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WSD-0922 is a novel, orally administered, small molecule inhibitor that selectively targets the epidermal growth factor receptor (EGFR) and its mutant forms, including EGFRvIII. It is designed to penetrate the blood-brain barrier and has demonstrated potent antineoplastic activity in preclinical models of glioblastoma. Unlike many other EGFR inhibitors, WSD‑0922 is CNS penetrant and acts as a non‑competitive inhibitor of EGFR. In addition to its primary action on wild-type and mutant EGFR, it also shows specificity for Ephrin receptors, HER4, and Src family kinases—targets associated with resistance to other EGFR tyrosine kinase inhibitors. Preclinical studies have shown that WSD‑0922 provides significant survival benefits in glioblastoma mouse models compared to erlotinib by suppressing tumor growth and inhibiting phosphorylation of proteins linked to resistance mechanisms[1][2][4][8]. The drug is under clinical investigation for central nervous system tumors such as glioblastoma.
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