Definition

An orally bioavailable, small molecule inhibitor of human vascular endothelial growth factor receptor 3 (VEGFR3; VEGFR-3; Flt-4), with potential anti-angiogenic and antineoplastic activities. Upon oral administration, VEGFR3 inhibitor EVT801 specifically targets, binds to and inhibits VEGFR3 tyrosine kinase, which may result in the inhibition of tumor angiogenesis and a decrease in tumor nutrient supply. EVT801 may also decrease the level of immune suppressive myeloid derived suppressor cells (MDSCs) in the blood, thereby activating anti-tumor immune responses. VEGFR3 plays a critical role in the embryonic vascular system development but is restricted postnatally to endothelial cells of lymphatic vessels and found to be expressed in many solid and hematologic malignancies.