Triptorelin, a synthetic peptide closely resembling gonadotropin-releasing hormones (GnRH), may play a potential role in modulating reproductive function by influencing the synthesis and secretion of follicle-stimulating hormone (FSH) and luteinizing hormone (LH).
Research suggests that GnRH, originating from the hypothalamus, may govern the secretion of both FSH and LH, both of which are considered to be crucial in various reproductive functions. Disruptions in GnRH pulsatility, possibly triggered by factors such as malnutrition, may impact fertility, potentially significantly.
Triptorelin, consisting of ten amino acids, has been suggested by researchers to act on the pituitary gland, possibly promoting the production and release of LH and FSH.(1) This mechanism is considered essential for testosterone production in male organisms and estrogen synthesis in females.(2)
Fig. 1 – Triptorelin Peptide Chemical Structure
Triptorelin Related Research
Studies suggest that Triptorelin’s potential may extend beyond reproductive function, as research delves into its implications in prostate cancer cell development, androgen deprivation, and receptor-positive breast cancer procedures. Through long-term research studies, Triptorelin has been hypothesized to inhibit testosterone and estrogen synthesis respectively, offering promising avenues for further research and scientific study.
Triptorelin Peptide and Endometriosis
Endometriosis is characterized by ectopic growth of endometrial tissue and may potentially lead to infertility.
A clinical trial(3) involving female models of endometriosis investigated the potential action of Triptorelin peptide when introduced routinely at four-week intervals. Assessment parameters encompassed symptomatology, endometrial size reduction, hormonal profiles, alterations in bone mineral density, and restoration of menstrual cycling. Following a duration of eight-weeks, all models exhibited alleviation of pain-associated symptoms. Concurrently, studies suggest that levels of follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were uniformly diminished, while there was a reported modest increase in cholesterol and triglyceride levels across the cohort. Studies suggest that these findings may underscore Triptorelin’s potential in ameliorating symptoms.(3)
Triptorelin Peptide and Fertility
Triptorelin is speculated to exert potentially protective action on reproductive processes and fertility, particularly notably in contexts of research models of chemotherapy-induced gonadal toxicity. In a small-scale clinical trial(4) involving chemotherapy models, Triptorelin exposure appeared to exhibit potential in preserving fertility in a substantial proportion of the cohort. Furthermore, Triptorelin exposure appeared to exhibit a notable reduction, approximately 17%,(5) in the incidence of premature menopause following chemotherapy.
Beyond chemotherapy-induced infertility, Triptorelin’s fertility-enhancing potential is speculated to extend to diverse cohorts. Studies(6) involving models of adenomyosis suggest its potential to augment spontaneous pregnancy rates and possibly ameliorate disease outcomes.
Triptorelin Peptide and Breast Cancer
Hormone suppression constitutes a cornerstone of research into hormone-sensitive breast cancers. Presently, selective estrogen receptor modulator (SERM), stand as the foremost compounds researched and studied for its action in such cancers. Despite their utility, researchers suggest that SERMs may present a series of drawbacks, with long-term exposure potentially culminating in resistance development and ancillary, unintended downstream physiological effects. In pursuit of expanding existing research with alternative compounds, researchers have turned their attention to Triptorelin.
Triptorelin is speculated to provide potentially superior efficacy over certain SERMs in augmenting disease-free 5-year survival rates among premenopausal breast cancer models.(7) Complementary studies continue to suggest that Triptorelin supplementation to SERM regimens may be “valid options [in the research of] endocrine-responsive, early-stage breast cancer … with sufficiently high risk of relapse to warrant receiving chemotherapy and [remaining] premenopausal thereafter.” (8)
Triptorelin Peptide and Testosterone
Research suggests that Triptorelin’s impact on testosterone secretion may be contingent upon the timing and duration of its exposure.
Studies suggest that Triptorelin initially appears to stimulate testosterone production, a phenomenon known as testosterone flare. However, with chronic exposure to the peptide, Triptorelin may gradually suppress testosterone synthesis. This temporal pattern suggests a potential utility in augmenting testosterone levels in select male organisms, contingent, as mentioned above, upon specific timing and duration.
Triptorelin Peptide and Prostate Cancer
Triptorelin has primarily appeared in research findings related to prostate cancer, with researchers hypothesizing its potential through an attenuation of testosterone levels, which may mitigate tumor growth. Particularly in hormone-sensitive prostate cancer, studies suggest that Triptorelin exposure may yield potentially remarkable outcomes, possibly reducing the 10-year mortality rate to less than 5%.(10)
Triptorelin Peptide and Central Precocious Puberty (CPP)
The initial clinical study which explored the potential of Triptorelin in CPP spanned a duration of 48 weeks, aiming to attain suppression of luteinizing hormone (LH) to prepubertal levels. A cohort comprising 88% female and 12% male, hitherto unexamined for CPP, were evaluated over the course of the study.(9) Analysis at the study’s conclusion suggested that Triptorelin elicited a notable suppression of LH, reaching prepubertal levels as early as month 6, a response sustained through month 12, in 93% of the cohort. These findings indicate the potential of Triptorelin to exert action in models of CPP.
Triptorelin Peptide and Immunity
Research conducted in rodent models has suggested the pivotal role of luteinizing hormone-releasing hormone (LHRH) in modulating thymic function, a cornerstone of immune regulation. A natural decline occurs in LHRH agonist binding sites on the thymus, culminating in a notable reduction, approximately 50%, in thymic mass over time. Consequently, immune dysfunction may ensue, characterized by heightened susceptibility to infectious diseases. Reportedly the influence of a supplemented LHRH agonist, such as Triptorelin, may exhibit the potential to enhance thymic proliferation and partially ameliorate age-induced alterations within the thymus.(11)
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References:
- National Center for Biotechnology Information. PubChem Compound Summary for CID 25074470, Triptorelin.
- 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/
- 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/
- 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. doi: 10.1097/MPH.0000000000001144. PMID: 29620680. https://pubmed.ncbi.nlm.nih.gov/29620680/
- Del Mastro L, Boni L, Michelotti A, Gamucci T, Olmeo N, Gori S, Giordano M, Garrone O, Pronzato P, Bighin C, Levaggi A, Giraudi S, Cresti N, Magnolfi E, Scotto T, Vecchio C, Venturini M. Effect of the gonadotropin-releasing hormone analogue triptorelin on the occurrence of chemotherapy-induced early menopause in premenopausal women with breast cancer: a randomized trial. JAMA. 2011 Jul 20;306(3):269-76. doi: 10.1001/jama.2011.991. PMID: 21771987. https://pubmed.ncbi.nlm.nih.gov/21771987/
- Xie M, Yu H, Zhang X, Wang W, Ren Y. Elasticity of adenomyosis is increased after GnRHa therapy and is associated with spontaneous pregnancy in infertile patents. J Gynecol Obstet Hum Reprod. 2019 Dec;48(10):849-853. doi: 10.1016/j.jogoh.2019.05.003. Epub 2019 May 5. PMID: 31067498. https://pubmed.ncbi.nlm.nih.gov/31067498/
- Perrone et al., “Adjuvant zoledronic acid and letrozole plus ovarian function suppression in premenopausal breast cancer: HOBOE phase 3 randomised trial,” Eur. J. Cancer Oxf. Engl. 1990, Jun. 2019. https://www.ejcancer.com/article/S0959-8049(19)30297-7/abstract
- Frampton JE. Triptorelin: A Review of its Use as an Adjuvant Anticancer Therapy in Early Breast Cancer. Drugs. 2017 Dec;77(18):2037-2048. doi: 10.1007/s40265-017-0849-3. PMID: 29177573. https://pubmed.ncbi.nlm.nih.gov/29177573/
- 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/
- Merseburger AS, Hupe MC. An Update on Triptorelin: Current Thinking on Androgen Deprivation Therapy for Prostate Cancer. Adv Ther. 2016 Jul;33(7):1072-93. doi: 10.1007/s12325-016-0351-4. Epub 2016 May 31. PMID: 27246172; PMCID: PMC4939158. https://pubmed.ncbi.nlm.nih.gov/27246172/
- Marchetti B, Guarcello V, Morale MC, Bartoloni G, Raiti F, Palumbo G Jr, Farinella Z, Cordaro S, Scapagnini U. Luteinizing hormone-releasing hormone (LHRH) agonist restoration of age-associated decline of thymus weight, thymic LHRH receptors, and thymocyte proliferative capacity. Endocrinology. 1989 Aug;125(2):1037-45. doi: 10.1210/endo-125-2-1037. PMID: 2546733. https://pubmed.ncbi.nlm.nih.gov/2546733/
- Image 1 source: National Center for Biotechnology Information (2024). PubChem Compound Summary for CID 25074470, Triptorelin. Retrieved April 13, 2024 from https://pubchem.ncbi.nlm.nih.gov/compound/Triptorelin.