Cetrorelix is a synthetic polypeptide that functions as a gonadotropin-releasing hormone (GnRH) antagonist. This peptide is primarily used as a hormone regulator for treating fertility issues such as infertility, subfertility, and endometriosis, as well as other medical conditions that require regulation of sex hormones, such as prostate cancer. Cetrorelix works by binding to the GnRH receptors located on the pituitary gland, which then prevents the release of gonadotropins like follicle-stimulating hormone (FSH) and luteinizing hormone (LH). This suppression results in a decrease in the production of sex hormones like testosterone and estrogen. In women, decreased estrogen production helps control ovulation timing, and in men, decreased testosterone production helps manage conditions related to excess of this hormone.
Usage And Benefits Of Using Cetrorelix
In women with fertility issues, when undergoing in vitro fertilization (IVF), the goal is to precisely ensure that the eggs are retrieved at the right moment for fertilization. Normally, after the release of GnRH by the pituitary gland, the ovaries are stimulated to produce the eggs and release them at the right time. However, in some women, the ovulation happens too early for the eggs to be retrieved, which results in the loss of eggs.
Cetrorelix is used to prevent premature ovulation during an IVF cycle. Its main benefit is that it allows for better timing of ovulation and more precise control over the whole IVF cycle overall. Using Cetrorelix improves the chances of successful egg retrieval and, therefore, fertilization. It is typically given to women during the stimulation phase of the IVF cycle (when the ovaries are being stimulated with FSH in order to develop multiple eggs), in the form of a daily injection. In some cases, Cetrorelix can be administered just once in the form of a single-dose injection.
In men with prostate cancer, testosterone acts as a stimulant to the cancer cells, promoting their rapid growth and multiplication. Therefore, one of the basic principles of treating prostate cancer is to reduce the amount of circulating testosterone in the body through various hormone therapies, one of which is Cetrorelix. It is important to note that this is not the intended use of this peptide, and therefore, it classifies as off-label use.
Cetrorelix can be used as a part of androgen deprivation therapy (ADT). Its notable benefit is that it effectively blocks the signals that lead to testosterone production, which is of great significance to the overall management of prostate cancer, especially in cases where the cancer is advanced or metastatic. It is administered as a subcutaneous injection in combination with another GnRH agonist or other prostate cancer treatments.
It is important to note that, despite its overall efficacy and safety, Cetrorelix should only be used under the supervision of a licensed healthcare provider who can adequately adjust the dosage and react accordingly if any side effects occur during the treatment.
Current Research on Cetrorelix
Cetrorelix has been heavily researched, as its properties have made it a promising solution for treating infertility and endometriosis by controlled ovarian stimulation, as well as prostate cancer and benign prostatic hyperplasia by reducing the effects of testosterone on both the epithelial and stromal cells of the prostate. This peptide has been the subject of various studies that have further explored its applications in reproductive medicine and urology in order to examine its efficacy, optimal applications, and overall safety for general use.
A randomized study from 2005 compared the use of Cetrorelix, a GnRH antagonist, with Busereline, a GnRH agonist, in controlled ovarian stimulation for in vitro fertilization. The results have indicated that the agonist approach shows the need for a longer duration of stimulation and suppression than the antagonist approach, which ultimately proves the Cetrorelix to be more efficient for use in IVF. Clinical pregnancy rates were comparable between the groups per attempt and per transfer.
Another study from 1998 investigated the efficacy and safety of using Cetrorelix for treating symptomatic benign prostatic hyperplasia. Patients who have received this treatment have quickly reported significant improvements in urinary symptoms, sexual function, and overall quality of life. There was a notable reduction in the volume of the prostate. Serum levels of testosterone have been consistently inhibited during the therapy and have quickly returned to normal shortly after the therapy cessation. The results of this study have exceeded expectations in terms of safety and efficacy and have proven Cetrorelix to be a reliable solution for long-term improvement in patients with this condition.
Summary
Cetrorelix is a man-made hormone that works as a GnRH antagonist and is used to lower the (predominantly negative) effects of sex hormones such as estrogen and testosterone on the body. It does so by inhibiting the release of GnRH, which results in reduced levels of FSH and LH. Cetrorelix is mainly known for its use in IVF treatments to prevent premature ovulation and help control the timing and the conditions of egg retrieval. This peptide can also be used for treating certain health conditions in men such as prostate cancer and benign prostatic hyperplasia, in which it plays the major role of reducing the stimulating effects of testosterone on the epithelial and stromal cells of the prostate. Despite its efficacy and overall safety, this peptide should only be used under the guidance of a licensed healthcare professional, specialized in reproductive medicine or urology.
Resources:
- Guillemin R. Purification, isolation, and primary structure of the hypothalamic luteinizing hormone-releasing factor of ovine origin. A historical account. Am J Obstet Gynecol. 1977;129:214–218. doi: 10.1016/0002-9378(77)90749-9. [DOI] [PubMed] [Google Scholar]
- Reissmann T., Felberbaum R., Diedrich K., Engel J., Comaru-Schally A.M., Schally A.V. Development and applications of luteinizing hormone-releasing hormone antagonists in the treatment of infertility: an overview. Hum Reprod. 1995;10:1974–1981. doi: 10.1093/oxfordjournals.humrep.a136219. [DOI] [PubMed] [Google Scholar]
- Schally A.V. New approaches to the therapy of various tumors based on peptide analogues. Horm Metab Res. 2008;40:315–322. doi: 10.1055/s-2008-1073142. [DOI] [PubMed] [Google Scholar]
- Reissmann T., Schally A.V., Bouchard P., Riethmiiller H., Engel J. The LHRH antagonist cetrorelix: a review. Hum Reprod Update. 2000;6:322–331. doi: 10.1093/humupd/6.4.322. [DOI] [PubMed] [Google Scholar]
- Diedrich K., Diedrich C., Santos E., Zoll C., al-Hasani S., Reissmann T., et al. Suppression of the endogenous luteinizing hormone surge by the gonadotrophin-releasing hormone antagonist Cetrorelix during ovarian stimulation. Hum Reprod. 1994;9:788–791. doi: 10.1093/oxfordjournals.humrep.a138597. [DOI] [PubMed] [Google Scholar]
- Albano C., Felberbaum R.E., Smitz J., Riethmüller-Winzen H., Engel J., Diedrich K., et al. Ovarian stimulation with HMG: results of a prospective randomized phase III European study comparing the luteinizing hormone-releasing hormone (LHRH)-antagonist cetrorelix and the LHRH-agonist buserelin. European Cetrorelix Study Group. Hum Reprod. 2000;15:526–531. doi: 10.1093/humrep/15.3.526. [DOI] [PubMed] [Google Scholar]
- Devroey P., Polyzos N.P., Blockeel C. An OHSS-Free Clinic by segmentation of IVF treatment. Hum Reprod. 2011;26:2593–2597. doi: 10.1093/humrep/der251. [DOI] [PubMed] [Google Scholar]
- Devroey P., Adriaensen P. OHSS Free Clinic. Facts Views Vis Obgyn. 2011;3:43–45. [PMC free article] [PubMed] [Google Scholar]
- Al-Inany H.G., Abou-Setta A.M., Aboulghar M. Gonadotrophin-releasing hormone antagonists for assisted conception. Cochrane Database Syst Rev. 2006;19:CD001750. doi: 10.1002/14651858.CD001750.pub2. [DOI] [PubMed] [Google Scholar]
- Griesinger G., Diedrich K., Devroey P., Kolibianakis E.M. GnRH agonist for triggering final oocyte maturation in the GnRH antagonist ovarian hyperstimulation protocol: a systematic review and meta-analysis. Hum Reprod Update. 2006;12:159–168. doi: 10.1093/humupd/dmi045. [DOI] [PubMed] [Google Scholar]
- Bosch E., Broer S., Griesinger G., Grynberg M., Humaidan P., Kolibianakis E., et al. ESHRE guideline: ovarian stimulation for IVF/ICSI. Hum Reprod Open. 2020;2020 doi: 10.1093/hropen/hoaa009. hoaa009. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Howles C.M. The place of gonadotrophin-releasing hormone antagonists in reproductive medicine. Reprod Biomed Online. 2002;4:64–71. doi: 10.1016/s1472-6483(12)60120-5. [DOI] [PubMed] [Google Scholar]
- Ludwig M., Albano C., Olivennes F., Felberbaum R.E., Smitz J., Ortmann O., et al. Plasma and follicular fluid concentrations of LHRH antagonist cetrorelix (Cetrotide) in controlled ovarian stimulation for IVF. Arch Gynecol Obstet. 2002;266:12–17. doi: 10.1007/pl00007490. [DOI] [PubMed] [Google Scholar]
- Leroy I., d'Acremont M., Brailly-Tabard S., Frydman R., de Mouzon J., Bouchard P. A single injection of a gonadotropin-releasing hormone (GnRH) antagonist (Cetrorelix) postpones the luteinizing hormone (LH) surge: further evidence for the role of GnRH during the LH surge. Fertil Steril. 1994;62:461–467. doi: 10.1016/s0015-0282(16)56932-5. [DOI] [PubMed] [Google Scholar]
- Engel J.B., Schultze-Mosgau A., Diedrich K. Five years' clinical use of GnRH antagonists: evaluation of safety and allergic potential. Reprod Biomed Online. 2005;10:61–65. doi: 10.1016/s1472-6483(11)60392-1. [DOI] [PubMed] [Google Scholar]