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Steroidal Antiandrogens

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Hormone Therapy in Breast and Prostate Cancer

Part of the book series: Cancer Drug Discovery and Development ((CDD&D))

Abstract

The era of antiandrogens started in 1962 with a steroidal compound. At that time an attempt was made to find progestogens for the indication of imminent abortion. Since most progestogens exerted androgenic activity, and consequently presented a risk for masculinisation of female fetuses, suitable candidates were investigated for their androgenic potential. It turned out that a derivative of hydroxyprogesterone, cyproterone acetate (CPA), was devoid of intrinsic androgenicity, but caused feminization of male rat fetuses, comparable to the clinical feature of testicular feminization (1). Further experiments revealed the underlying mechanism, and showed that it consisted of a direct inhibition of the action of androgens at the target organ. The inhibition is a result of interaction at the level of the androgen receptor (AR), where CPA competes with the endogenous ligand (2).

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Authors and Affiliations

  1. Department of Urology, Erasmus University and Academic Hospital Rotterdam, Rotterdam, The Netherlands

    Fritz H. Schröder

  2. Clinical Development Oncology, Schering AG, Berlin, Germany

    Albert Radlmaier

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  1. Fritz H. Schröder
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  1. Lombardi Comprehensive Cancer Center, Georgetown University, 3970 Reservoir Rd. NW Research Bldg. E501, Washington, DC, 20057, USA

    V. Craig Jordan

  2. AstraZeneca Pharmaceuticals Zeneca Pharmaceutical, Alderly Park, Alderly House, Macclesfield, SK 10 4TF, UK

    Barrington J.A. Furr

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Schröder, F.H., Radlmaier, A. (2009). Steroidal Antiandrogens. In: Jordan, V.C., Furr, B.J. (eds) Hormone Therapy in Breast and Prostate Cancer. Cancer Drug Discovery and Development. Humana Press. https://doi.org/10.1007/978-1-59259-152-7_15

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  • DOI: https://doi.org/10.1007/978-1-59259-152-7_15

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  • Print ISBN: 978-1-60761-471-5

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