GnRH system (gonadorelin analogs)
GnRH (gonadotropin-releasing hormone, gonadorelin) governs the pituitary release of LH and FSH and thereby the sex hormones. Synthetic GnRH peptides act either as agonists (initial 'flare', then sustained suppression via receptor downregulation) or as antagonists (immediate suppression without a flare). GnRH analogs are used in prostate cancer, endometriosis, precocious puberty and assisted reproduction (IVF).
Peptides on this topic
10 peptides researched for this topicBuserelin is a synthetic GnRH agonist (including as a nasal spray). It is used in endometriosis, hormone-dependent prostate cancer and assisted reproduction; approved in Europe (Suprefact), not in the US.
- Human RCTSuppresses sex hormones after an initial flare — the basis of efficacy in endometriosis and prostate cancer.
Cetrorelix is a synthetic decapeptide and GnRH antagonist. It is used in assisted reproduction (IVF) to prevent a premature LH surge during controlled ovarian stimulation.
- Human RCTReliably prevents the premature LH surge — and thus premature ovulation — in IVF protocols.
Degarelix (trade name Firmagon) is a synthetic decapeptide and a gonadotropin-releasing hormone (GnRH) receptor antagonist. Unlike GnRH agonists, it blocks the receptor directly and does not trigger an initial testosterone surge (flare). It is an approved prescription medicine for the treatment of advanced, hormone-dependent prostate cancer. This page neutrally summarizes the evidence base and legal status and is not a usage or dosing recommendation.
- Human RCTIn a randomized phase III study, degarelix lowered testosterone without the initial surge (flare) seen with GnRH agonists and achieved castrate-range suppression over the study year, comparable to leuprorelin.
Ganirelix is a synthetic decapeptide and GnRH antagonist. In assisted reproduction (IVF) it prevents the premature LH surge during controlled ovarian stimulation.
- Human RCTReliably prevents the premature LH surge in IVF protocols.
Gonadorelin is the synthetic decapeptide with an amino-acid sequence identical to endogenous gonadotropin-releasing hormone (GnRH/LHRH). Historically approved in several countries for diagnostic testing of pituitary function and for fertility indications (pump systems). A defining feature is the opposite effect of pulsatile versus continuous administration: pulsatile stimulates, continuous leads to receptor desensitisation.
- Human trialPulsatile delivery via a pump system induced spermatogenesis in men with congenital hypogonadotropic hypogonadism, earlier than under cyclical gonadotropin therapy in a comparative study
Goserelin is a synthetic decapeptide and an agonist of gonadotropin-releasing hormone (GnRH). The medical literature describes it as a hormonal agent that suppresses the release of sex hormones through sustained receptor stimulation. Regulatory-approved indications include prostate cancer, advanced breast cancer, endometriosis, and endometrial thinning, among others.
- Human trialHuman studies observed suppression of circulating sex hormones down to castration levels.
Histrelin is a nonapeptide GnRH agonist delivered as a once-yearly implant. Approved for central precocious puberty in children (Supprelin LA) and advanced prostate cancer (Vantas).
- Human RCTSuppresses sex hormones via a yearly implant — in precocious puberty and prostate cancer.
Leuprorelin (also leuprolide) is a synthetic nonapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH). It is an approved prescription medicine in several jurisdictions, including for advanced prostate cancer, endometriosis, uterine fibroids and central precocious puberty. This page neutrally summarizes the evidence base and legal status and is not a usage or dosing recommendation.
- Human RCTWith continuous exposure, LH and FSH are suppressed, with subsequent lowering of sex steroids.
Nafarelin is a GnRH agonist and the only member of this class delivered as a nasal spray. It is approved for treating endometriosis and central precocious puberty.
- Human RCTRelieves endometriosis symptoms and shrinks endometriotic lesions through hormone suppression.
Synthetic decapeptide GnRH agonist with increased affinity over native gonadotropin-releasing hormone. FDA- and EMA-approved since the 1980s for prostate cancer, endometriosis and precocious puberty.
- Human RCTSuppression of testosterone into the castration range (<50 ng/dL) within 4 weeks in men with prostate cancer documented