Definition

An orally bioavailable inhibitor of multiple receptor tyrosine kinases (RTKs), with potential antineoplastic activity. Upon oral administration, DDR1-2/VEGFR2-3/PDGFRalpha-beta inhibitor ICP-033 selectively targets, binds to and inhibits the activity of numerous RTKs including discoid domain receptor type 1 (DDR1) and 2 (DDR2), vascular endothelial growth factor receptors type 2 (VEGFR2) and 3 (VEGFR3) and platelet-derived growth factor receptor alpha (PDGFRa) and beta (PDGFRb). By inhibiting multiple RTKs located in endothelial cells, pericytes and stroma, ICP-033 may be able to inhibit angiogenesis and tumor cell invasion, normalize abnormal blood vessels, and reverse the immunosuppressive state of the tumor microenvironment (TME). This may halt tumor cell proliferation in susceptible tumor cells.