Gonadotropin-releasing hormone agonist

Gonadotropin-releasing hormone agonist
Drug class
Leuprorelin, one of the most widely used GnRH agonists.
Class identifiers
SynonymsGnRH receptor agonists; GnRH blockers; GnRH inhibitors; Antigonadotropins
UseFertility medicine; Prostate cancer; Breast cancer; Menorrhagia; Endometriosis; Uterine fibroids; Hyperandrogenism; Hirsutism; Precocious puberty; Transgender people; Chemical castration for paraphilias and sex offenders
Biological targetGnRH receptor
Chemical classPeptides
Legal status
In Wikidata

A gonadotropin-releasing hormone agonist (GnRH agonist) is a type of medication which affects gonadotropins and sex hormones.[1] They are used for a variety of indications including in fertility medicine and to lower sex hormone levels in the treatment of hormone-sensitive cancers such as prostate cancer and breast cancer, certain gynecological disorders like heavy periods and endometriosis, high testosterone levels in women, early puberty in children, as a part of transgender hormone therapy, and to delay puberty in transgender youth among other uses. It is also used in the suppression of spontaneous ovulation as part of controlled ovarian hyperstimulation, an essential component in IVF. GnRH agonists are given by injections into fat, as implants placed into fat, and as nasal sprays.

Side effects of GnRH agonists are related to sex hormone deficiency and include symptoms of low testosterone levels and low estrogen levels such as hot flashes, sexual dysfunction, vaginal atrophy, penile atrophy, osteoporosis, infertility, and diminished sex-specific physical characteristics. They are agonists of the GnRH receptor and work by increasing or decreasing the release of gonadotropins and the production of sex hormones by the gonads. When used to suppress gonadotropin release, GnRH agonists can lower sex hormone levels by 95% in both sexes.[2][3][4][5]

GnRH was discovered in 1971, and GnRH analogues were introduced for medical use in the 1980s.[6][7] Their nonproprietary names usually end in -relin. The most well-known and widely used GnRH analogues are leuprorelin (brand name Lupron) and triptorelin (brand name Decapeptyl). GnRH analogues are available as generic medications. Despite this, they continue to be very expensive.

  1. ^ Magon N (October 2011). "Gonadotropin releasing hormone agonists: Expanding vistas". Indian Journal of Endocrinology and Metabolism. 15 (4): 261–7. doi:10.4103/2230-8210.85575. PMC 3193774. PMID 22028996.
  2. ^ Hemat RA (2 March 2003). Andropathy. Urotext. pp. 120–. ISBN 978-1-903737-08-8.
  3. ^ Becker KL (2001). Principles and Practice of Endocrinology and Metabolism. Lippincott Williams & Wilkins. pp. 973–. ISBN 978-0-7817-1750-2.
  4. ^ Corson SL, Derman RJ (15 December 1995). Fertility Control. CRC Press. pp. 249–250. ISBN 978-0-9697978-0-7.
  5. ^ Novara G, Galfano A, Secco S, Ficarra V, Artibani W (2009). "Impact of surgical and medical castration on serum testosterone level in prostate cancer patients". Urologia Internationalis. 82 (3): 249–55. doi:10.1159/000209352. PMID 19440008.
  6. ^ Gardner DK, Simón C (26 June 2017). Handbook of In Vitro Fertilization (Fourth ed.). CRC Press. pp. 131–. ISBN 978-1-4987-2947-5.
  7. ^ Jameson JL, De Groot LJ (25 February 2015). Endocrinology: Adult and Pediatric E-Book. Elsevier Health Sciences. pp. 2135–. ISBN 978-0-323-32195-2.