Cilengitide is a potent and selective integrin inhibitor for αvβ3 and αvβ5 receptors, with IC50 values of 4 nM and 79 nM, respectively. It functions as an αvβ3 and αvβ5 integrin receptor antagonist. In cell adhesion studies, it inhibits integrin-mediated binding to vitronectin with IC50s of 0.4 and 0.4 μM in human melanoma M21 or UCLA-P3 human lung carcinoma cell lines. In vitro, concentrations greater than 1 μM show concentration- and time-dependent cytotoxic effects. In nude mice bearing M21-L melanoma tumors, it demonstrates inhibition of tumor growth with reductions in both tumor volume and tumor weight.
- Potent and selective integrin inhibitor for αvβ3 and αvβ5 receptors.
- Inhibits integrin-mediated binding to vitronectin.
- Exhibits cytotoxic effects in vitro at concentrations greater than 1 μM.
- Inhibits tumor growth in melanoma models.