Medicinal Organometallic Chemistry pp 1-20

Part of the Topics in Organometallic Chemistry book series (TOPORGAN, volume 32) | Cite as

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

Abstract

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were used for intestinal parasite infections but carcinogenic effects were displayed and all the drugs have been withdrawn in USA, in Europe, and elsewhere.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.

Keywords

Atoxyl Leukemia Melarsoprol Salvarsan Syphilis Trypanosomiasis Tryparsamide 

List of Abbreviations

APL

Acute promyelocytic leukemia

CML

Chronic myeloid leukemia

CNS

Central nervous system

HAT

Human African trypanosomiasis

HIV

Human Immunodeficiency Virus

Mel

Melarsen

Mel B

Melarsoprol

Mel W

Melarsonyl potassium

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Copyright information

© Springer-Verlag Berlin Heidelberg 2010

Authors and Affiliations

  1. 1.EA 3452, Cibles thérapeutiques, formulation et expertise pré-clinique du médicamentNancy Université - Faculté de pharmacieNancyFrance
  2. 2.Ecole Nationale Supérieure de Chimie de ParisLaboratoire Charles Friedel (UMR 7223)Paris Cedex 05France

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