Cetrorelix (Cetrotide)
Overview
A synthetic decapeptide GnRH antagonist that competitively blocks pituitary GnRH receptors, producing immediate and dose-dependent suppression of LH and FSH without the initial flare effect seen with GnRH agonists. Cetrorelix prevents premature LH surges during controlled ovarian stimulation in IVF, allowing precise timing of oocyte maturation and retrieval.
Key Research Findings
FDA-approved for prevention of premature LH surges in women undergoing controlled ovarian stimulation for IVF. GnRH antagonist protocols (including cetrorelix) associated with significantly lower risk of ovarian hyperstimulation syndrome (OHSS) compared to agonist protocols. Flexible dosing allows initiation when lead follicle reaches 14 mm, reducing treatment burden.
Subcutaneous injection
FDA Approved
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FDA ApprovedA synthetic nonapeptide GnRH agonist approximately 15-fold more potent than native GnRH. After an initial stimulatory phase (flare effect) lasting 1-2 weeks, chronic leuprolide administration downregulates pituitary GnRH receptors, resulting in profound suppression of LH, FSH, and downstream sex steroids. This chemical castration effect is exploited in treating hormone-sensitive cancers, endometriosis, and precocious puberty.
Goserelin (Zoladex)
FDA ApprovedA synthetic decapeptide GnRH agonist administered as a biodegradable subcutaneous implant that provides sustained drug release over 1 or 3 months. Like other GnRH agonists, goserelin initially stimulates and then suppresses the HPG axis, reducing sex hormone production to castrate or postmenopausal levels. The implant formulation eliminates the need for repeated injections and ensures compliance.
Ganirelix
FDA ApprovedA synthetic decapeptide GnRH antagonist that competitively and reversibly blocks GnRH receptors on pituitary gonadotroph cells. Ganirelix rapidly suppresses LH secretion within hours of administration, preventing premature ovulation during assisted reproductive technology (ART) cycles. Its mechanism provides immediate suppression without the flare phase associated with GnRH agonists.
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