WSD1227

WSD1227 is a brain-penetrable small molecule antiangiogenic agent developed by Wayshine Biopharm for the treatment of primary and metastatic brain tumors. It functions as a potent and selective inhibitor of vascular endothelial growth factor receptors 1, 2, and 3 (VEGFR1/2/3), with IC50 values of 0.69 nM, 0.35 nM, and 0.41 nM, respectively. A key pharmacological feature of WSD1227 is its ability to effectively cross the blood-brain barrier (BBB), as it is not a substrate for the P-glycoprotein (P-gp) or Breast Cancer Resistance Protein (BCRP) efflux transporters. Preclinical studies have demonstrated significant tumor growth inhibition in various xenograft models, including glioblastoma (GBM) and brain metastases originating from non-small cell lung cancer (NSCLC), colorectal cancer (CRC), and ovarian cancer (OC). The drug is currently in the preclinical/IND-enabling stage of development.