bisantrene

Bisantrene is a small molecule anthracenyl bishydrazone with anthracycline-like antineoplastic activity. It acts primarily as a DNA intercalator and topoisomerase II inhibitor, disrupting DNA configuration and causing single-strand breaks, DNA-protein crosslinking, and inhibition of both DNA and RNA synthesis. This results in the inhibition of cancer cell replication. Bisantrene preferentially binds to A-T rich regions of DNA and has demonstrated reduced cardiotoxicity compared to other anthracyclines such as doxorubicin[1][4]. In addition to its cytotoxic effects on tumor cells, recent research has identified bisantrene as a potent inhibitor of the fat mass and obesity-associated protein (FTO), an m^6A RNA demethylase implicated in cancer biology[1]. Bisantrene was originally developed by Lederle Laboratories (a division of American Cyanamid) in the 1970s as an alternative chemotherapeutic agent for cancers including acute myeloid leukemia (AML), breast cancer, ovarian cancer, lymphoma, multiple myeloma, solid tumors such as lung or renal cell carcinoma and melanoma[3][6][7]. It was approved for relapsed/refractory AML in France in 1988 but never marketed due to formulation challenges[3].

Brand names

XanteneZantreneOrange Crush

Other names

bisantrene hydrochloride9,10-anthracenedicarboxaldehyde bis(2-imidazolin-2-ylhydrazone)9,10-anthracenedicarboxaldehyde, bis((4,5-dihydro‑1h‑imidazol‑2‑yl)hydrazone)