Cetrotide
Evidence Grade A — Regulatory approved. 570 published studies. 69 registered clinical trials.
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Cetrorelix (sold as Cetrotide) is an injectable medication used during IVF and other fertility treatments to prevent the body from ovulating too early, before eggs are ready to be collected. Available as a daily injection or a single higher dose, it gives fertility specialists precise control over timing — a critical factor in the success of assisted reproduction.
570 published studies: 369 human, 141 animal, 168 in-vitro, 45 reviews
Cetrorelix is marketed as Cetrotide (approved 2000) for the prevention of premature ovulation in women undergoing controlled ovarian stimulation for IVF. It is available as a 0.25 mg daily injection or a 3 mg single dose, both administered subcutaneously.
Cetrorelix is used as part of the GnRH antagonist IVF protocol, which has become the dominant approach in fertility clinics worldwide, largely replacing the older GnRH agonist ('long') protocol. The antagonist approach requires fewer injections, a shorter stimulation period, and carries a lower risk of ovarian hyperstimulation syndrome — a potentially serious complication of fertility treatment. Cetrorelix competes directly with ganirelix in this market, with both agents showing equivalent clinical outcomes.
During fertility treatment, the ovaries are stimulated to develop multiple eggs simultaneously. The risk is that the body's natural LH surge triggers ovulation too early, before the eggs can be collected. Cetrorelix directly blocks the GnRH receptor in the pituitary gland, preventing this premature LH surge. Unlike GnRH agonists, which cause an initial hormone spike before suppression, cetrorelix provides immediate suppression with no flare — and its effects reverse quickly once stopped, which is important for the precisely timed sequences required in IVF.
Cetrorelix, along with the similar drug ganirelix, helped establish the GnRH antagonist approach to IVF that is now the dominant protocol worldwide. Multiple large analyses confirm that this approach achieves pregnancy rates comparable to the older, longer protocols while requiring fewer injections, shorter treatment courses, and carrying a lower risk of ovarian hyperstimulation syndrome — a potentially serious complication. No meaningful clinical differences have been demonstrated between cetrorelix and ganirelix; the choice between them is typically driven by local availability, cost, and practical factors like prefilled syringe convenience. Generic versions have improved access. Some research has explored cetrorelix for endometriosis and uterine fibroids, though oral alternatives have largely taken over that research space.
Administration of Increased Dose of GnRH Antagonist for Coasting for Decreasing the Risk for Ovarian Hyperstimulation Syndrome( OHSS)
Trial Comparing Subcutaneous Natural Progesterone (Prolutex) vs. Cetrorelix Acetate for Luteinizing Hormone Surge Suppression in Freeze-All IVF Cycles.
Serum FSH Monitoring for Identification of an Optimal Range During Ovarian Stimulation
Can Drospirenone be Used to Prevent LH Surge in Controlled Ovarian Stimulation in PCOS?!
Potential Benefit of r-hLH Addition in Patients Aged 35 to 40 Under Ovarian Stimulation Treatment
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Histrelin is available as Supprelin LA for central precocious puberty (approved 2007). The Vantas implant for prostate cancer was approved in 2004 but discontinued in 2021. The implant requires a minor surgical procedure for insertion and removal/replacement each year. Supprelin LA's main clinical advantage is its 12-month duration — the longest of any GnRH agonist — which is particularly valuable in paediatric patients where treatment compliance over years is important. Clinical studies demonstrated effective suppression of puberty markers in over 97% of patients. The implant has also seen significant off-label use in gender-affirming care as a puberty blocker, where its annual dosing schedule offers practical benefits for adolescent patients and their families.
Goserelin is marketed as Zoladex by AstraZeneca, available as 3.6 mg monthly and 10.8 mg three-monthly subcutaneous implants. First approved in 1989, it is used in advanced prostate cancer, premenopausal breast cancer, endometriosis, and for thinning the uterine lining before surgical procedures. Goserelin achieves castrate-level testosterone suppression (below 50 ng/dL) within two to four weeks. Its unique implant delivery system means there is no liquid injection, reconstitution, or refrigeration required — a practical advantage in some clinical settings. Like all GnRH agonists, it causes an initial hormone flare before suppression takes effect. Goserelin holds an important niche in breast cancer treatment, where it is used to suppress ovarian function in premenopausal women with hormone-receptor-positive disease, often in combination with aromatase inhibitors.
Nafarelin is marketed as Synarel (approved 1990) for endometriosis and central precocious puberty. It requires administration as one spray in each nostril twice daily — a higher frequency than injectable alternatives but avoids needles entirely, which can be a significant advantage for some patients, particularly children. Clinical trials showed symptom improvement in 75–92% of endometriosis patients. However, absorption can be affected by nasal congestion or concurrent use of nasal decongestants, which can be a practical limitation. As with all GnRH agonists, prolonged use leads to bone density loss, and treatment for endometriosis is typically limited to six months. Nafarelin occupies a niche for patients who prefer non-injectable hormone suppression, though it has become less commonly prescribed as longer-acting depot injections and oral alternatives have become available.
