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WSD0922 + fluorouracil is an investigational combination therapy consisting of WSD0922, a potent and selective small molecule inhibitor of the epidermal growth factor receptor (EGFR), and fluorouracil (5-FU), a widely used antimetabolite chemotherapeutic agent. WSD0922 is orally active, blood-brain barrier penetrant, and has demonstrated preclinical efficacy in models of glioblastoma and other central nervous system tumors by inhibiting EGFR signaling pathways associated with tumor growth and resistance to other EGFR inhibitors[6][7][9]. Fluorouracil acts as a pyrimidine analog that interferes with DNA synthesis by inhibiting thymidylate synthase after being metabolized intracellularly[3][4]. The combination aims to leverage the targeted inhibition of EGFR-driven oncogenic signaling by WSD0922 together with the cytotoxic effects on rapidly dividing cells provided by fluorouracil. This regimen is under clinical investigation for primary brain tumors such as glioblastoma and for cancers that have metastasized to the central nervous system[9][10].
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