Abstract
Angiogenesis and vasculogenesis, regulated by VEGF/VEGFR signaling pathways, play key roles in tumor growth and metastasis. Selective inhibition of VEGFR kinase has been explored as a highly successful clinical strategy in cancer treatment. A number of VEGFR inhibitors have been approved in clinical use and many more are in various stages of drug development. This paper reviews selective small-molecule VEGFR inhibitors in clinical uses and in clinical trials, with particular focus on in vitro, in vivo and clinical trial results of these inhibitors. The VEGF/VEGFR genes and signaling pathways involved in tumor angiogenesis, and the strategies for accessing and improving the therapeutic efficacy of VEGFR inhibitors are also discussed.
Publication types
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Research Support, Non-U.S. Gov't
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Review
MeSH terms
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Angiogenesis Inhibitors / pharmacology*
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Animals
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Antineoplastic Agents / pharmacology
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Drug Design
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Humans
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Neoplasms / blood supply
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Neoplasms / drug therapy
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Neovascularization, Pathologic / drug therapy
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Neovascularization, Pathologic / pathology
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Protein Kinase Inhibitors / pharmacology*
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Receptors, Vascular Endothelial Growth Factor / antagonists & inhibitors*
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Receptors, Vascular Endothelial Growth Factor / metabolism
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Signal Transduction / drug effects
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Vascular Endothelial Growth Factor A / antagonists & inhibitors
Substances
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Angiogenesis Inhibitors
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Antineoplastic Agents
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Protein Kinase Inhibitors
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Vascular Endothelial Growth Factor A
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Receptors, Vascular Endothelial Growth Factor