AST5902

AST5902 is the principal active metabolite of the third-generation EGFR tyrosine kinase inhibitors alflutinib (also known as furmonertinib or AST2818). AST5902 exhibits **antineoplastic activity** and has similar potency and selectivity for mutant EGFR and HER family kinases as furmonertinib[1][2][3][5][7]. It targets both classical (e.g., L858R, exon 19 deletion, T790M) and uncommon EGFR mutations including exon 20 insertions, and is less potent against wild-type EGFR[2]. The active metabolite is generated primarily by **CYP3A4-mediated N-demethylation** of the parent drug, and significantly contributes to in vivo efficacy due to high plasma exposure and a long half-life[3][5]. Both furmonertinib and AST5902 inhibit not only EGFR (ErbB1) but also HER2 (ErbB2) and HER4 (ErbB4) kinases[2]. AST5902 is not itself approved as a standalone drug but is important to the efficacy and pharmacology of alflutinib/furmonertinib therapy in non-small cell lung cancer with EGFR mutations[2][5][7].

Other names

AST5902 trimesylateAST-5902 trimesylateAST 5902 trimesylate