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

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Medicinal Organometallic Chemistry

Part of the book series: Topics in Organometallic Chemistry ((TOPORGAN,volume 32))

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were used for intestinal parasite infections but carcinogenic effects were displayed and all the drugs have been withdrawn in USA, in Europe, and elsewhere.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

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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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Acknowledgments

The authors are thankful to Miss Amy Jones (University of Glasgow) for improving the manuscript.

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Authors and Affiliations

  1. EA 3452, Cibles thérapeutiques, formulation et expertise pré-clinique du médicament, Nancy Université - Faculté de pharmacie, 5, rue Albert Lebrun, 54000, Nancy, France

    Stéphane Gibaud

  2. Ecole Nationale Supérieure de Chimie de Paris, Laboratoire Charles Friedel (UMR 7223), 11, rue Pierre et Marie Curie, 75231, Paris Cedex 05, France

    Gérard Jaouen

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  1. Stéphane Gibaud
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Correspondence to Stéphane Gibaud .

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  1. Chimie de Paris (ENSCP), Ecole Nationale Superieure de, rue Pierre et Marie Curie 11, Paris CX 05, 75231, France

    Gérard Jaouen

  2. LS für Anorganische Chemie I -, Bioanorganische Chemie, Universität Bochum, Universitätsstr. 150, Bochum, 44801, Germany

    Nils Metzler-Nolte

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Gibaud, S., Jaouen, G. (2010). Arsenic-Based Drugs: From Fowler’s Solution to Modern Anticancer Chemotherapy. In: Jaouen, G., Metzler-Nolte, N. (eds) Medicinal Organometallic Chemistry. Topics in Organometallic Chemistry, vol 32. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-13185-1_1

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