Pharmacology of Cyproterone Acetate — A Short Review

  • Friedmund Neumann
Conference paper
Part of the ESO Monographs book series (ESO MONOGRAPHS)


Cyproterone acetate (CPA) was the first antiandrogen to be used in clinical practice. The antiandrogenic activity was discovered in 1962/ 1963 — 30 years ago. But the term “antiandrogen” was not really new [for review see 1].


Precocious Puberty Cyproterone Acetate LHRH Agonist Testosterone Propionate Testosterone Propionate 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.


  1. 1.
    Dorfman RI: Anti-androgenic substances. In: Dorfmann RI (ed) Methods in Hormone Research. Academic Press, New York, London 1962, vol II, pp 315–323Google Scholar
  2. 2.
    Dorfman RI: Biological activity of antiandrogens. Br J Derm 1970 (82 Suppl 6): 3–8CrossRefGoogle Scholar
  3. 3.
    Wiechert R and Neumann F: Gestagene Wirksamkeit von 1-Methyl-und 1,2-Methylen-Steroiden. Arzneimittelforschung 1965 (15): 244–246Google Scholar
  4. 4.
    Neumann F and Hamada F: Intrauterine Feminisierung männlicher Ratten-feten durch das stark gestagen wirksame 6-chlor-6-1.2-methylen-17-hy-droxyprogesteronacetat. 10. Symp Dtsch Ges Endokrinol, Springer Verlag, Berlin, Göttingen, Heidelberg 1964Google Scholar
  5. 5.
    Hamada H, Neumann F and Junkmann K: Intrauterine antimaskuline Beeinflussung von Rattenfeten durch ein stark gestagen wirksames Steroid. Acta Endocrinol 1963 (44): 380–388PubMedGoogle Scholar
  6. 6.
    Jensen EV: Remembrance: Gregory Pincus — Catalyst for early receptor studies. Endocrinology 1992 (131): 1581–1582PubMedCrossRefGoogle Scholar
  7. 7.
    Jensen EV and Jacobson HI: Basic guides to the mechanism of estrogen action. Recent Progr Horm Res 1962 (18): 387Google Scholar
  8. 8.
    Fang and Liao S: Antagonistic action of antiandrogens on the formation of a specific dihydrotestosterone-receptor protein complex in rat ventral prostate. Mol Pharmacol 1969 (5): 428–431PubMedGoogle Scholar
  9. 9.
    Becker H, Düsterberg B and Klosterhalfen H: Bioavailability of cyproterone acetate after oral and intramuscular application in men. Urol Int 1980 (35): 381PubMedCrossRefGoogle Scholar
  10. 10.
    Gerhards E, Gutsche H and Riemann J: Biodynamik von Cyproteronacetat nach oraler Verabreichung beim Menschen. Arzneimittelforschung 1973 (13): 1550Google Scholar
  11. 11.
    Bhargawa AS, Seeger A and Günzel P: Isolation and identification of 15-ß-hydroxy cyproterone acetate in dog, monkey and man. Steroids 1977 (30): 407CrossRefGoogle Scholar
  12. 12.
    Speck U, Jentsch D, Kühne G, Schulze PE and Wendt H: Bioverfügbarkeit und Pharmakokinetik von Cyproteronacetat-14C nach Applikation als 50-mg-Tablette. Arzneimittelforschung 1976 (26): 1717PubMedGoogle Scholar
  13. 13.
    Neumann F, von Berswordt-Wallrabe R, Elger W, Steinbeck H, Hahn JD and Kramer M: Aspects of androgen-dependent events as studied by antiandrogens. Recent Prog Horm Res 1970 (26): 337–410PubMedGoogle Scholar
  14. 14.
    Neumann F: Pharmacology and clinical uses of cyproterone acetate. In: Furr BJA and Wakeling A (eds) Pharmacology and Clinical Uses of Inhibitors of Hormone Secretion and Action. Baillière Tindall, London, Philadelphia, Toronto, Mexico City, Sydney, Tokyo, Hong Kong 1987 pp 132–159Google Scholar
  15. 15.
    Neumann F and Töpert M: Pharmacology of antiandrogens. J Steroid Biochem 1986 (25 5B): 885–895CrossRefGoogle Scholar
  16. 16.
    Neumann F and Töpert M: Antiandrogens: Chemistry, pharmacology and experimental basis with special reference to the effect on the skin and its appendages. In: Orfanos CE and Happle R (eds) Hair and Hair Diseases. Springer Verlag, New York, Berlin, Heidelberg 1986 pp 791–826Google Scholar
  17. 17.
    Schleusener A, Albring M and Neumann F: Pharmacology of old and new antiandrogens. In: Jeffcoate SL (ed) Androgens and Ant-Androgen Therapy. John Wiley & Sons, Chichester, New York, Brisbane, Toronto, Singapore 1982 pp 71–93Google Scholar
  18. 18.
    Neumann F and Steinbeck H: Antiandrogens. In: Eichler O, Farah A, Herken H and Welch AD (eds) Handbook of Experimental Pharmacology. Springer Verlag, Berlin, Heidelberg, New York 1974 Vol XXXV/2 pp 235–484Google Scholar
  19. 19.
    Neumann F: The antiandrogen cyproterone acetate: Discovery, chemistry, basic pharmacology, clinical use and tool in basic research. Clin Exp Endocrinol 1994 (102 suppl): 1–32CrossRefGoogle Scholar
  20. 20.
    Neumann F, Steinbeck H and Hahn JD: Hormones and brain differentiation. In: Martini L, Motta M, Fraschini F (eds) The Hypothalamus. Academic Press, New York, London 1970 pp 569–603Google Scholar
  21. 21.
    Neumann F, Elger W and Steinbeck H: Antiandrogens and reproductive development. Philos Trans R Soc Lond B 1970 (259): 179–184CrossRefGoogle Scholar
  22. 22.
    Neumann F and Elger W: Sexual differentiation: Studies with antiandrogens. In: Serio M, Motta M, Zanisi M and Martini L (eds) Sexual Differentiation: Basic and Clinical Aspects. Raven Press, New York 1984 pp 191–208Google Scholar
  23. 23.
    Neumann F and Jacobi GH: Antiandrogens in tumour therapy. In: Furr BJA (ed) Clinics in Oncology. WB Saunders Co Ltd, London, Philadelphia 1982 pp 41–64Google Scholar
  24. 24.
    Tunn U, Senge TH, Schenck B and Neumann F: Effects of cyproterone acetate on experimentally induced canine prostatic hyperplasia. A morphological and histochemical study. Urol Int 1980 (35): 125–140PubMedCrossRefGoogle Scholar
  25. 25.
    Tunn U, Senge TH, Schenck B and Neumann F: Biochemical and histological studies on prostates in castrated dogs after treatment with androstanediol, oestradiol and cyproterone acetate. Acta Endocrinol 1979 (91): 373–384PubMedGoogle Scholar
  26. 26.
    Neumann F, Habenicht UF and Schacher A: Antiandrogens and target cell response — different in vivo effects of cyproterone acetate, flutamide and cyproterone. In: McKerns KW, Aakvaag A and Hanssen V (eds) Regulation of Target Cell Responsiveness. Plenum Press, New York 1984 vol II pp 489–527Google Scholar
  27. 27.
    Furr BJA: The case for pure antiandrogens. In: Furr BJA and Denis L (eds) Clinical Oncology. Baillière Tindall, London, Philadelphia, Sydney, Tokyo, Toronto 1988 pp 581–590Google Scholar
  28. 28.
    Habenicht UF, Witthaus E and Neumann F: Antiandrogens and LH-RH agonists endocrinology in the initial phase of their use. Aktuel Urol 1986 (17): 10–16CrossRefGoogle Scholar
  29. 29.
    Svensson M, Varenhorst E and Kagedal B: Initial administration of cyproterone acetate to prevent the rise of testosterone concentration during treatment with an LHRH agonist in prostatic cancer. Anticancer Res 1986 (6): 379Google Scholar
  30. 30.
    Radlmaier A, Bormacher K and Neumann F: Hitzewallungen bei Endokrintherapie des Prostatakarzinoms: Modellvorstellung zu ihrer Genese. Aktuel Urol 1989 (20): 143–147CrossRefGoogle Scholar
  31. 31.
    Krämer P, Andrzejak-Nolten N, Kalischnigg and Neumann F: Prevention of hot flushes with CPA in the hormonal treatment of prostatic cancer — Results of placebo-controlled double-blind trial. In: Murphy G, Khoury S, Shatelain S and Denis L (eds) Proceedings IIIrd International Symposium on Recent Advances in Urological Cancer — Diagnosis and Treatment, Paris, June 1992. Scientific Communication Intern Ltd, Jersey 1933 pp 111-115Google Scholar
  32. 32.
    Horn HJ: Administration of antiandrogens in hypersexuality and sexual deviations. In: Eichler O, Farah A, Herken H and Welch AD (eds) Androgens II and Antiandrogens. Springer Verlag, Berlin 1974 pp 543–562Google Scholar
  33. 33.
    Neumann F and Schenck B: Antiandrogens: Basic concepts and clinical trials. In: Cunningham GR, Schill WB and Hafez ESE (eds) Regulation of Male Fertility. Martinus Nijhoff Publishers, The Hague, Boston, London 1980 pp 93–104CrossRefGoogle Scholar
  34. 34.
    Ott F and Hoffet H: Beeinflussung von Libido, Potenz und Hodenfunktion durch Antiandrogene. Schweiz Med Wochenschr 1968 (98): 1812–1815PubMedGoogle Scholar
  35. 35.
    Laschet U and Laschet L: Psychopharmacotherapy of sex offenders with cyproterone acetate. Pharmakopsychiatr Neuropsychopharmakol 1971 (4): 99–104Google Scholar
  36. 36.
    Laschet U and Laschet L: Eine neue Möglichkeit der medikamentösen Behandlung dissozialer Jugendlicher. In: Hoffmann W and Katein W (eds) Jugend-Dissozialität. Neckar-Verlag, Villingen 1971 pp 114–117Google Scholar
  37. 37.
    Raspé G (ed) Schering Symposium über Sexualdeviationen und ihre medikamentöse Behandlung. Life Science Monographs 2. Pergamon Press, Vieweg, Oxford, Edinburgh, New York, Toronto, Sydney, Braunschweig 1972Google Scholar
  38. 38.
    Mothes C, Lehnert J, Samimi F and Ufer J: Klinische Prüfung von Cyproteronacetat (Androcur) bei Sexualdeviationen — Gesamtauswertung. Medizinische Mitteilungen (Schering AG) 1973 (2): 26–39Google Scholar
  39. 39.
    Steinbeck H and Neumann F: Effect of cyproterone acetate on puberty. J Reprod Fertil 1971 (26): 59–63PubMedCrossRefGoogle Scholar
  40. 40.
    Hertel P, Kramer M and Neumann F: Einfluß eines Antiandrogens (Cyproteronacetat) auf Knochenwachstum und Knochenreifung männlicher Ratten. Arzneimittelforschung 1969 (19): 1777–1790PubMedGoogle Scholar
  41. 41.
    Burton JL, Laschet U and Shuster S: Reduction of sebum excretion in man by the antiandrogen, cyproterone acetate. Br J Dermatol 1973 (89): 487–490PubMedCrossRefGoogle Scholar
  42. 42.
    Wendt H and Hümmelinck R: The effect of cyproterone acetate on some endocrinological parameters. In: Hammerstein J, Lachnit-Fixson U, Neumann F, Plewig G (eds) Androgenization in Women — Acne, Seborrhoea, Androgenetic Alopecia and Hirsutism. Excerpta Medica, Amsterdam, Oxford, Princeton 1980 pp 259–265Google Scholar
  43. 43.
    Girard J, Helge H, and v. Mühlendahl KE: Treatment of idiopathic precocious puberty with cyproterone acetate. Horm Res (Basel) 1978 (9): 301–312CrossRefGoogle Scholar
  44. 44.
    Poyet P and Labrie F: Comparison of the antiandrogenic/androgenic activities of flutamide, cyproterone acetate and megestrol acetate. Mol Cell Endocrinol 1985 (42): 283–288PubMedCrossRefGoogle Scholar
  45. 45.
    Bridge RW and Scott WW: A new antiandrogen, SH-714. Invest Urol 1964 (2): 99PubMedGoogle Scholar
  46. 46.
    Sugimura Y, Cunha GR and Bigsby RM: Androgenic induction of DNA synthesis in prostatic glands induced in the urothelium of testicular feminized (Tfm/Y) mice. Prostate 1986 (9): 217–225PubMedCrossRefGoogle Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 1996

Authors and Affiliations

  • Friedmund Neumann
    • 1
  1. 1.Ernst Schering Research FoundationBerlinGermany

Personalised recommendations