Chan, B., Hotaling, T., Champe, M., Fox, J. A., Jardieu, P. M., Berman, P. W., and Presta, L. G. Humanization of an anti-lymphocyte function-associated antigen (LFA)-1 monoclonal antibody and reengineering of the humanized antibody for binding to rhesus LFA-1. J. Immunol., 157: 4986-4995, 1996.
32. Carter, P., Presta, L., Gorman, C. M., Ridgway, J. B. B., Henner, D., Wong, W. L. T., Rowland, A. M., Kotts, C., Carver, M. E., and Shepard, H. M. Humanization of an anti-p185HER2 antibody for human cancer therapy. Proc. Natl. Acad. Sci. USA, 89: 4285-4289, 1992.
33. Eigenbrot, C., Randal, M., Presta, L., and Kossiakoff, A. A. X-ray structures of the antigen-binding domains from three variants of humanized anti-p185HER2 antibody 4D5 and comparison with molecular modeling. J. Mol. Biol., 229: 969-995, 1993.
34. Kunkel, T. A. Rapid and efficient site-specific mutagenesis without phenotypic selection. Proc. Natl. Acad. Sci. USA, 82: 488-492, 1985.
35. Eaton, D. L., Wood, W. I., Eaton, D., Mass, P. E., Hollingshead, P., Wion, K., Mather, J., Lawn, R. M., Vehar, G. A., and Gorman, C. Construction, and characterization of an active factor VIII variant lacking the central one-third of the molecule. Biochemistry, 25: 8343-8347, 1986.
36. Graham, F. L., Smiley, J., Russell, W. C., and Nairn, R. Characteristics of a human cell line transformed by DNA from human adenovirus type 5. J. Gen. Virol., 36: 59-74, 1977.
37. Gorman, C. M., Gies, D. R., and McCray, G. Transient production of proteins using an adenovirus transformed cell line. DNA Prot. Eng. Tech., 2: 3-10, 1990.
38. Lucas, B. K., Giere, L. M., DeMarco, R. A., Chisholm, V., and Crowley, C. W. High-level production of recombinant proteins in CHO cells using a dicistronic DHFR intron expression vector. Nucleic Acids Res., 24: 1774-1779, 1996.
39. Chisholm, V. High efficiency gene transfer in mammalian cells. In: D. M. Glover and B. D. Hames (eds.), DNA Cloning 4. Mammalian systems, pp. 1-41. Oxford: Oxford University Press, 1996.
40. Park, J. E., Chen, H., Winer, J., Houck, K. A., and Ferrara, N. Placenta growth factor. Potentiation of VEGF bioactivity, in vitro and in vivo, and high affinity binding to Flt-1 but not to Flk-1/KDR. J. Biol. Chem., 209, 25646-25645, 1994.
41. Karlsson, R., Roos, H., Fagerstam, L., and Persson, B. Kinetic and concentration analysis using BIA technology. Methods: A Companion to Methods in Enzymology, Vol. 6, pp. 97-108, 1994.
42. Leung, D. W., Cachianes, G., Kuang, W-J., Goeddel, D. V., and Ferrara, N. Vascular endothelial growth factor is a secreted angiogenic mitogen. Science (Washington DC), 246: 1306-1309, 1989.
43. Presta, L. G., Lahr, S. J., Shields, R. L., Porter, J. P., Gorman, C. M., Fendly, B. M., and Jardieu, P. M. Humanization of an antibody directed against IgE. J. Immunol., 151: 2623-2632, 1993.
44. Eigenbrot, C., Gonzalez, T., Mayeda, J., Carter, P., Werther, W., Hotaling, T., Fox, J., and Kessler, J. X-ray structures of fragments from binding and nonbinding versions of a humanized anti-CD 18 antibody: structural indications of the key role of VH residues 59 to 65. Proteins, 18: 49-62, 1994.
45. Chothia, C., Lesk, A. M., Tramontane, A., Levitt, M., Smith-Gill, S. J., Air, G., Sheriff, S., Padlan, E. A., Davies, D., Tulip, W. R., Colman, P. M., Spinelli, S., Alzari, P. M., and Poljak, R. J. Conformations of immunoglobulin hypervariable regions. Nature (Lond.), 342: 877-883, 1989.
46. Xiang, J., Sha, Y., Jia, Z., Prasad, L., and Delbaere, L. T. Framework residues 71 and 93 of the chimeric B72.3 antibody are major determinants of the conformation of heavy-chain hypervariable loops. J. Mol. Biol., 253: 385-390, 1995.
47. Tramontano, A., Chothia, C., and Lesk, A. M. Framework residue 71 is a major determinant of the position and conformation of the second hypervariable region in the VH domains of immunoglobulins. J. Mol. Biol., 215: 175-182, 1990.
48. Fischmann, T. O., Bentley, G. A., Bhat, T. N., Boulot, G., Mariuzza, R. A., Phillips, S. E. V., Tello, D., and Poljak, R. J. Crystallographic refinement of the three-dimensional structure of the FabD1.3-lysozyme complex at 2.5-Å resolution. J. Biol. Chem., 266: 12915-12920, 1994.
49. Baca, M., Presta, L. G., O'Connor, S. J., and Wells, J. A. Antibody humanization using monovalent phage display. J. Biol. Chem., 272: 10678-10684, 1997.
50. Barbas, C. F., III. Selection and evolution of high-affinity anti-viral antibodies. Trends Biotechnol., 14: 230-234, 1996.
51. HER2 monoclonal antibody in patients with HER2/neu overexpressing metastatic breast cancer. J. Clin. Oncol., 14: 737-744, 1996.
52. von Mehren, M., and Weiner, L. M. Monoclonal antibody-based therapy. Curr. Opin. Oncol., 8: 493-498, 1996.
53. Riethmuller, G., Schneider-Gadicke, E., and Johnson, J. P. Monoclonal antibodies in cancer therapy. Curr. Opin. Immunol., 5: 732-739, 1993.