Pharmacological Characterization of CP-547,632, a Novel Vascular Endothelial Growth Factor Receptor-2 Tyrosine Kinase Inhibitor for Cancer Therapy

Cancer Research

Volumn 63, Issue 21, 2003, Pages 7301-7309

  Beebe, Jean S ^a   Jani, Jitesh P ^a   Knauth, Elisabeth ^a   Goodwin, Peter ^a   Higdon, Carla ^a   Rossi, Ann Marie ^a   Emerson, Erling ^a   Finkelstein, Martin ^a   Floyd, Eugenia ^a   Harriman, Shawn ^a   Atherton, Jim ^a   Hillerman, Steve ^a   Soderstrom, Cathy ^a   Kou, Kou ^a   Gant, Tom ^a   Noe, Mark C ^a   Foster, Barb ^a   Rastinejad, Farzan ^a   Marx, Matthew A ^a   Schaeffer, Tracey ^a   Whalen, Pamela M ^a   Roberts, W Gregory ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 (4 BROMO 2,6 DIFLUOROBENZYLOXY) 5 [3 (4 PYRROLIDIN 1 YLBUTYL)UREIDO]ISOTHIAZOLE 4 CARBOXYLIC ACID AMIDE; 3 (4 BROMO 2,6 DIFLUOROBENZYLOXY) 5 [3 [4 (1 PYRROLIDINYL)BUTYL]UREIDO] 4 ISOTHIAZOLECARBOXAMIDE; ANGIOGENESIS INHIBITOR; BASIC FIBROBLAST GROWTH FACTOR; BASIC FIBROBLAST GROWTH FACTOR KINASE; EPIDERMAL GROWTH FACTOR RECEPTOR; FIBROBLAST GROWTH FACTOR; FIBROBLAST GROWTH FACTOR RECEPTOR 2; ISOTHIAZOLE DERIVATIVE; PLATELET DERIVED GROWTH FACTOR B; UNCLASSIFIED DRUG; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 SMALL MOLECULE INHIBITOR; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR 2 TYROSINE KINASE INHIBITOR; VASCULOTROPIN RECEPTOR 2;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ARTICLE; AUTOPHOSPHORYLATION; CANCER INHIBITION; CANCER THERAPY; CELL PROLIFERATION; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFICACY; DRUG STRUCTURE; DRUG TOLERABILITY; ENDOTHELIUM CELL; ENZYME LINKED IMMUNOSORBENT ASSAY; FEMALE; IC 50; METASTASIS INHIBITION; MOUSE; NONHUMAN; NUDE MOUSE; PRIORITY JOURNAL; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION;

ANIMALS; ENDOTHELIUM, VASCULAR; ENZYME INHIBITORS; FEMALE; HUMANS; KINETICS; MALE; MICE; MICE, INBRED C3H; MICE, NUDE; NEOPLASMS, EXPERIMENTAL; NEOVASCULARIZATION, PATHOLOGIC; NIH 3T3 CELLS; PHOSPHORYLATION; RATS; RATS, SPRAGUE-DAWLEY; THIAZOLES; UREA; VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 10744222964     PISSN: 00085472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (43)

1. Folkman, J. Antiangiogenesis: new concept for theory of solid tumors. Ann. Surg., 175: 409-416, 1972.
2. Folkman, J. Tumor angiogenesis. Adv. Cancer Res., 43: 175-203, 1985.
3. Folkman, J., and Shing, Y. Angiogenesis. J. Biol. Chem., 267: 10931-10934, 1992.
4. Boehm, T., Folkman, J., Browder, T., and O'Reilly, M. S. Antiangiogenic therapy of experimental cancer does not induce acquired drug resistance. Nature (Lond.), 390: 404-407, 1997.
5. Nagashima, M., Yoshino, S., Ishiwata, T., and Asano, G. Role of vascular endothelial growth factor in angiogenesis of rheumatoid arthritis. J. Rheumatol., 22: 1624-1630, 1995.
6. Alon, T., Hemo, I., Itin, A., Pe'er, J., Stone, J., and Keshet, E. Vascular endothelial growth factor acts as a survival factor for newly formed retinal vessels and has implications for retinopathy of prematurity. Nat. Med., 1: 1024-1028, 1995.
7. Folkman, J. Angiogenesis in cancer, vascular, rheumatoid and other diseases. Nat. Med., 1: 27-31, 1995.
8. Lindner, V., Majack, R. A., and Reidy, M. A. Basic fibroblast growth factor stimulates endothelial regrowth and proliferation in denuded arteries. J. Clin. Investig., 85: 2004-2008, 1990.
9. Jackson, M. R., Carney, E. W., Lye, S. J., and Ritchie, J. W. Localization of two angiogenic growth factors (PDECGF and VEGF) in human placenta throughout gestation. Placenta, 15: 341-353, 1994.
10. Rifkin, D. B., and Klagsbrun, M. Angiogenesis: Mechanisms and Pathobiology. Cold Spring Harbor: Cold Spring Harbor Laboratory. 1987.
11. Bohling, T., Hatva, E., Kujala, M. Claesson-Welsh, L., Alitalo, K., and Haltia, M. Expression of growth factors and growth factor receptors in capillary hemangioblastoma. J. Neuropathol. Exp. Neurol., 55: 522-527, 1996.
12. Ferrara, N., Houck, K., Jakeman, L., and Leung, D. W. Molecular and biological properties of the vascular endothelial growth factor family of proteins. Endocr. Rev., 13: 18-32, 1992.
13. Fu, X., Roberts, W. G., Nobile, V., Shapiro, R., and Kamps, M. Angiogenin-3, a target gene of E2a-Pbx1 in NIH3T3 fibroblasts, is a new angiogenic member of the angiogenin family. Growth Factors., 17: 125-137, 1999.
14. Ferrara, N. Molecular and biological properties of vascular endothelial growth factor. J. Mol. Med., 77: 527-543, 1999.
15. Senger, D. R., Galli, S. J., Dvorak, A. M., Peruzzi, C. A., Harvey, V. S., and Dvorak, H. F. Tumor cells secrete a vascular permeability factor that promotes accumulation of ascites fluid. Science (Wash. DC), 219: 983-985, 1983.
16. Ferrara, N., and Henzel, W. J. Pituitary follicular cells secrete a novel heparin-binding growth factor specific for vascular endothelial cells. Biochem. Biophys. Res. Comm., 161: 851-858, 1989.
17. Shweiki, D., Neeman, M., Itin, A., and Keshet, E. Induction of vascular endothelial growth factor expression by hypoxia and by glucose deficiency in multicell spheroids: Implications for tumor angiogenesis. Proc. Natl. Acad. Sci. USA, 92: 768-772, 1995.
18. De Vries, C., Escobedo, J. A., Ueno, H., Houck, K., Ferrara, N., and Williams, L. T. The fms-like tyrosine kinase, a receptor for vascular endothelial growth factor. Science (Wash. DC), 255: 989-991, 1992.
19. Quinn, T. P., Peters, K. G., DeVries, C., Ferrara, N., and Williams, L. T. Fetal liver kinase 1 is a receptor for vascular endothelial growth factor and is selectively expressed in vascular endothelium. Proc. Natl. Acad. Sci. USA, 90: 7533-7537, 1993.
20. Yamaguchi, T. P., Dumont, D. J., Conlon, R. A., Breitman, M. L., and Rossant, J. flk-1, an flt-related receptor kinase is an early marker for endothelial cell precursors. Development, 118: 489-498, 1993.
21. Fong, G. H., Klingensmith, J., Wood, C. R., Rossant, J., and Breitman, M. L. Regulation of flt-1 expression during mouse embryogenesis suggests a role in the establishment of vascular endothelium. Dev. Dyn., 207: 1-10, 1996.
22. Presta, L. G., Chen, H., O'Connor, S. J., Chisholm, V., Meng, Y. G., Krummen, L., Winkler, M., and Ferrara, N. Humanization of an anti-vascular endothelial growth factor monoclonal antibody for the therapy of solid tumors and other disorders. Cancer Res., 57: 4593-4599, 1997.
23. Gordon, M. S., Margolin, M. M., Sledge, G. W., Holmgren, E., Benjamin, R., Stalter, S., Shak, S., and Adelman, D. C. Phase I safety and pharmacokinetic study of recombinant human anti-vascular endothelial growth factor receptor in patients with advanced cancer. J. Clin. Oncol., 19: 843-850, 2001.
24. Pavco, P. A., Bouhana, K. S., Gallegos, A. M., Agrawal, A., Blanchard, K. S., Grimm, S. L., Jensen, K. L., Andrews, L. E., Wincott, F. E., Pitot, P. A., Tressler, R. J., Cushman, C., Reynolds, M. A., and Parry, T. J. Antitumor and antimetastatic activity of ribozymes targeting the messenger RNA of vascular endothelial growth factor receptors. Clin. Cancer Res., 6: 2094-2103, 2000.
25. Shaheen, R. M., Tseng, W. W., Vellagas, R., Liu, W., Ahmad, S. A., Jung, Y. D., Reinmuth, N., Drazan, K. E., Bucana, C. D., Hicklin, D. J., and Ellis, L. M. Effects of an antibody to vascular endothelial growth factor receptor-2 on survival, tumor vascularity, and apoptosis in a murine model of colon carcinomatosis. Int. J. Oncology, 18: 221-226, 2001.
26. Drevs, J., Hofmann, I., Hugenschmidt, H., Wittig, C., Madjar, H., Muller, M., Wood, J., Martiny-Baron, G., Unger, C., and Marme, D. Effects of PTK787/ZK 222584, a specific inhibitor of vascular endothelial growth factor receptor tyrosine kinases, on primary tumor, metastasis, vessel density, and blood flow in a murine renal cell carcinoma model. Cancer Res., 60: 4819-4824, 2000.
27. Wedge, S. R., Ogilvie, D. J., Dukes, M., Kendrew, J., Curwen, J. O., Hennequin, L. F., Thomas, A. P., Stokes, E. S. E., Curry, B., Richmond, G. H. P., and Wadsworth, P. F. ZD4190: an orally active inhibitor of vascular endothelial growth factor signaling with broad-spectrum antitumor efficacy. Cancer Res., 60: 970-975, 2000.
28. Hess, C., Vuong, V., Hegyi, I., Riesterer, O., Wood, J., Fabbro, D., Glanzmann, C., Bodis, S., and Pruschy, M. Effect of VEGF receptor inhibitor PTK787/ZK222584 combined with ionizing radiation on endothelial cells and tumour growth. Br. J. Cancer, 85: 2010-2016, 2001.
29. Klement, G., Huang, P., Mayer, B., Green, S. K., Man, S., Bohlen, P., Hicklin, D., and Kerbel, R. S. Differences in therapeutic indexes of combination metronomic chemotherapy and an anti-VEGFR-2 antibody in multidrug-resistant human breast cancer xenografts. Clin. Cancer Res., 8: 221-232, 2002.
30. Waltenberger, J., Claesson-Welsh, L., Siegbahn, A., Shibuya, M., and Heldin, C-H. Different signal transduction properties of KDR and Flt-1, two receptors for vascular endothelial growth factor. J. Biol. Chem., 269: 26988-95, 1994.
31. Kenyon, B. M., Voest, E. E., Chen, C. C., Flynn, E., Folkman, J., and D'Amato, R. J., A model of angiogenesis in the mouse cornea. Investigative Ophthalmol. Vis. Sci., 37: 1625-1632, July 1996.
32. Rak, J., Mitsuhashi, Y., Sheehan, C., Tamir, A., Viloria-Petit, A., Filmus, J., Mansour, S. J., Ahn, N. G., and Kerbel, R. S. Oncogenes and tumor angiogenesis: differential modes of vascular endothelial growth factor up-regulation in ras-transformed epithelial cells and fibroblasts. Cancer Res., 60: 490-988, 2000.
33. Ferrara, N., Winer, J., Burton, T., Rowland, A., Siegel, M., Phillips, H. S., Terrell, T., Keller, G. A., and Levinson, A. D. Expression of vascular endothelial growth factor does not promote transformation but confers a growth advantage in vivo to Chinese hamster ovary cells. J. Clin. Investig., 91: 160-170, 1993.
34. Roberts, W. G., and Palade, G. E. Neovasculature induced by vascular endothelial growth factor is fenestrated. Cancer Res., 57: 765-772, 1997.
35. Drevs, J., Muller-Driver, R., Wittig, C., Fuxius, S., Esser, N., Hugenschmidt, H., Konerding, M. A., Allegrini, P. R., Wood, J., Hennig, J., Unger, C., and Marme, D. PTK787/ZK 222584, a specific vascular endothelial growth factor receptor tyrosine kinase inhibitor, affects the anatomy of the tumor vascular bed and the functional vascular properties as detected by dynamic enhanced magnetic resonance imaging. Cancer Res., 62: 4015-4022, 2002.
36. Gerber, H., Vu, T. H., Ryan, A. M., Kowalski, J., Werb, Z., and Ferrara, N. VEGF couples hypertrophic cartilage remodeling, ossification and angiogenesis during endochondral bone formation. Nat. Med., 5: 623-628, 1999.
37. Wedge, S. R., Ogilvie, D. J., Dukes, M., Kendrew, J., Chester, R., Jackson, J. A., Boffey, S. J., Valentine, P. J., Curwen, J. O., Musgrove, H. L., Graham, G. A., Hughes, G. D., Thomas, A. P., Stokes, E. S. E., Curry, B., Richmond, G. H. P., Wadsworth, P. F., Bigley, A. L., and Hennequin, L. F. ZD6474 inhibits vascular endothelial growth factor signaling, angiogenesis, and tumor growth following oral administration. Cancer Res., 62: 4645-4655, 2002.
38. Ryan, A. M., Eppler, D. B., Hagler, K. E., Bruner, R. H., Thomford, P. J., Hall, R. L., Shopp, G. M., and O'Neill, C. A. Preclinical safety evaluation of rhuMAbVEGF, an antiangiogenic humanized monoclonal antibody. Toxicologic Pathol., 27: 78-86, 1999.
39. Mater, A. Tumor angiogenesis as a therapeutic target. Drug Discovery Today, 6: 1005-1024, 2001.
40. Toi, M., Matsumoto, T., and Bando, H. Vascular endothelial growth factor: its prognostic, predictive, and therapeutic implications. Lancet, 2: 667-673, 2001.
41. Wood, J. M., Bold, G., Buchdunger, E., Cozens, R., Ferrari, S., Frei, J., Hofmann, F., Mestan, J., Mett, H., O'Reilly, T., Persohn, E., Rosel, J., Schnell, C., Stover, D., Theuer, A., Towbin, H., Wegner, F., Woods-Cook, K., Menrad, A., Siemeister, G., Schirner, M., Thierauch, K., Schneider, M. R., Drevs, J., Martiny-Baron, G., Totzke, F., and Marme, D. PTK787/ZK 222584, a novel and potent inhibitor of vascular endothelial growth factor receptor tyrosine kinases, impairs vascular endothelial growth factor-induced responses and tumor growth after oral administration. Cancer Res., 60: 2178-2189, 2000.
42. Sandberg, J. A., Parker, V. P., Blanchard, K. S., Sweedler, D., Powell, J. A., Kachensky, A., Bellon, L., Usman, N., Rossing, T., Borden, E., and Blatt, L. M. Pharmacokinetics and tolerability of an antiangiogenic ribozyme (Angiozyme) in healthy volunteers. J. Clin. Pharmacol., 40: 1462-1469, 2000.
43. Hunt, S. Technology evaluation: IMC-IC11. ImClone Systems. Curr. Opin. Mol. Ther., 3: 418-424, 2001.