Triptorelin Explained

Triptorelin, sold under the brand name Decapeptyl among others, is a medication that acts as an agonist analog of gonadotropin-releasing hormone, repressing expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH).^{[1] [2]}

It is a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH₂) and a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts.

Primary indications include endometriosis,^[3] for the reduction of uterine fibroids, to treat prostate cancer, and to treat male hypersexuality with severe sexual deviation. The drug has also been used off label to delay puberty in patients with gender dysphoria.^[4]

It was patented in 1975 and approved for medical use in 1986.^[5] It is on the World Health Organization's List of Essential Medicines.^[6]

Medical uses

Triptorelin is used to treat prostate cancer as part of androgen deprivation therapy.^[7]

Another common use in the United Kingdom is for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people (in conjunction with estradiol valerate for trans women or testosterone for trans men). Spironolactone and cyproterone acetate are other drugs used by trans people to suppress sex hormones, but these drugs have a completely different mechanism of action.^[8] It can also be used as a puberty blocker^[9] in the case of precocious puberty.^[7]

Triptorelin has been used as a chemical castration agent for reducing sexual urges in sex offenders.^[10]

Drug action

Triptorelin is a gonadorelin analogue, also known as luteinizing hormone releasing analogue (GnRH analogue, LHRH analogue).^[1] The drug binds to receptors in the pituitary gland and stimulates secretion of gonadotropins (namely luteinizing hormone LH and follicle-stimulating hormone FSH). This causes an initial phase of LH and FSH stimulation, prior to down-regulation of the gonadotrophin-releasing hormone receptors, thereby reducing the release of gonadotropins in the long term, which in turn leads to the inhibition of androgen and estrogen production.

Side-effects

General side effects can include:

• Anaphylaxis
• Arthralgia
• Asthenia
• Asthma
• Breast tenderness (males and females)
• Changes in blood pressure
• Changes in breast size
• Depression
• Ovarian cysts
• Mood changes
• Skin rashes
• Hot flushes
• Weight changes

Society and culture

Brand names

Triptorelin is marketed under the brand names Decapeptyl (Ipsen) for treating prostate cancer, endometriosis, uterine myomas, and precocious puberty,^[11] and Diphereline and Gonapeptyl (Ferring Pharmaceuticals).^[12] In the United States, it is sold by Watson Pharmaceuticals as Trelstar ^[13] and by Arbor Pharmaceuticals as Triptodur (an extended-release 6-month depot injection).^[14] In Iran, triptorelin is marketed under the brand name Variopeptyl. In the UK and Germany, it is sold as Salvacyl for the treatment of sexual deviations.^[15]

History

Triptorelin was developed in Andrew V. Schally's lab at Tulane University.^[16] Debiopharm licensed the drug from Tulane in 1982.^[17]

Research

Triptorelin and other antiandrogens may be effective in the treatment of obsessive–compulsive disorder.^[18]

Further reading

• Lahlou N, Carel JC, Chaussain JL, Roger M . Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics . Journal of Pediatric Endocrinology & Metabolism . 13 . Suppl 1 . 723–737 . July 2000 . 10969915 . 10.1515/jpem.2000.13.s1.723 . 3639804 .
• Padula AM . GnRH analogues--agonists and antagonists . Animal Reproduction Science . 88 . 1–2 . 115–126 . August 2005 . 15955640 . 10.1016/j.anireprosci.2005.05.005 .

External links

• Web site: Triptorelin . U.S. National Library of Medicine . Drug Information Portal .

Notes and References

1. Web site: gonadorelin analogue . Encyclopedia.com. 2019-09-21.
2. Book: British National Formulary (BNF) 70. Joint Formulary Committee. Pharmaceutical Press. 2018. 978-0-85711-173-9. London. 635.
3. Leone Roberti Maggiore U, Scala C, Remorgida V, Venturini PL, Del Deo F, Torella M, Colacurci N, Salvatore S, Ferrari S, Papaleo E, Candiani M, Ferrero S . 6 . Triptorelin for the treatment of endometriosis . Expert Opinion on Pharmacotherapy . 15 . 8 . 1153–1179 . June 2014 . 24832495 . 10.1517/14656566.2014.916279 . Informa Healthcare . 23843087 .
4. Cohen D, Barnes H . Gender dysphoria in children: puberty blockers study draws further criticism . BMJ . 366 . l5647 . September 2019 . 31540909 . 10.1136/bmj.l5647 . 202711942 .
5. Book: Fischer J, Ganellin CR . Analogue-based Drug Discovery . 2006 . John Wiley & Sons . 9783527607495 . 514 .
6. Book: ((World Health Organization)) . World Health Organization model list of essential medicines: 22nd list (2021) . 2021 . 10665/345533 . World Health Organization . World Health Organization . Geneva . WHO/MHP/HPS/EML/2021.02 . free .
7. Web site: triptorelin (Intramuscular route). Drugs.com. 11 November 2016.
8. Wylie KR, Fung Jr R, Boshier C, Rotchell M . Recommendations of endocrine treatment for patients with gender dysphoria. Sexual and Relationship Therapy. 24. 2. 175–187. 10.1080/14681990903023306. 2009 . 20471537.
9. Shumer DE, Nokoff NJ, Spack NP . Advances in the Care of Transgender Children and Adolescents . Advances in Pediatrics . 63 . 1 . 79–102 . August 2016 . 27426896 . 4955762 . 10.1016/j.yapd.2016.04.018 .
10. Web site: Study: Drug effectively treats pedophilia . . 11 February 1998 .
11. Web site: Decapeptyl SR 11.25mg (triptorelin pamoate) - Patient Information Leaflet (PIL) - (emc) . 2022-11-14 . www.medicines.org.uk.
12. Web site: Gonapeptyl Depot 3.75 mg - Summary of Product Characteristics (SmPC) - (emc) . 2022-11-14 . www.medicines.org.uk.
13. Web site: Trelstar intramuscular: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing . WebMD . 2022-11-14 . en.
14. Web site: Triptodur Intramuscular: Uses, Side Effects, Interactions, Pictures, Warnings & Dosing . WebMD . 2022-11-14 . en.
15. Web site: Salvacyl®, developed by Debiopharm, is launched in two European countries - a new therapeutic avenue for the treatment of sexual deviations . 2022-11-14 . Debiopharm . 23 June 2009 . en-US.
16. Web site: About Us – Technology Transfer at Tulane University. 4 January 2024 . Tulane University .
17. Web site: Dr. Reddy's Launches Debiopharm's Pamorelin LA in India for the Treatment of Locally Advanced or Metastatic, Hormone-Dependent Prostate Cancer. 4 January 2024 . Fierce Pharma . 7 December 2012 .
18. Nomani H, Mohammadpour AH, Moallem SM, YazdanAbad MJ, Barreto GE, Sahebkar A . Anti-Androgen Drugs in the Treatment of Obsessive-Compulsive Disorder: A Systematic Review . Current Medicinal Chemistry . 27 . 40 . 6825–6836 . December 2019 . 31814547 . 10.2174/0929867326666191209142209 . 208956450 .