The arsphenamine, more known as Salvarsan and 606, is a drug used in the first half of the 20th century against syphilis and trypanosomiasis. This arsenical compound is often regarded as the first modern chemotherapeutic agent.
Arsenic derivatives are known for a long time for their therapeutic properties, but for their toxicity, when, in 1863, Antoine Béchamp synthesizes a compound of arsenic aniliné and the named atoxyl to mark its relatively low toxicity. In 1902, German doctors introduce the atoxyl in the treatment of certain skin diseases. In 1905, a Canadian and an Austrian discover that it is effective against the sleeping sickness. Yet, the toxic effects are still far too high, and the drug is soon abandoned.
However, the discovery of the atoxyl on trypanosome activity has attracted the attention of the German bacteriologist Paul Ehrlich. With the Alfred Bertheim chemist and bacteriologist Sahachiro Hata, he began to rework the molecule. He synthesized and experimented with more than nine hundred derivatives, including the six hundred sixth, so called 606 and Ehrlich and Hata sign all the discovery in 1908, is introduced in 1911 against syphilis and is of a very high efficiency. Improved secondarily in Néosalvarsan (néoarsphénamine), and Mapharsen (arsphénoxide), the rest for a decade product reference of syphilis treatment.
The success of the Salvarsan having relaunched the search, many new arsenical drugs are introduced in the following years, such as the tryparsamide of Jacobs and Heidelberger (1919), the stovarsol (1921) and the orsanine (1925) furnace, then the Friedheim melarsoprol (1949).
Although abandoned in turn as too toxic, the Salvarsan, directly derived from the Béchamp atoxyl, marks an essential step in the development of the chemistry of drug synthesis. It is often considered the first modern chemotherapeutic agent and Ehrlich is honored by many as “the father of chemotherapy.”