Cilengitide is a cyclo-(Arg-Gly-Asp-D-Phe-Val) (cRGDfV) peptide and integrin αVβ3 receptor antagonist.1 It inhibits adhesion and induces apoptosis of U87MG and U373MG malignant glioma (MG) cells, but not U251MG cells that lack the integrin αVβ3 receptor, in vitro at a concentration of 20 μg/ml. Cilengitide (200 μg/animal per day) delays tumor implantation time, reduces tumor growth, and prolongs survival in a U87MG mouse model of glioblastoma.2
1.Chatterjee, S., Matsumura, A., Schradermeier, J., et al.Human malignant glioma therapy using anti-αVβ3 integrin agentsJ. Neurooncol.46(2)135-144(2000) 2.Yamada, S., Bu, X.-Y., Khankaldyyan, V., et al.Effect of the angiogenesis inhibitor cilengitide (EMD 121974) on glioblastoma growth in nude miceNeurosurgery59(6)1304-1312(2006)