Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2023 Feb 24;4(2 Suppl):56-61.
doi: 10.1016/j.xfre.2023.02.009. eCollection 2023 Jun.

Ganirelix and the prevention of premature luteinizing hormone surges

Bernadette Mannaerts  1
Affiliations

Ganirelix and the prevention of premature luteinizing hormone surges

Bernadette Mannaerts. F S Rep. .

Abstract

Ganirelix is a gonadotropin-releasing hormone (GnRH) antagonist with high antagonistic activity that blocks the GnRH receptor by competitive binding. A daily dose of 0.25 mg of ganirelix was sel5ected after a phase II study because it was the minimal, effective daily dose to prevent premature luteinizing hormone surges and this dose yielded the highest ongoing pregnancy rate per started cycle. After subcutaneous administration, ganirelix is rapidly absorbed, reaching peak levels within 1-2 hours (tmax), and has a high absolute bioavailability (>90%). Prospective, comparative studies have demonstrated the advantages of GnRH antagonists over long GnRH agonist treatment in assisted reproduction, including the immediate reversibility of drug effects, a requirement for less follicle-stimulating hormone, a shortened duration of stimulation, a reduced incidence of ovarian hyperstimulation syndrome, and reduced patient burden. Combined analyses concluded that in the general in vitro fertilization population, there is a trend for a slightly lower ongoing pregnancy rate and a lower risk of ovarian hyperstimulation syndrome that is largely eliminated when considering triggering with GnRH agonist instead of human chorionic gonadotropin. Regardless of all the research, it is still not fully elucidated why the long GnRH agonist protocol has a trend for higher pregnancy rates after fresh transfer of the same number of good-quality embryos.

Keywords: GnRH antagonist; OHSS; ganirelix; pregnancy rates; prevention of premature LH surges.

PubMed Disclaimer

Figures

Figure 1
Figure 1
(A) Schematic presentation of the amino acid sequence of native gonadotropin-releasing hormone (GnRH) and ganirelix. (B) A 3-dimensional model of native GnRH and ganirelix.
Figure 2
Figure 2
Mechanism of action of a gonadotropin-releasing hormone (GnRH) agonist and a GnRH antagonist, the latter causing immediate and reversible blockage of the GnRH receptor. LH = luteinizing hormone.
Figure 3
Figure 3
Serum ganirelix levels (upper panel) and serum luteinizing hormone (LH) levels (lower panel) measured just before ganirelix injection in the morning and approximately 8 hours later in the afternoon for patients who received at least 5 days of ganirelix treatment. (Adapted from the ganirelix dose-finding study group [2], 1998.).
Figure 4
Figure 4
The development of gonadotropin-releasing hormone (GnRH) analogue protocols for in vitro fertilization treatment over time. FSH = follicle-stimulating hormone.
See this image and copyright information in PMC

References

    1. Mannaerts B., Gordon K. Embryo implantation and GnRH antagonists: GnRH antagonists do not activate the GnRH receptor. Hum Reprod. 2000;15:1882–1883. - PubMed
    1. A double-blind, randomized, dose-finding study to assess the efficacy of the gonadotrophin-releasing hormone antagonist ganirelix (Org 37462) to prevent premature luteinizing hormone surges in women undergoing ovarian stimulation with recombinant follicle stimulating hormone (Puregon). The ganirelix dose-finding study group. Hum Reprod. 1998;13:3023–3031. - PubMed
    1. Kol S., Lightman A., Hillensjö T., Devroey P., Fauser B., Tarlatzis B., et al. High doses of gonadotrophin-releasing hormone antagonist in in-vitro fertilization cycles do not adversely affect the outcome of subsequent freeze-thaw cycles. Hum Reprod. 1999;14:2242–2244. - PubMed
    1. Simon C., Oberyé J., Bellver J., Vidal C., Bosch E., Horcajadas J.A., et al. Similar endometrial development in oocyte donors treated with either high- or standard-dose GnRH antagonist compared to treatment with a GnRH agonist or in natural cycles. Hum Reprod. 2005;20:3318–3327. - PubMed
    1. Oberyé J.J.L., Mannaerts B.M.J.L., Kleijn H.J., Timmer C.J. Pharmacokinetic and pharmacodynamic characteristics of ganirelix (Antagon/Orgalutran). Part I. Absolute bioavailability of 0.25 mg of ganirelix after a single subcutaneous injection in healthy female volunteers. Fertil Steril. 1999;72:1001–1005. - PubMed

LinkOut - more resources