[2] It was first discovered in 1921 at Pasteur Institute by Ernest Fourneau,[3] and sold under the brand name Stovarsol.

[3] Acetarsol has been used for the treatment of diseases such as syphilis, amoebiasis, yaws, trypanosomiasisiasis and malaria.

[3] Although the mechanism of action is not fully known, acetarsol may bind to protein-containing sulfhydryl groups located in the parasite, which then creates lethal As-S bonds, which then kills the parasite.

[3] Acetarsol has the molecular formula N-acetyl-4-hydroxy-m-arsinillic acid, and it is a pentavalent arsenical compound with antiprotozoal and anthelmintic properties.

The level of arsenic after acetarsol administration reaches close to the toxic range in urine.