GX-BP1 + osimertinib

GX-BP1 + osimertinib is an investigational combination of Genexine's GX-BP1 (formerly EPD-301) and AstraZeneca's osimertinib (Tagrisso). GX-BP1 is a first-in-class bioPROTAC (protein-based targeted protein degrader) designed to degrade the transcription factor SOX2 through the ubiquitin-proteasome system. SOX2 is a key driver of cancer stemness, treatment resistance, recurrence, and metastasis. Osimertinib is a small-molecule, third-generation epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor approved for EGFR-mutant non-small cell lung cancer (NSCLC). In EGFR-mutant lung cancer cells, osimertinib treatment has been shown to increase SOX2 expression, contributing to drug resistance and tumor relapse. Preclinical studies have demonstrated that combining GX-BP1 with osimertinib prevents tumor relapse and eliminates cancer stem cell populations, offering a potential therapeutic strategy to overcome osimertinib resistance in EGFR-mutant lung cancers.

Other names

EPD-301 + AZD9291EPD-301 + TagrissoEPD-301 + osimertinibGX-BP1 + AZD9291GX-BP1 + TagrissoGX-BP1 and osimertinibGX-BP-1 and osimertinibGX-BP 1 and osimertinibosimertinib + GX-BP1