BO-1978

BO-1978 is a small molecule indolizino[6,7-b]indole derivative developed as a DNA crosslinking agent. It was identified by researchers at Academia Sinica and National Yang-Ming University as a potential therapeutic for non-small cell lung cancer (NSCLC), particularly cases resistant to tyrosine kinase inhibitors (TKIs) like gefitinib. BO-1978 functions by inducing DNA double-strand crosslinks and modulating the expression of DNA repair proteins, which leads to cell cycle delay in the G1 and S phases. Preclinical studies have demonstrated that BO-1978 effectively suppresses the growth of various lung cancer cell lines harboring EGFR mutations, including the T790M resistance mutation, and significantly inhibits tumor growth in xenograft models.