BPI-361175

BPI-361175 is a novel, oral, highly potent and selective fourth-generation small molecule inhibitor of the epidermal growth factor receptor (EGFR), developed by Betta Pharmaceutical. It is specifically designed to target EGFR mutations that confer resistance to earlier generations of EGFR tyrosine kinase inhibitors (TKIs), including the C797S mutation as well as other related mutations such as L858R, T790M, and exon 19 deletions. By binding to and inhibiting mutant forms of EGFR—including those resistant to third-generation TKIs—BPI-361175 blocks EGFR-mediated signaling pathways, leading to inhibition of tumor cell proliferation and induction of cell death in non-small cell lung cancer (NSCLC) and other solid tumors. Preclinical studies have demonstrated strong inhibitory effects on tumor models harboring these mutations. The drug is currently in early clinical development for advanced NSCLC with relevant EGFR mutations.