hycanthone

Hycanthone is a small molecule antischistosomal agent and a metabolite of lucanthone. It was approved by the FDA in 1975 for the treatment of schistosomiasis but is no longer used due to toxicity concerns, particularly hepatotoxicity. Mechanistically, hycanthone acts as an inhibitor of acetylcholinesterase (AChE) in Schistosoma species, interfering with parasite nerve function and causing paralysis and death. It also intercalates into DNA and inhibits RNA synthesis, which underlies its potential antineoplastic activity. Additionally, it inhibits apurinic endonuclease 1 (APE1) by direct protein binding and has been investigated as a topoisomerase II inhibitor in cancer therapy. Clinical development for cancer indications such as colorectal carcinoma and lymphoma reached Phase II but was discontinued due to adverse effects[1][3][5][9].

Brand names

Etrenol

Other names

HycanthonHicantonaHycanthonumLucanthone metabolite1-{[2-(diethylamino)ethyl]amino}-4-(hydroxymethyl)-9H-thioxanthen-9-one