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BO-1922 is a novel indolizino[6,7-b]indole derivative that acts as a DNA crosslinking agent. Developed by researchers at Academia Sinica and National Yang-Ming University, it is designed to overcome resistance to EGFR tyrosine kinase inhibitors (TKIs) in non-small cell lung cancer (NSCLC). The compound induces DNA double-strand crosslinks, leading to cell cycle accumulation in the G2/M phase and subsequent cell death. In preclinical models, BO-1922 has shown significant growth suppression against various NSCLC cell lines harboring EGFR mutations, including the T790M gatekeeper mutation, and has demonstrated efficacy in gefitinib-resistant xenograft models.
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