Drugs in Clinical Pipeline: Vatalanib Vatalanib [ N-(4-chlorophenyl)-4-(pyridine-4-ylmethyl)phthalazin-1-amine ] is an orally bioavailable anilinophthalazine compound that has potent antineoplastic activity. Vatalanib binds to and inhibits the protein kinase domain of vascular endothelial growth factor receptors 1 and 2 (VEGFR 1 and VEGFR2); both receptor tyrosine kinases are involved in angiogenesis. This agent also binds to and inhibits related receptor tyrosine kinases, including platelet-derived growth factor (PDGF) receptor, c-Kit, and c-Fms [1]. Preclinical studies demonstrated antitumor activity against a broad range of cancer types, including colorectal, prostate, renal, hepatocellular, myeloma, recurrent glioblastoma multiform and ovarian. The compound has been investigated in phase I/II studies, alone and in combination with chemotherapy. The activity of Vatalanib is as follows: IC 50 (VEGFR2/KDR, cell-free assay) = 37 nM IC 50 (VEGFR1/F...
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Showing posts from September, 2018