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Drug intelligence / Profile preview
Semaxanib is a synthetic small molecule and potent, selective inhibitor of vascular endothelial growth factor (VEGF) receptor tyrosine kinases, particularly VEGFR2 (also known as KDR/Flk-1), and to a lesser extent VEGFR1. It also inhibits other tyrosine kinases including KIT, MET, FLT3, and RET. By blocking the ATP-binding site of these receptors' kinase domains, semaxanib disrupts downstream signaling pathways essential for angiogenesis—the formation of new blood vessels—which is critical for tumor growth and metastasis. Developed by Sugen (later acquired by Pharmacia), semaxanib was investigated primarily as an antiangiogenic agent in cancer therapy. Clinical development focused on advanced colorectal cancer and lung cancer; however, phase III trials were terminated early due to lack of efficacy compared to next-generation agents. The drug remains investigational and is not approved for clinical use but has been used in research models of pulmonary arterial hypertension due to its effects on the VEGF pathway[1][3][5][6][7].
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