cilengitide

Cilengitide is a cyclic Arg-Gly-Asp (RGD) pentapeptide and a peptidomimetic integrin inhibitor with potential antineoplastic activity. It selectively binds to and inhibits the αvβ3 and αvβ5 integrins, which are cell surface receptors involved in tumor angiogenesis, invasion, and metastasis. By blocking these integrins, cilengitide disrupts endothelial cell-cell and cell-matrix interactions, thereby inhibiting angiogenesis (the formation of new blood vessels) essential for tumor growth. Cilengitide induces apoptosis in growing endothelial cells via inhibition of the FAK/Src/AKT pathway. It was developed by Merck KGaA (also known as Merck Serono). The drug has been investigated primarily for glioblastoma but also in other malignancies such as sarcoma, lymphoma, leukemia, and lung cancer[1][2][3][4][5][6][7].

Brand names

Cilcane

Other names

cyclo[Arg-Gly-Asp-D-Phe-N-methyl-Val]cyclo(L-arginylglycyl-L-alpha-aspartyl-D-phenylalanyl-N-methyl-L-valyl)