Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI) with potent activity against both common activation EGFR and resistance T790M mutations. Additionally, Rezivertinib demonstrates excellent central nervous system (CNS) penetration and exhibits antitumor activity[1][2].

Rezivertinib (BPI-7711) effectively inhibits the proliferation of cells with EGFR mutations, demonstrating selective activity across various cell lines with GI50 values of 13.3 nM (PC9, del19), 6.8 nM (HCC827, L858R), and 22 nM (NCI-H1975, del19/T790M), while showing minimal effect on cells expressing wild-type EGFR with a GI50 of >1000 nM (A431, EGFR WT)[1].

Rezivertinib (BPI-7711; orally administered at dosages ranging from 6.25 to 25 mg/kg/day over a period of 14 days) demonstrates significant tumor regression[2]. When given at a concentration of 12.5 mg/kg/day for the same duration, it results in a 112% increase in the average lifespan of mice in the H1975-luc human NSCLC model[2]. At a higher dosage of 50 mg/kg/day, Rezivertinib exhibits anti-tumor effectiveness, leading to an average survival extension of the test animals by 115% (comparing 28 days to 13 days)[2].