Ganirelix

Ganirelix (also known as Orgalutran, Ganirelixum, Antagon, Ganirelix (INN)) is a anti-aging research peptide. Ganirelix is a gonadotropin-releasing hormone (GnRH) receptor antagonist used to inhibit premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation.

Ganirelix is a synthetic decapeptide that functions as a gonadotropin-releasing hormone receptor antagonist. It works by competitively blocking GnRH receptors in the pituitary gland, thereby suppressing the release of gonadotropins like LH and follicle-stimulating hormone (FSH). This action is crucial in assisted reproductive technologies (ART) to prevent premature ovulation during controlled ovarian hyperstimulation. Ganirelix is FDA-approved and has been studied for female infertility and assisted reproductive techniques. Research also explores its role in polycystic ovary syndrome and optimal GnRH antagonist protocols for ovarian stimulation.

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 hyperstimulation
• Female Infertility
• Assisted Reproductive Techniques

2.2 Side effects

• Abdominal Pain (gynecological)
• Fetal Death
• Headache
• Ovarian Hyperstimulation Syndrome
• Vaginal Bleeding
• Injection Site Reaction
• Nausea
• Abdominal Pain (gastrointestinal)

3 Chemical and physical properties

4 Research dosages

250 mcg subcutaneously once daily

5 Research studies (8)

1. Ganirelix
   Drugs (2000) · Review
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. LHRH antagonists
   Pharmaceutical biotechnology (1998) · Review
4. GnRH-receptor antagonism as a targeted approach to reproductive dysfunction in polycystic ovary syndrome
   EBioMedicine (2026)
5. The gonadotrophin-releasing hormone antagonist ganirelix--history and introductory data
   Human fertility (Cambridge, England) (2002) · Review
6. GnRH Peptide Antagonist: Comparative Analysis of Chemistry and Formulation with Implications for Clinical Safety and Efficacy
   Pharmaceuticals (Basel, Switzerland) (2024) · Review
7. Ganirelix acetate
   American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists (1999)
8. Synthesis and characterization of two potential impurities (des-ethyl-Ganirelix) generated in the Ganirelix manufacturing process
   Journal of peptide science : an official publication of the European Peptide Society (2023)

6 Safety and risk profile

6.1 Regulatory status

Ganirelix 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:

• Known hypersensitivity to ganirelix acetate or any of its components, including dry natural rubber/latex
• Known hypersensitivity to GnRH or any other GnRH analog
• Known or suspected pregnancy

6.3 Research best practices

• Store at 20° to 25°C (68° to 77°F)
• Protect from light
• Discard unused portion

7 Frequently asked questions

What is Ganirelix used for?

Ganirelix is indicated for the inhibition of premature luteinizing hormone (LH) surges in women undergoing controlled ovarian hyperstimulation as part of assisted reproductive technologies. It helps prevent early ovulation, which is important for successful fertility treatments.

How does Ganirelix work?

Ganirelix functions as a gonadotropin-releasing hormone (GnRH) receptor antagonist. It competitively binds to GnRH receptors in the pituitary gland, blocking the natural action of GnRH. This suppression prevents the premature release of LH and FSH, thereby controlling the timing of ovulation during fertility treatments.

Is Ganirelix FDA approved?

Yes, Ganirelix is FDA approved. It received approval in 1999 for its use in fertility treatments, specifically for inhibiting premature LH surges during controlled ovarian hyperstimulation.

What are the side effects of Ganirelix?

Common side effects of Ganirelix include gynecological abdominal pain, headache, ovarian hyperstimulation syndrome, vaginal bleeding, and injection site reactions. Rare cases of hypersensitivity reactions, including anaphylaxis, have also been reported.

How is Ganirelix administered?

Ganirelix is administered by subcutaneous injection. It is typically prescribed by physicians experienced in infertility treatment, and pregnancy must be excluded before starting treatment.

8 References

1. Ganirelix — compound summary PubChem. View source
2. Ganirelix — molecule record ChEMBL. View source
3. Ganirelix — FDA approved prescribing information U.S. Food and Drug Administration. View source
4. Ganirelix — published literature (189 records) PubMed. View source

9 See also

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