E-3810

E-3810 is a novel dual inhibitor of the VEGF and FGF receptors. E-3810 has shown strong antiangiogenic properties as well as outstanding antitumor activity in a large number of preclinical models after oral administration, including resistant settings, and has shown high synergy in combination. E-3810 potently and selectively inhibited VEGF receptor (VEGFR)-1, -2, and -3 and FGF receptor (FGFR)-1 and -2 kinases in the nanomolar range. E-3810 exhibited striking antitumor properties at well-tolerated oral doses administered daily in a variety of tumor xenograft models, including early- or late-stage subcutaneous and orthotopic models. In Matrigel plug assays performed in nude mice, E-3810 inhibited basic FGF-induced angiogenesis and reduced blood vessel density as assessed by histologic analysis. E-3810 reduced the distribution of angiogenesis-sensitive contrast agents after only 5 days of treatment.