Abstract
In 1999, the peptidic antagonist of gonadotropin-releasing hormone (GnRH), cetrorelix, was the first compound of this class to be marketed. Cetrorelix is a classic antagonist at the GnRH pituitary receptor. It is used to achieve reversible, dose-dependent suppression of the gonadotropins and the sex steroids. Cetrorelix is approved in over 80 countries including the USA and Japan for the prevention of the premature luteinizing hormone surge in controlled ovarian stimulation (COS) cycles. Using GnRH antagonists instead of GnRH agonists in COS cycles may facilitate infertility treatment. Pregnancy rates after both treatment regimens appear to be similar, while in GnRH-controlled COS cycles a lower rate of side effects such as ovarian hyperstimulation syndrome occur. Cetrorelix may also be useful in minimal stimulation cycles for in vitro fertilization or intrauterine insemination, although further and larger studies are required. Other indications for cetrorelix may be sex steroid-dependent benign and malignant conditions, such as uterine leiyomyoma, endometriosis, benign prostatic hyperplasia, prostate cancer and ovarian cancer, although in these fields cetrorelix still has to be considered as an experimental treatment modality and should only be used within clinical studies. This article summarizes the chemistry, pharmacokinetics, pharmacodynamics, clinical efficacy, safety and tolerability of cetrorelix. Clinical studies in the fields of reproductive medicine, endometriosis, uterine leiyomyoma, benign prostatic hyperplasia, prostate cancer and ovarian cancer are reviewed. The article also provides a brief overview on experimental data of cetrorelix for the treatment of different GnRH receptor-positive tumors, which may present a future indication for cetrorelix.
Disclosure
JB Engel received travel fundings from Zentaris GmbH. L Rieger and J Dietl have no conflict of interest to declare. A Hönig has received travel grants from AstraZeneca, Sanofi Aventis, Pfizer, Amgen, Roche and Pierre Fabre.