Development of SU5416, a selective small molecule inhibitor of VEGF receptor tyrosine kinase activity, as an anti-angiogenesis agent.

摘要: Angiogenesis, or the sprouting of new blood vessels, is a central process in growth solid tumors. For many cancers, extent vascularization tumor negative prognostic indicator signifying aggressive disease and increased potential for metastasis. Recent efforts to understand molecular basis tumor-associated angiogenesis have identified several therapeutic targets, including receptor tyrosine kinases angiogenic factor vascular endothelial (VEGF). Here we review approach taken at SUGEN, Inc. discover develop small molecule inhibitors as anti-angiogenic agents. We focus on SU5416, selective inhibitor VEGF receptors that currently clinical development treatment advanced malignancies. Its biochemical, biological pharmacological properties are reviewed implications discussed.