lucanthone

Lucanthone is an orally available thioxanthone-based small molecule that acts as a DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1 (APEX1 or APE1). It was originally developed and used as a schistosomicide for the treatment of parasitic diseases such as bilharziasis and schistosomiasis, but has largely been replaced by hycanthone and praziquantel. Lucanthone is also a prodrug, metabolized to hycanthone in vivo. In oncology research, it has shown potential antineoplastic activity by inhibiting post-radiation DNA repair in tumor cells, specifically through inhibition of APE1 and topoisomerase II. This leads to un-repaired DNA strand breaks, potentially sensitizing tumor cells to radiation therapy. Additionally, lucanthone can inhibit autophagy via disruption of lysosomal function. It crosses the blood-brain barrier efficiently and has been investigated as a radiation sensitizer for brain tumors[1][2][3][4][7].

Brand names

Miracil D

Other names

Lucanthone hydrochlorideTixantone