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Research ArticleENDOCRINE AND REPRODUCTIVE

Pharmacological Profile of a New, Potent, and Long-Acting Gonadotropin-Releasing Hormone Antagonist: Degarelix

Pierre Broqua, Pierre J.-M. Riviere, P. Michael Conn, Jean E. Rivier, Michel L. Aubert and Jean-Louis Junien
Journal of Pharmacology and Experimental Therapeutics April 2002, 301 (1) 95-102; DOI: https://doi.org/10.1124/jpet.301.1.95
Pierre Broqua
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Pierre J.-M. Riviere
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P. Michael Conn
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Jean E. Rivier
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Michel L. Aubert
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Jean-Louis Junien
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Abstract

We describe the pharmacological profile in rats and monkeys of degarelix (FE200486), a member of a new class of long-acting gonadotropin-releasing hormone (GnRH) antagonists. At single subcutaneous injections of 0.3 to 10 μg/kg in rats, degarelix produced a dose-dependent suppression of the pituitary-gonadal axis as revealed by the decrease in plasma luteinizing hormone (LH) and testosterone levels. Duration of LH suppression increased with the dose: in the rat, significant suppression of LH lasted 1, 2, and 7 days after a single subcutaneous injection of degarelix at 12.5, 50, or 200 μg/kg, respectively. Degarelix fully suppressed plasma LH and testosterone levels in the castrated and intact rats as well as in the ovariectomized rhesus monkey for more than 40 days after a single 2-mg/kg subcutaneous injection. In comparative experiments, degarelix showed a longer duration of action than the recently developed GnRH antagonists abarelix, ganirelix, cetrorelix, and azaline B. The in vivo mechanism of action of degarelix was consistent with competitive antagonism, and the prolonged action of degarelix was paralleled by continued presence of radioimmunoassayable degarelix in the general circulation. In contrast to cetrorelix and similarly to ganirelix and abarelix, degarelix had only weak histamine-releasing properties in vitro. These results demonstrate that the unique and favorable pharmacological properties of degarelix make it an ideal candidate for the management of sex steroid-dependent pathologies requiring long-term inhibition of the gonadotropic axis.

Footnotes

  • Abbreviations:
    GnRH
    gonadotropin-releasing hormone
    LH
    luteinizing hormone
    Aph
    aminophenylalanine
    Amf
    aminomethylphenylalanine
    RIA
    radioimmunoassay
    ANOVA
    analysis of variance
    • Received September 28, 2001.
    • Accepted December 6, 2001.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics: 301 (1)
Journal of Pharmacology and Experimental Therapeutics
Vol. 301, Issue 1
1 Apr 2002
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Research ArticleENDOCRINE AND REPRODUCTIVE

Pharmacological Profile of a New, Potent, and Long-Acting Gonadotropin-Releasing Hormone Antagonist: Degarelix

Pierre Broqua, Pierre J.-M. Riviere, P. Michael Conn, Jean E. Rivier, Michel L. Aubert and Jean-Louis Junien
Journal of Pharmacology and Experimental Therapeutics April 1, 2002, 301 (1) 95-102; DOI: https://doi.org/10.1124/jpet.301.1.95

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Research ArticleENDOCRINE AND REPRODUCTIVE

Pharmacological Profile of a New, Potent, and Long-Acting Gonadotropin-Releasing Hormone Antagonist: Degarelix

Pierre Broqua, Pierre J.-M. Riviere, P. Michael Conn, Jean E. Rivier, Michel L. Aubert and Jean-Louis Junien
Journal of Pharmacology and Experimental Therapeutics April 1, 2002, 301 (1) 95-102; DOI: https://doi.org/10.1124/jpet.301.1.95
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