Medicinal Organometallic Chemistry

Volume 32 of the series Topics in Organometallic Chemistry pp 1-20


Arsenic-Based Drugs: From Fowler’s Solution to Modern Anticancer Chemotherapy

  • Stéphane GibaudAffiliated withEA 3452, Cibles thérapeutiques, formulation et expertise pré-clinique du médicament, Nancy Université - Faculté de pharmacie Email author 
  • , Gérard JaouenAffiliated withEcole Nationale Supérieure de Chimie de Paris, Laboratoire Charles Friedel (UMR 7223)

* Final gross prices may vary according to local VAT.

Get Access


Although arsenic is a poison and has a predominantly unfavorable reputation, it has been used as pharmaceutical agent since the first century bc. In 1786, Thomas Fowler reported the effects of arsenic in the cure of agues, remittent fevers, and periodic headaches. From this time on and despite abusive use, some interesting indications began to appear for trypanosomiasis, syphilis, and blood diseases. The first significant organoarsenical drug (atoxyl) was synthesized by Pierre Antoine Béchamp in 1859 by chemically reacting arsenic acid with aniline but additional experimentations on the properties of arsenic led Paul Ehrlich, the founder of chemotherapy, to the discovery of salvarsan in 1910. From the Second World War, Ernst A.H. Friedheim greatly improved the treatment of trypanosomiasis by melaminophenyl arsenicals. Until the 1990s some organoarsenicals were used for intestinal parasite infections but carcinogenic effects were displayed and all the drugs have been withdrawn in USA, in Europe, and elsewhere. In 2003, arsenic trioxide (Trisenox®) was re-introduced for the treatment of very specific hematological malignancies.


Atoxyl Leukemia Melarsoprol Salvarsan Syphilis Trypanosomiasis Tryparsamide