Luteinizing hormone-releasing hormone (GnRH) antagonists competitively block pituitary GnRH receptors, thus leading to an immediate decrease of the circulating levels of follicle stimulating hormone (FSH) and luteinizing hormone (LH) and consequently of sex steroids. They are clinically used when pharmacologically induced hormone suppression is desired, e.g. in sex steroid dependent benign and malignant diseases and for prevention of premature LH surges in assisted reproduction. The article reviews the clinical experience with the well established GnRH antagonists cetrorelix, ganirelix and the approved, but recently withdrawn abarelix. Clinical studies with the new depot formulations of cetrorelix, teverelix, degarelix and D-63153 are summarized.
Keywords: GnRH antagonists, cancer, sex-steroid dependent disease, in vitro fertilization, cetrorelix, review
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