xl820

XL820 is an orally bioavailable, investigational small molecule receptor tyrosine kinase inhibitor developed for the treatment of cancer. It selectively inhibits multiple clinically validated targets implicated in tumor proliferation and angiogenesis, including platelet-derived growth factor receptor alpha (PDGFRα), platelet-derived growth factor receptor beta (PDGFRβ), mast/stem cell growth factor receptor KIT, and vascular endothelial growth factor receptor 2 (VEGFR2). Preclinical studies demonstrated dose-dependent inhibition of tumor cell growth in models of breast carcinoma, gliomas, and leukemia. In animal models of advanced malignancy, significant tumor regression was observed. XL820 has shown good oral bioavailability and sustained inhibition of its target kinases following a single oral dose. Clinical development included trials for solid tumors and gastrointestinal stromal tumors (GIST), but development was discontinued[1][2][3][4][5][7].