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Chemical Compound Review

Axitinib     N-methyl-2-[[3-[(E)-2- pyridin-2-ylethenyl]...

Synonyms: Inlyta, axitinibum, QCR-109, Inlyta (TN), S1005_Selleck, ...
 
 
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Disease relevance of Axitinib

  • Blood vessels that survived treatment with AG-013736, a small molecule inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptors, had only 4% as much binding of RGD-4C phage compared with vessels in untreated tumors [1].
  • AG-013736 significantly inhibited growth of breast tumors in vivo at all doses studied (10-100 mg/kg) and disrupted tumor microvasculature as assessed by DCE-MRI [2].
  • The anti-angiogenesis agent, AG-013736, has minimal activity in elderly patients with poor prognosis acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) [3].
  • Axitinib was well tolerated, showed a selective VEGFR-inhibitory profile, and showed single-agent activity in metastatic melanoma [4].
 

High impact information on Axitinib

 

Chemical compound and disease context of Axitinib

 

Associations of Axitinib with other chemical compounds

  • Although axitinib inhibits platelet-derived growth factor receptors and KIT with nanomolar in vitro potencies, based on pharmacokinetic/pharmacodynamic analysis, axitinib acts primarily as a VEGFR tyrosine kinase inhibitor at the current clinical exposure [7].

References

  1. Antiangiogenic therapy decreases integrin expression in normalized tumor blood vessels. Yao, V.J., Ozawa, M.G., Varner, A.S., Kasman, I.M., Chanthery, Y.H., Pasqualini, R., Arap, W., McDonald, D.M. Cancer Res. (2006) [Pubmed]
  2. AG-013736, a novel inhibitor of VEGF receptor tyrosine kinases, inhibits breast cancer growth and decreases vascular permeability as detected by dynamic contrast-enhanced magnetic resonance imaging. Wilmes, L.J., Pallavicini, M.G., Fleming, L.M., Gibbs, J., Wang, D., Li, K.L., Partridge, S.C., Henry, R.G., Shalinsky, D.R., Hu-Lowe, D., Park, J.W., McShane, T.M., Lu, Y., Brasch, R.C., Hylton, N.M. Magnetic resonance imaging (2007) [Pubmed]
  3. The anti-angiogenesis agent, AG-013736, has minimal activity in elderly patients with poor prognosis acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS). Giles, F.J., Bellamy, W.T., Estrov, Z., O'Brien, S.M., Verstovsek, S., Ravandi, F., Beran, M., Bycott, P., Pithavala, Y., Steinfeldt, H., Reich, S.D., List, A.F., Yee, K.W. Leuk. Res. (2006) [Pubmed]
  4. Multicenter, Phase II Study of Axitinib, a Selective Second-Generation Inhibitor of Vascular Endothelial Growth Factor Receptors 1, 2, and 3, in Patients with Metastatic Melanoma. Fruehauf, J., Lutzky, J., McDermott, D., Brown, C.K., Meric, J.B., Rosbrook, B., Shalinsky, D.R., Liau, K.F., Niethammer, A.G., Kim, S., Rixe, O. Clin. Cancer Res. (2011) [Pubmed]
  5. Phase I trial of the oral antiangiogenesis agent AG-013736 in patients with advanced solid tumors: pharmacokinetic and clinical results. Rugo, H.S., Herbst, R.S., Liu, G., Park, J.W., Kies, M.S., Steinfeldt, H.M., Pithavala, Y.K., Reich, S.D., Freddo, J.L., Wilding, G. J. Clin. Oncol. (2005) [Pubmed]
  6. Current status and future directions of oral tyrosine kinase inhibitors in the treatment of cancer (part 3 of a 3-part series on angiogenesis inhibition in solid tumor malignancies). Pegram, M., George, D., Miller, K. Clinical advances in hematology & oncology : H&O (2006) [Pubmed]
  7. Nonclinical antiangiogenesis and antitumor activities of axitinib (AG-013736), an oral, potent, and selective inhibitor of vascular endothelial growth factor receptor tyrosine kinases 1, 2, 3. Hu-Lowe, D.D., Zou, H.Y., Grazzini, M.L., Hallin, M.E., Wickman, G.R., Amundson, K., Chen, J.H., Rewolinski, D.A., Yamazaki, S., Wu, E.Y., McTigue, M.A., Murray, B.W., Kania, R.S., O'Connor, P., Shalinsky, D.R., Bender, S.L. Clin. Cancer Res. (2008) [Pubmed]
 
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