Human Reproduction Update, Vol.6, No.4 pp.322-331, 2000
© European Society of Human Reproduction and Embryology 2000; all rights reserved
The LHRH antagonist Cetrorelix: a review
1 Corporate Research and Development, ASTA Medica AG, D-60314 Frankfurt, Germany, 2 Endocrine, Polypeptide and Cancer Institute, Veterans Affairs Medical Center and Section of Experimental Medicine, Tulane University School of Medicine, New Orleans, LA, USA 3 Hôpital Saint Antoine, Assistance Hôpitaux Pb, F-75021 Paris, France
To whom correspondence should be addressed at: T. Reissmann, Corporate Research and Development, ASTA Medica AG, Weismüllerstraße 45, D-60314 Frankfurt, Germany. Phone: +49-(0)69-4001-2822; Fax: +49-(0)69-4001-2777; e-mail: Dr_Thomas.Reissmann{at}astamedica.de
Abstract
In those clinical situations in which an immediate and profound suppression of gonadotrophins is desired, LHRH agonists have the disadvantage of producing an initial stimulatory effect on hormone secretion. Therefore, the use of GnRH antagonists which cause an immediate and dose-related inhibition of LH and FSH by competitive blockade of the receptors is much more advantageous. One of the most advanced antagonist produced to date is Cetrorelix, a decapeptide which has been shown to be safe and effective in inhibiting LH and sex-steroid secretion in a variety of animal species and in clinical studies as well. Clinical trials in patients suffering from advanced carcinoma of the prostate, benign prostate hyperplasia, and ovarian cancer are currently in progress and have already shown the usefulness of this new treatment modality. In particular, the concept that a complete suppression of sex-steroids may not be necessary in indications such as uterine fibroma, endometriosis and benign prostatic hyperplasia represents a promising novel perspective for treatment of these diseases. Following completion of phase III trials in controlled ovarian stimulation for IVF regimens, Cetrorelix was given marketing approval and, thus, became the first LHRH antagonist available clinically.
Key words: benign prostatic hyperplasia / cancer treatment / GnRH antagonist / gonadotrophins / ovarian stimulation
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