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.
Keywords: Selective, VEGFR inhibitor, anticancer, angiogenesis, vasculogenesis, tumor growth, metastasis, clinical trials, signaling pathways, growth factors
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