Cetrorelix

Cetrorelix (also known as Cetrorelixum, Cetrotide, Cetrorelixum [INN-Latin], Cetrorelix (INN)) is a anti-aging research peptide. Cetrorelix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used to inhibit premature LH surges in women undergoing controlled ovarian stimulation.

Cetrorelix, also known as Cetrotide, is a synthetic peptide that acts as a gonadotropin-releasing hormone (GnRH) receptor antagonist. It works by blocking the action of GnRH, thereby preventing the premature surge of luteinizing hormone (LH) during controlled ovarian stimulation. This mechanism is crucial in fertility treatments to optimize the timing of egg retrieval. Cetrorelix is FDA-approved for this specific indication and has been studied for ovulation inhibition, ovulation induction, polycystic ovary syndrome, and infertility. Research on cetrorelix frequently focuses on its role in assisted reproductive technology (ART) protocols and its efficacy in managing conditions like uterine fibroids and hyperandrogenism.

1 Mechanism of action

Gonadotropin-releasing hormone receptor antagonist (antagonist)

Primary targets: Gonadotropin-releasing hormone receptor

2 Reported effects

Effects below are those reported in the published literature cited on this page. They are not claims of clinical benefit and not medical advice.

2.1 Indicated / studied for

• Inhibition of premature LH surges in women undergoing controlled ovarian stimulation
• Ovulation Inhibition
• Ovulation Induction
• Polycystic Ovary Syndrome
• Infertility

2.2 Side effects

• Ovarian Hyperstimulation Syndrome
• Nausea
• Headache
• Local site reactions (redness, erythema, bruising, itching, swelling, pruritus)
• Hypersensitivity reactions including anaphylactoid reactions

3 Chemical and physical properties

4 Research dosages

0.25 mg subcutaneously once daily

5 Research studies (8)

1. Efficacy of GnRH antagonists in the treatment of uterine fibroids: a meta-analysis
   Archives of gynecology and obstetrics (2025) · Meta-Analysis
2. What is the optimal GnRH antagonist protocol for ovarian stimulation during ART treatment? A systematic review and network meta-analysis
   Human reproduction update (2023)
3. Cetrorelix suppression test in the diagnostic work-up of severe hyperandrogenism in adolescence
   Journal of pediatric endocrinology & metabolism : JPEM (2008) · Case Series
4. LHRH antagonists
   Pharmaceutical biotechnology (1998) · Review
5. Cetrorelix in reproductive medicine
   F&S reports (2023)
6. Arzneimittelentwicklung in der Onkologie. Status und Ausblick unter besonderer Berucksichtigung des Standortes Deutschland
   Arzneimittel-Forschung (2000)
7. Cetrorelix promotes cell apoptosis via the PI3K-AKT-FOXO1 pathway in epithelial ovarian cancer
   Frontiers in oncology (2025)
8. GnRH Peptide Antagonist: Comparative Analysis of Chemistry and Formulation with Implications for Clinical Safety and Efficacy
   Pharmaceuticals (Basel, Switzerland) (2024) · Review

6 Safety and risk profile

6.1 Regulatory status

Cetrorelix is currently classified as FDA approved. Approval applies to specific clinical indications and dosing; research-grade material is not the approved product.

6.2 Contraindications

Conditions and populations in which use is contraindicated:

• Hypersensitivity to cetrorelix acetate, extrinsic peptide hormones or mannitol
• Known hypersensitivity to GnRH or any other GnRH analogs
• Known or suspected pregnancy
• Lactation
• Severe renal impairment

6.3 Research best practices

• Store refrigerated, 2-8C (36-46F)
• Store in the outer carton to protect from light

7 Frequently asked questions

What is cetrorelix used for?

Cetrorelix is primarily used for the inhibition of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian stimulation as part of fertility treatments. It is also studied for other applications such as ovulation inhibition, ovulation induction, polycystic ovary syndrome, and infertility.

How does cetrorelix work?

Cetrorelix functions as a gonadotropin-releasing hormone (GnRH) receptor antagonist. It works by binding to and blocking the GnRH receptors, which prevents the release of gonadotropins like LH from the pituitary gland. This action helps to prevent premature ovulation during assisted reproductive procedures.

Is cetrorelix FDA approved?

Yes, cetrorelix is FDA approved. It received approval in 1999 for its use in fertility treatments to prevent premature LH surges in women undergoing controlled ovarian stimulation.

What are the side effects of cetrorelix?

Common side effects of cetrorelix include ovarian hyperstimulation syndrome, nausea, and headache. Local site reactions such as redness, erythema, bruising, itching, swelling, and pruritus at the injection site are also reported. Hypersensitivity reactions, including anaphylactoid reactions, have occurred during post-marketing surveillance.

What should be avoided when taking cetrorelix?

Cetrorelix is contraindicated in individuals with hypersensitivity to cetrorelix acetate, extrinsic peptide hormones, mannitol, GnRH, or any other GnRH analogs. It should also not be used during known or suspected pregnancy, lactation, or in patients with severe renal impairment.

8 References

1. Cetrorelix — compound summary PubChem. View source
2. Cetrorelix — molecule record ChEMBL. View source
3. Cetrorelix — FDA approved prescribing information U.S. Food and Drug Administration. View source
4. Cetrorelix — published literature (575 records) PubMed. View source

9 See also

• Peptide encyclopedia index
• Peptide reconstitution calculator
• Glossary of peptide research terms