Cilengitide is a cyclic arginine-glycine-aspartic acid (RGD) motif containing peptide that selectively inhibits the integrin αv subunit. Integrins are cell adhesion molecules which mediate cell-cell and cell-matrix interactions and creating a scaffold for tissue organisation. Integrins also act to regulate cell attachment, proliferation, differentiation, apoptosis and motility.

Integrin αv can form heterodimers with integrin subunits β1, β3, β5, β6, or β8. Cilengitide is a highly selective antagonist of αvβ3 and αvβ5 integrins. It also and shows anti-angiogenic effects and inhibits growth and promotes apoptosis of tumour cells that express integrins, such as glioblastoma.

Cilengitide has gone on to phase II trials for cancers such as glioblastoma, melanoma, prostate, breast, lung and head and neck cancers.

The linear form of cilengitide is also available in our catalogue.