Drugs targeting integrins for cancer therapy

BACKGROUND: Integrins are cell adhesion receptors involved in development, angiogenesis, blood clotting, inflammation and cancer. Abnormal integrin expression is a hallmark of cancer and angiogenic endothelial cells. Integrin-targeted therapy is, therefore, considered a promising novel treatment approach in oncology.

OBJECTIVE: We describe the biological background making integrins an attractive therapeutic target as well as the effects of integrin-targeted therapies in preclinical and clinical settings.

METHODS: A literature search in integrin-targeted therapy was conducted, focusing on αvβ3, αvβ5, α5β1 and α4β1 integrin ligands as well as in vivo models and clinical trials.

RESULTS/CONCLUSION: Blocking certain integrins can inhibit tumor growth and integrin ligands can be used to target cytotoxic agents to cancer tissue. Clinical trials using integrin inhibitors have yielded variable results and continuing studies evaluate their role as monotherapy or in combination with chemo- or radiotherapy.