Triptorelin (2mg)

Triptorelin Peptide

Gonadotropin-releasing hormones (GnRH), secreted by the hypothalamus, are considered by scientists to be responsible for the synthesis and secretion of the follicle-stimulating hormone (FSH) and luteinizing hormone (LH). Fertility is reportedly affected when GnRH pulsatility gets impaired, possibly due to excessive malnutrition, aging, or other reproductive dysfunctions.⁽¹⁾

Triptorelin is a synthetic peptide composed of ten amino acids, similar to gonadotropin-releasing hormones (GnRH).⁽²⁾ Triptorelin acts on the pituitary gland to stimulate the synthesis and release of the LH and FSH hormones, both apparently vital for testosterone production in males and for estrogen synthesis in females.⁽³⁾

Overview

As an agonist analog of gonadotropin releasing hormone (GnRH), Triptorelin has been suggested by researchers to bind to the receptors in the pituitary gland which may then stimulate the secretion of luteinizing hormone (LH)  and follicle-stimulating hormone (FSH). This at first may cause an upsurge in the initial phase of LH and FSH stimulation. Later, as the receptors become less sensitive to the compound (i.e., downregulation of the receptors), it may possibly lead to reduced release of LH and FSH.

Scientists consider that reduction in the levels of LH and FSH hormones eventually leads to decrease in testosterone and estrogen levels. This event may lead to the suppression of steroidogenesis by ovaries and testicles.⁽⁵⁾ Researchers suggest that Triptorelin exhibits some potential in sustaining the decline in the LH and FSH secretion.

Research and Clinical Studies

Triptorelin Peptide and Cancer Cells

In this randomized phase III clinical trial,⁽¹¹⁾ 1,065 premenopausal female test subjects diagnosed with early breast cancer were enrolled. All candidates received Triptorelin as well as either Tamoxifen, Letrozole or Zoledronic acid for five years. After 64 months and follow-up analysis, the disease-free rate in the subjects was reported to be 85%, 93.2% and 93.3% in subjects co-presented with Tamoxifen, Letrozole or Zoledronic acid.

Scientists consider the prostate, a small gland in males, to be the producer and transporter of seminal fluid to sperm.⁽⁷⁾ One method by which scientists are approaching prostate cancer cell mitigation is by depriving androgen production. Through such deprivation, scientists suggest that it deeply impacts plasma levels of testosterone.⁽⁸⁾ As part of one clinical study,⁽⁸⁾ a retrospective analysis was conducted where the impact of 1, 3, and 6-month presentation of the Triptorelin peptide was studied. 920 male subjects with prostate cancer were enrolled in this study. During the 12 months, the testosterone levels were analyzed after 1, 3, 6, 9 and 12 months of peptide presentation. Upon analyzing, it was reported by the researchers that 80%, 92%, 93%, 90% and 91% of subjects (respectively) exhibited lowered plasma testosterone levels.

Triptorelin Peptide and Endometriosis

Scientists characterize endometriosis by uterine tissue growth outside of the womb. Research in this condition suggests it may lead to excessive abdominal pain, heavy menstruation and infertility.⁽⁹⁾ In this clinical trial,⁽¹⁰⁾ 45 women with endometriosis were presented with Triptorelin every 4 weeks. To analyze the peptide potential, parameters such as symptom relief, reduction in endometrium size, hormonal impact, modulations in bone mineral density and regular menstruation were measured after the study. After 8 weeks, the pain associated symptoms had reportedly decreased in all subjects. The levels of FH and LSH had apparently decreased as well, in all subjects, while the cholesterol and triglycerides level reportedly slightly increased.

Triptorelin Peptide and Fertility Preservation

In this clinical study spanning from 2000 to 2015,⁽¹²⁾ 36 female test subjects undergoing chemotherapy who were also presented with Triptorelin were monitored. The subjects were evaluated for long-term ovarian functions – whether there were any signs of damage, miscarriages, and pregnancies. Out of the 36 subjects, 27 of them reportedly maintained optimal ovarian functions, five of whom also achieved a physiological pregnancy. Nine subjects underwent hematopoietic stem cell transplantation (HSCT), four of whom developed ovarian failure.

Triptorelin Peptide and Central Precocious Puberty (CPP)

This was the first clinical study conducted to examine the potential of Triptorelin in Central Precocious Puberty (CPP). The study⁽¹⁴⁾ was conducted for 48 weeks, and the main objective was to achieve LH suppression at prepubertal levels. 44 subjects (39 female and 5 male), never previously observed for CPP, were enrolled in this study. They were all given the peptide twice, with an interval of 24 weeks in between. At the end of this study, it was reported by the researchers that the peptide appeared to cause possible suppression of LH at month 6 and maintained the levels through month 12 in 41 subjects.

Triptorelin peptide is available for research and laboratory purposes only. Please review and adhere to our Terms and Conditions before ordering.

References:

1. Tsutsumi, Rie, and Nicholas J G Webster. “GnRH pulsatility, the pituitary response and reproductive dysfunction.” Endocrine journal vol. 56,6 (2009): 729-37. doi:10.1507/endocrj.k09e-185. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4307809/
2. National Center for Biotechnology Information. PubChem Compound Summary for CID 25074470, Triptorelin. https://pubchem.ncbi.nlm.nih.gov/compound/Triptorelin.
3. LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Triptorelin. https://www.ncbi.nlm.nih.gov/books/NBK548756/
4. Lepor, Herbert. “Comparison of single-agent androgen suppression for advanced prostate cancer.” Reviews in urology vol. 7 Suppl 5 (2005): S3-S12. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1477619/
5. Triptorelin. https://www.drugs.com/ppa/triptorelin.html
6. Triptorelin (Intramuscular Route). https://www.mayoclinic.org/drugs-supplements/triptorelin-intramuscular-route/description/drg-20066536
7. Prostate cancer. https://www.mayoclinic.org/diseases-conditions/prostate-cancer/symptoms-causes/syc-20353087
8. Breul J, Lundström E, Purcea D, Venetz WP, Cabri P, Dutailly P, Goldfischer ER. Efficacy of Testosterone Suppression with Sustained-Release Triptorelin in Advanced Prostate Cancer. Adv Ther. 2017 Feb;34(2):513-523. doi: 10.1007/s12325-016-0466-7. Epub 2016 Dec 27. https://pubmed.ncbi.nlm.nih.gov/28028737/
9. Endometriosis Health Center. https://www.webmd.com/women/endometriosis/default.htm
10. Choktanasiri W, Boonkasemsanti W, Sittisomwong T, Kunathikom S, Suksompong S, Udomsubpayakul U, Rojanasakul A. Long-acting triptorelin for the treatment of endometriosis. Int J Gynaecol Obstet. 1996 Sep;54(3):237-43. https://pubmed.ncbi.nlm.nih.gov/8889631/
11. Francesco Perrone et al, Adjuvant zoledronic acid and letrozole plus ovarian function suppression in premenopausal breast cancer: HOBOE phase 3 randomised trial. June 01, 2019. https://doi.org/10.1016/j.ejca.2019.05.004
12. Meli M, Caruso-Nicoletti M, La Spina M, Nigro LL, Samperi P, D'Amico S, Bellia F, Miraglia V, Licciardello M, Cannata E, Marino S, Cimino C, Puglisi F, Valvo LL, Pezzulla A, Russo G, Di Cataldo A. Triptorelin for Fertility Preservation in Adolescents Treated With Chemotherapy for Cancer. J Pediatr Hematol Oncol. 2018 May;40(4):269-276. https://pubmed.ncbi.nlm.nih.gov/29620680/
13. Lahlou N. Pharmacocinétique et pharmacodynamique de la triptoréline [Pharmacokinetics and pharmacodynamics of triptorelin]. Ann Urol (Paris). 2005 Oct;39 Suppl 3:S78-84. French. https://pubmed.ncbi.nlm.nih.gov/16302716/
14. Klein K, Yang J, Aisenberg J, Wright N, Kaplowitz P, Lahlou N, Linares J, Lundström E, Purcea D, Cassorla F. Efficacy and safety of triptorelin 6-month formulation in patients with central precocious puberty. J Pediatr Endocrinol Metab. 2016 Nov 1;29(11):1241-1248. https://pubmed.ncbi.nlm.nih.gov/26887034/