Evidence Grade A — Regulatory approved. 571 published studies. 83 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.
Cetrorelix is also known by these brand and alternate names:
571 published studies: 370 human, 142 animal, 168 in-vitro, 46 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.
PeptideTrace tracks 83 registered clinical trials for Cetrorelix sourced from ClinicalTrials.gov.
Administration of Increased Dose of GnRH Antagonist for Coasting for Decreasing the Risk for Ovarian Hyperstimulation Syndrome( OHSS)
Comparison of the Euploid Rate of Blastocyst Between PPOS and GnRH Antagonist Protocol in Women With PCOS Undergoing PGT-A
A Study to Compare the Efficacy and Safety of Follitropin Alfa/Lutropin Alfa Versus hMG in Japanese Participants With LH and FSH Deficiency Undergoing ART (HINATA)
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
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Cetrorelix is a synthetic decapeptide (10 amino acids) GnRH antagonist. It competitively blocks the GnRH receptor without causing an initial hormonal flare. It is formulated as a lyophilized powder for subcutaneous injection.
Cetrorelix binds competitively to GnRH receptors in the anterior pituitary, directly blocking endogenous GnRH-stimulated release of LH and FSH. Onset of LH suppression occurs within approximately 1 hour of the 3 mg dose. Effects are dose-dependent and rapidly reversible—LH/FSH levels recover within 48 hours of the last dose, making it well suited for controlled ovarian stimulation protocols.
Cetrorelix is marketed as Cetrotide (approved August 11, 2000) for prevention of premature LH surges during controlled ovarian stimulation in IVF/ART protocols. Available as 0.25 mg daily dose (multiple-dose protocol) or 3 mg single dose. Used in the GnRH antagonist IVF protocol as an alternative to the longer agonist down-regulation protocol.
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Carbetocin has not been approved by the FDA. It is registered in over 80 countries for prevention of uterine atony and excessive bleeding after caesarean delivery. A heat-stable formulation was added to the WHO Essential Medicines List in 2019. The CHAMPION trial (WHO, 2018; over 29,000 women) compared a heat-stable carbetocin formulation to oxytocin for preventing postpartum haemorrhage after vaginal delivery, and found it to be non-inferior. The heat-stable formulation addresses a significant limitation of oxytocin, which degrades in warm climates without refrigeration — a major concern in low-resource settings where postpartum haemorrhage causes the most deaths. Its regulatory status varies by jurisdiction.
Kisspeptin-54 has no marketing authorisation. Phase II trials conducted primarily at Imperial College London have investigated its use as an IVF oocyte maturation trigger. One trial (60 patients) reported 95% oocyte maturation with zero cases of ovarian hyperstimulation syndrome. Kisspeptin-54 has a more advanced clinical evidence base than kisspeptin-10, with multiple Phase II studies in reproductive medicine. Its potential advantage over conventional IVF triggers relates to a lower risk of the serious complication of ovarian hyperstimulation. Clinical development is ongoing in academic settings. No Phase III trials have been completed.
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.
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