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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
Chemical Compound Review

Vatalanib     butanedioic acid; N-(4-chlorophenyl)-4...

Synonyms: PTK-787, CHEMBL75232, PTK787, SureCN675786, PTK/ZK, ...
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Disease relevance of Vatalanib


High impact information on Vatalanib


Chemical compound and disease context of Vatalanib


Biological context of Vatalanib


Anatomical context of Vatalanib


Associations of Vatalanib with other chemical compounds

  • In this study, we examined the activity of PTK787/ZK 222584 (PTK787), a molecule designed to bind specifically to the tyrosine kinase domain of VEGFR and inhibit angiogenesis [7].
  • We evaluated the effects of selective VEGF receptor (VEGFR; PTK787/ZK222584) and ErbB (PKI166 and ZD1839) inhibitors on tumor growth and angiogenesis and asked whether additional therapeutic benefit was conferred by combination treatment [14].
  • In vivo, combined treatment with PTK787 and imatinib significantly reduced the formation of neointimal lesions in arteries of cardiac allografts at 8 weeks, producing a greater effect than either drug alone [15].
  • RESULTS: In either rho/PDGF-B or rho/PDGF-A mice, oral administration of PKC412 or PTK787, but not SU1498 or imatinib mesylate, significantly reduced ERM formation [16].
  • Seven days later, groups of mice were given daily oral administrations of PTK 787 alone, twice weekly i.p. injections of gemcitabine, or combination therapy [11].

Gene context of Vatalanib


Analytical, diagnostic and therapeutic context of Vatalanib


  1. Dynamic contrast-enhanced magnetic resonance imaging as a biomarker for the pharmacological response of PTK787/ZK 222584, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinases, in patients with advanced colorectal cancer and liver metastases: results from two phase I studies. Morgan, B., Thomas, A.L., Drevs, J., Hennig, J., Buchert, M., Jivan, A., Horsfield, M.A., Mross, K., Ball, H.A., Lee, L., Mietlowski, W., Fuxuis, S., Unger, C., O'Byrne, K., Henry, A., Cherryman, G.R., Laurent, D., Dugan, M., Marmé, D., Steward, W.P. J. Clin. Oncol. (2003) [Pubmed]
  2. 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. Drevs, J., Hofmann, I., Hugenschmidt, H., Wittig, C., Madjar, H., Müller, M., Wood, J., Martiny-Baron, G., Unger, C., Marmé, D. Cancer Res. (2000) [Pubmed]
  3. Enhanced susceptibility of irradiated tumor vessels to vascular endothelial growth factor receptor tyrosine kinase inhibition. Zips, D., Eicheler, W., Geyer, P., Hessel, F., Dörfler, A., Thames, H.D., Haberey, M., Baumann, M. Cancer Res. (2005) [Pubmed]
  4. 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. Drevs, J., Müller-Driver, R., Wittig, C., Fuxius, S., Esser, N., Hugenschmidt, H., Konerding, M.A., Allegrini, P.R., Wood, J., Hennig, J., Unger, C., Marmé, D. Cancer Res. (2002) [Pubmed]
  5. Vascular endothelial growth factor contributes to prostate cancer-mediated osteoblastic activity. Kitagawa, Y., Dai, J., Zhang, J., Keller, J.M., Nor, J., Yao, Z., Keller, E.T. Cancer Res. (2005) [Pubmed]
  6. Both antiangiogenesis- and angiogenesis-independent effects are responsible for hepatocellular carcinoma growth arrest by tyrosine kinase inhibitor PTK787/ZK222584. Liu, Y., Poon, R.T., Li, Q., Kok, T.W., Lau, C., Fan, S.T. Cancer Res. (2005) [Pubmed]
  7. The vascular endothelial growth factor receptor tyrosine kinase inhibitor PTK787/ZK222584 inhibits growth and migration of multiple myeloma cells in the bone marrow microenvironment. Lin, B., Podar, K., Gupta, D., Tai, Y.T., Li, S., Weller, E., Hideshima, T., Lentzsch, S., Davies, F., Li, C., Weisberg, E., Schlossman, R.L., Richardson, P.G., Griffin, J.D., Wood, J., Munshi, N.C., Anderson, K.C. Cancer Res. (2002) [Pubmed]
  8. Ionizing radiation antagonizes tumor hypoxia induced by antiangiogenic treatment. Riesterer, O., Honer, M., Jochum, W., Oehler, C., Ametamey, S., Pruschy, M. Clin. Cancer Res. (2006) [Pubmed]
  9. Targeting vascular endothelial growth factor pathway offers new possibilities to counteract microvascular disturbances during ischemia/reperfusion of the pancreas. von Dobschuetz, E., Meyer, S., Thorn, D., Marme, D., Hopt, U.T., Thomusch, O. Transplantation (2006) [Pubmed]
  10. A phase IB, open-label dose-escalating study of the oral angiogenesis inhibitor PTK787/ZK 222584 (PTK/ZK), in combination with FOLFOX4 chemotherapy in patients with advanced colorectal cancer. Thomas, A., Trarbach, T., Bartel, C., Laurent, D., Henry, A., Poethig, M., Wang, J., Masson, E., Steward, W., Vanhoefer, U., Wiedenmann, B. Ann. Oncol. (2007) [Pubmed]
  11. Inhibition of growth and metastasis of human pancreatic cancer growing in nude mice by PTK 787/ZK222584, an inhibitor of the vascular endothelial growth factor receptor tyrosine kinases. Solorzano, C.C., Baker, C.H., Bruns, C.J., Killion, J.J., Ellis, L.M., Wood, J., Fidler, I.J. Cancer Biother. Radiopharm. (2001) [Pubmed]
  12. 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. Wood, J.M., Bold, G., Buchdunger, E., Cozens, R., Ferrari, S., Frei, J., Hofmann, F., Mestan, J., Mett, H., O'Reilly, T., Persohn, E., Rösel, J., Schnell, C., Stover, D., Theuer, A., Towbin, H., Wenger, F., Woods-Cook, K., Menrad, A., Siemeister, G., Schirner, M., Thierauch, K.H., Schneider, M.R., Drevs, J., Martiny-Baron, G., Totzke, F. Cancer Res. (2000) [Pubmed]
  13. Phase I study of the safety, tolerability, pharmacokinetics, and pharmacodynamics of PTK787/ZK 222584 administered twice daily in patients with advanced cancer. Thomas, A.L., Morgan, B., Horsfield, M.A., Higginson, A., Kay, A., Lee, L., Masson, E., Puccio-Pick, M., Laurent, D., Steward, W.P. J. Clin. Oncol. (2005) [Pubmed]
  14. The antitumor and antiangiogenic activity of vascular endothelial growth factor receptor inhibition is potentiated by ErbB1 blockade. Sini, P., Wyder, L., Schnell, C., O'Reilly, T., Littlewood, A., Brandt, R., Hynes, N.E., Wood, J. Clin. Cancer Res. (2005) [Pubmed]
  15. Combined vascular endothelial growth factor and platelet-derived growth factor inhibition in rat cardiac allografts: beneficial effects on inflammation and smooth muscle cell proliferation. Nykänen, A.I., Krebs, R., Tikkanen, J.M., Raisky, O., Sihvola, R., Wood, J., Koskinen, P.K., Lemström, K.B. Transplantation (2005) [Pubmed]
  16. The kinase inhibitor PKC412 suppresses epiretinal membrane formation and retinal detachment in mice with proliferative retinopathies. Saishin, Y., Saishin, Y., Takahashi, K., Seo, M.S., Melia, M., Campochiaro, P.A. Invest. Ophthalmol. Vis. Sci. (2003) [Pubmed]
  17. Soluble markers for the assessment of biological activity with PTK787/ZK 222584 (PTK/ZK), a vascular endothelial growth factor receptor (VEGFR) tyrosine kinase inhibitor in patients with advanced colorectal cancer from two phase I trials. Drevs, J., Zirrgiebel, U., Schmidt-Gersbach, C.I., Mross, K., Medinger, M., Lee, L., Pinheiro, J., Wood, J., Thomas, A.L., Unger, C., Henry, A., Steward, W.P., Laurent, D., Lebwohl, D., Dugan, M., Marmé, D. Ann. Oncol. (2005) [Pubmed]
  18. Inhibition of vascular endothelial growth factor (VEGF) as a novel approach for cancer therapy. Wood, J.M. Medicina (B Aires) (2000) [Pubmed]
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