Last years saw the development of anti-angiogenic strategies in the treatment of 
cancers. Cilengitide (EMD121974; Merck KGaA, Darmstadt, Germany) is a new drug 
targeting αvβ3 and αvβ5 integrins thanks to a specific peptide called RGD 
sequence. Cilengitide acts in correlations between endothelial cells, tumor 
cells and extracellular matrix. The promising results obtained with Cilengitide 
in vitro, used alone or in combination with cytotoxic chemotherapy or ionizing 
radiations, could give many hopes especially for the treatment of cerebral 
tumors. Clinical trials are nowadays ongoing in this indication. The aim of this 
review is to take stock of the situation on the mechanisms of action of the 
integrin inhibitor Cilengitide (EMD121974; Merck KGaA, Darmstadt, Germany) with 
a focus on the first pre-clinical and clinical results.