Triptorelin 5mg

What is Triptorelin?

Triptorelin is a decapeptide known as an analogue of the gonadotropin-releasing hormone (GnRH). This peptide acts on the pituitary gland (an endocrine gland) to stimulate the secretion of two gonadotropins, luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This leads to increased production of testosterone in males and estrogen in females. However, Triptorelin initially causes a sharp boost in the production of these gonadotropins but later leads to a reduction in the stimulation of their secretion so that testosterone and estrogen levels decrease.

 Many studies indicate that this effect can potentially be used in the treatment of various conditions such as prostate cancer (as part of androgen deprivation therapy), precocious puberty, endometriosis, uterine fibroids, but also conditions such as male hypersexuality. The efficacy of this peptide has also been studied in patients suffering from various diseases, including Alzheimer's disease.

Triptorelin Research Benefits

The Effect of Triptorelin on Advanced Metastatic Prostate Cancer

 Advanced metastatic prostate cancer is a serious condition that can often be fatal. Androgen deprivation therapy (ADT) could be an effective treatment with a high progression-free survival rate of 12 to 30 months. ADT can be achieved by bilateral orchiectomy (castration), antiandrogens, or luteinizing hormone-releasing hormone (LHRH) agonists. The first option, which requires surgical intervention, is effective but is psychologically difficult for patients to tolerate. The second option, antiandrogens, is associated with poorer survival outcomes and is, therefore, less commonly used, even if well tolerated. LHRH has the greatest advantage because it has been shown to be a potentially more effective and more comfortable option for patients with advanced metastatic prostate cancer. However, there are different LHRH agonists, and one of the many studies compared the efficacy of Goserelin, Triptorelin, and Leuprolide. The primary endpoint was mean testosterone levels. Although there were no significant differences, Triptorelin showed the most successful biopsy results and the percentage of distant metastases. A significant difference was also observed in the prostate-specific antigen (PSA) values in patients treated with this peptide compared to the start of treatment. 

 Triptorelin showed the best results when it came to mean testosterone concentration (which was the main parameter of the study). The value of this hormone continuously decreased and remained the lowest throughout the study, only in the case of Triptorelin treatment. This, and many other studies, suggest that this peptide, due to its effects, could potentially be part of prostate cancer therapy, whether it is primary or metastatic form.

The Connection between Triptorein and Alzheimer's Disease

 Alzheimer's disease is a severe neurodegenerative disease and the primary cause of dementia in the elderly population. Given that men with prostate cancer are most often part of the middle-aged or elderly population, the question arises whether Triptorelin affects Alzheimer's disease and whether they can potentially be used as part of prostate cancer therapy. The study included only male patients over 60 years who suffered from this malignancy and received LHRH therapy in the form of Triptorelin or other peptides. The results of the study indicated that a negligible percentage of side effects related to dementia or memory loss that would indicate Alzheimer's disease occurred. In addition, the cognition of these patients was maintained at the same level as before the start of the study. Some studies even suggest that prostate cancer patients who used LHRH agonists were at a lower risk of death from Alzheimer's disease than those who did not. The cancer itself and chemotherapy may affect the patient and his psychophysical state. Still, the potentially beneficial treatment with Triptorelin or other LHRH agonists alone is absolutely not associated with any risk or increased mortality from Alzheimer's disease.

Triptorelin for the Treatment of Endometriosis

 Endometriosis is a condition characterized by the presence of ectopic endometrial glands and stroma outside the uterus. This condition affects women of reproductive age and can present with severe symptoms such as painful and irregular periods and even lead to infertility. The most common symptoms are dysmenorrhea, dyspareunia, dyschezia, and chronic pelvic pain or even gastrointestinal symptoms. Endometriotic lesions can also appear on other internal organs, including the ovaries, pleura, and even the brain. Some patients may be candidates for surgery, but symptoms often return after the operation, so hormone therapy may be an excellent solution. 

 Various studies suggest that gonadotropin-releasing hormone agonists, as part of hormone therapy, may be a way to reduce painful symptoms and regulate endometriosis. This multicenter clinical trial was concerned with examining the efficacy of this peptide itself, and the main parameter monitored in this study was the intensity of pain in patients, which was examined both before and after the administration of Triptorelin. The clinical trial included 45 patients with moderate to severe endometriosis, and all were treated with intramuscular injection of peptide. 

 The results showed a significant improvement in pain symptoms (dysmenorrhea, dyspareunia, and severe pelvic pain) in almost all patients after the first month of treatment, and after 8 weeks, all patients were completely pain-free. The size of ovarian endometriomas was also significantly reduced. Other types of prospective, randomized, double-blind studies have researched the intensity of pain symptoms in patients treated with Triptorelin and those treated with a placebo. 

 The results also showed a significant decrease in severe pain but also levels of estradiol, follicle-stimulating hormone (FSH), and luteinizing hormone (LH). In addition to these, the main parameters were changes in symptoms, visible extension of endometriosis, and frequency and amount of bleeding. All of the mentioned parameters were significantly improved in the group of patients treated with Triptorelin compared to the group that received a placebo. This indicates that this peptide may be effective in treating this very painful condition in female patients.

Summary

According to various scientific sources, Triptorelin represents an amino acid sequence with many potential beneficial properties. Only some of those described are possible positive therapeutic effects in the treatment of endometriosis and advanced metastatic prostate cancer. The results of numerous studies indicate that its use may also be safe in patients suffering from Alzheimer's disease. This peptide will certainly be studied further in the future.

Resources:

1.     National Center for Biotechnology Information. PubChem Compound Summary for CID 25074470, Triptorelin.
2.     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/
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/
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6.     Chung LY, Kang E, Nam HK, Rhie YJ, Lee KH. Efficacy of Triptorelin 3-Month Depot Compared to 1-Month Depot for the Treatment of Korean Girls with Central Precocious Puberty in Single Tertiary Center. J Korean Med Sci. 2021 Aug 30;36(34):e219. doi: 10.3346/jkms.2021.36.e219. PMID: 34463062; PMCID: PMC8405405.
7.     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.