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Curr Opin Investig Drugs. 2004 Jun;5(6):597-604.

Receptor tyrosine kinase inhibitors as anti-angiogenic agents.

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  • 1Department of Radiation Oncology, Vanderbilt-Ingram Cancer Center, 1301 22nd Avenue South, Nashville, TN 37232-5671, USA.


Receptor tyrosine kinases (RTKs) and their ligands have been implicated in angiogenesis and current data suggest that they are potential cancer therapeutic targets. Split-kinase domain RTKs, including receptors for vascular endothelial growth factor receptor, platelet-derived growth factor and fibroblast growth factor, have important roles in tumor angiogenesis. RTK inhibitors targeting tumor microvasculature have shown promising results in preclinical studies, and use of these compounds as single agents, or in combination with other cytotoxic therapies, including radiation, is an area of active clinical investigation. Preclinical and clinical data from representative anti-angiogenic RTK inhibitors will be discussed in this review.

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