Novel targeted agents such as bevacizumab, sorafenib, sunitinib, vandetanib, and others that have antiangiogenic properties have been developed in recent years. The angiogenesis process and its perpetuation in the tumor microenvironment is considered one of the major components of tumor progression and metastasis. Thus, interfering with the formation and stabilization of abnormal tumor blood vessels could increase tumor response rates to therapies and might translate into improved clinical outcomes in cancer patients. Some of the agents like bevacizumab, a monoclonal antibody which targets vascular endothelial growth factor ligand, have been fully developed and in the case of non-small cell lung cancer, a phase III clinical trial from the Eastern Cooperative Oncology Group established its clinical utility. These novel agents suggested 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. 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 receptor, and platelet-derived growth factor receptor. The first clinical phase I and II trials and the toxicity and efficacy of BIBF 1120 in non-small cell lung cancer are reviewed and discussed here.
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