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Chemical Compound Review

Cilengitide     2-[(2S,5R,8S,11S)-5-benzyl- 11-[3...

Synonyms: SureCN34082, CHEMBL429876, SureCN451423, AG-E-37840, EMD-12192, ...
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Disease relevance of EMD 121974

  • No increased toxicity attributable to Cilengitide was observed based upon pooled blood sample and no statistical increase in mortality [1].
  • In conclusion, CMRIT, combining Cilengitide and RIT, significantly increased the efficacy of therapy and increased apoptosis compared with single-modality therapy with either agent, in an aggressive, well-studied breast cancer model [1].
  • Orthotopic brain tumor growth is inhibited in athymic mice by the daily systemic administration of the alpha v-integrin antagonist EMD 121974 [2].
  • CONCLUSIONS: We conclude that radiation induces expression of alpha v beta 3 integrin in endothelial and non-small-cell lung cancer models, and that integrin antagonist Cilengitide is a radiosensitizer in proportion to the levels of target integrin expression [3].
  • Currently, patients with melanoma and glioblastoma multiforme benefit from Vitaxin (MedImmune, Gaithersburg, MD) or cilengitide treatment, respectively [4].

High impact information on EMD 121974


Chemical compound and disease context of EMD 121974


Biological context of EMD 121974


Anatomical context of EMD 121974


Associations of EMD 121974 with other chemical compounds


Gene context of EMD 121974

  • In contrast, the tumor volume in Cilengitide-treated mice stayed unchanged at 1 to 2 mm during the entire length of the experiment, with staining for Ki-67 and CD31 remaining low [10].
  • We used cyclic peptides EMD 121974, 85189 and 66203, which selectively inhibit alphav beta 3 and alphav beta 5, but not gpIIbIIIa or alpha5 beta 1, to probe in vitro angiogenesis induced by angiogenic cytokines in three-dimensional fibrin or collagen gels [11].

Analytical, diagnostic and therapeutic context of EMD 121974


  1. Cilengitide targeting of alpha(v)beta(3) integrin receptor synergizes with radioimmunotherapy to increase efficacy and apoptosis in breast cancer xenografts. Burke, P.A., DeNardo, S.J., Miers, L.A., Lamborn, K.R., Matzku, S., DeNardo, G.L. Cancer Res. (2002) [Pubmed]
  2. alpha v-Integrin antagonist EMD 121974 induces apoptosis in brain tumor cells growing on vitronectin and tenascin. Taga, T., Suzuki, A., Gonzalez-Gomez, I., Gilles, F.H., Stins, M., Shimada, H., Barsky, L., Weinberg, K.I., Laug, W.E. Int. J. Cancer (2002) [Pubmed]
  3. Integrin alpha v beta 3 antagonist Cilengitide enhances efficacy of radiotherapy in endothelial cell and non-small-cell lung cancer models. Albert, J.M., Cao, C., Geng, L., Leavitt, L., Hallahan, D.E., Lu, B. Int. J. Radiat. Oncol. Biol. Phys. (2006) [Pubmed]
  4. Integrins: molecular targets in cancer therapy. Tucker, G.C. Current oncology reports. (2006) [Pubmed]
  5. Divalent cations and the relationship between alphaA and betaA domains in integrins. Seow, K.T., Xiong, J.P., Arnaout, M.A., Welge, J., Rippmann, F., Goodman, S.L. Biochem. Pharmacol. (2002) [Pubmed]
  6. Phase II evaluations of cilengitide in asymptomatic patients with androgen-independent prostate cancer: scientific rationale and study design. Beekman, K.W., Colevas, A.D., Cooney, K., Dipaola, R., Dunn, R.L., Gross, M., Keller, E.T., Pienta, K.J., Ryan, C.J., Smith, D., Hussain, M. Clinical genitourinary cancer. (2006) [Pubmed]
  7. Longitudinal microPET imaging of brain tumor growth with F-18-labeled RGD peptide. Chen, X., Park, R., Khankaldyyan, V., Gonzales-Gomez, I., Tohme, M., Moats, R.A., Bading, J.R., Laug, W.E., Conti, P.S. Molecular imaging and biology : MIB : the official publication of the Academy of Molecular Imaging. (2006) [Pubmed]
  8. A randomized multi-center phase II trial of the angiogenesis inhibitor Cilengitide (EMD 121974) and gemcitabine compared with gemcitabine alone in advanced unresectable pancreatic cancer. Friess, H., Langrehr, J.M., Oettle, H., Raedle, J., Niedergethmann, M., Dittrich, C., Hossfeld, D.K., St??ger, H., Neyns, B., Herzog, P., Piedbois, P., Dobrowolski, F., Scheithauer, W., Hawkins, R., Katz, F., Balcke, P., Vermorken, J., van Belle, S., Davidson, N., Esteve, A.A., Castellano, D., Kleeff, J., Tempia-Caliera, A.A., Kovar, A., Nippgen, J. BMC Cancer (2006) [Pubmed]
  9. Evaluation of absorption enhancement for a potent cyclopeptidic alpha(nu)beta(3)-antagonist in a human intestinal cell line (Caco-2). Kamm, W., Jonczyk, A., Jung, T., Luckenbach, G., Raddatz, P., Kissel, T. European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences. (2000) [Pubmed]
  10. Effect of the angiogenesis inhibitor Cilengitide (EMD 121974) on glioblastoma growth in nude mice. Yamada, S., Bu, X.Y., Khankaldyyan, V., Gonzales-Gomez, I., McComb, J.G., Laug, W.E. Neurosurgery (2006) [Pubmed]
  11. alphav beta 3 and alphav beta 5 integrin antagonists inhibit angiogenesis in vitro. Nisato, R.E., Tille, J.C., Jonczyk, A., Goodman, S.L., Pepper, M.S. Angiogenesis (2003) [Pubmed]
  12. Cilengitide Merck. Smith, J.W. Current opinion in investigational drugs (London, England : 2000) (2003) [Pubmed]
  13. Epidermal growth factor receptor blockade mediates smooth muscle cell apoptosis and improves survival in rats with pulmonary hypertension. Merklinger, S.L., Jones, P.L., Martinez, E.C., Rabinovitch, M. Circulation (2005) [Pubmed]
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