Targeting angiogenesis from multiple pathways simultaneously: BIBF 1120, an investigational novel triple angiokinase inhibitor.

Invest New Drugs 30(3):1261-9 (2012) PMID 21350804

Angiogenesis is considered one of the major components of tumor progression and metastasis. Interfering with the formation and stabilization of tumor blood vessels could increase tumor response rates and may translate into improved clinical outcomes in cancer patients. The clinical efficacy demonstrated in phase III trials with bevacizumab, a monoclonal antibody that targets vascular endothelial growth factor ligand, suggests that targeting angiogenesis is a rational approach to cancer management. Agents that target additional proangiogenic intracellular signaling pathways also have the potential to contribute to our anticancer armamentarium. Novel targeted agents that have antiangiogenic properties have been developed in recent years such as sorafenib, sunitinib, vandetanib, and others. Many of them inhibit additional pathways beyond vascular endothelial growth factor signaling. One of these investigational targeted agents is a triple angiokinase inhibitor known as BIBF 1120. This compound targets not only vascular endothelial growth factor receptors, but also fibroblast growth factor receptors, and platelet-derived growth factor receptors. The preliminary clinical efficacy of BIBF 1120 is discussed in the context of the most relevant clinical data in several malignancies including non-small cell lung cancer.