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Triptorelin 5mg
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Triptorelin 5mg

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Triptorelin, a synthetic analogue of gonadotropin-releasing hormone, has emerged as a key therapeutic agent in the treatment of advanced prostate cancer. Its role within comprehensive androgen deprivation therapy has been underscored by its ability to effectively inhibit the synthesis of testosterone and estrogen through prolonged, continuous administration. Additionally, noteworthy applications of Triptorelin include its utilization in the United Kingdom to manage testosterone and estrogen production in transgender individuals, as well as its efficacy in treating hormone-receptor-positive breast cancer in premenopausal women.

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Description

What Is Triptorelin (GnRH)?

Triptorelin, a Gonadotropin-releasing hormone (GnRH) agonist, is a synthetic peptide analog of the natural gonadotropin-releasing hormone. It acts by binding to and activating the GnRH receptors in the pituitary gland, leading to the initial release of luteinizing hormone and follicle-stimulating hormone. With continued administration, triptorelin downregulates these receptors, ultimately inhibiting the production of testosterone and estrogen in both men and women. This mechanism of action makes it a valuable tool in the treatment of various hormone-related conditions, including prostate cancer, breast cancer, and transgender medicine.

Triptorelin Structure

triptorelin structureSource: PubChem
  • Sequence: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly
  • Molecular Formula: C64H82N18O13
  • Molecular Weight: 1311.473 g/mol
  • PubChem CID: 25074470
  • CAS Number: 57773-63-4
  • Synonyms: Decapeptyl, TRP(6)-LHRH, Trelstar, Triptoreline, Decapeptyl, Gonapeptyl

Triptorelin Restores Testosterone Secretion in Some Men

As a gonadotropin-releasing hormone (GnRH) agonist, Triptorelin is crucial in modulating testosterone secretion in men. By inhibiting the synthesis of testosterone through its action on luteinizing hormone (LH) and follicle-stimulating hormone (FSH), it effectively suppresses testosterone production in the treatment of prostate cancer. However, it's noteworthy that reports are indicating that triptorelin can also restore testosterone secretion in some men, suggesting a dynamic and complex interplay within the endocrine system.

Triptorelin Administration Determines Effects

Triptorelin exhibits the ability to stimulate the anterior pituitary gland, thereby triggering the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). 

The specific levels of LH and FSH produced are directly influenced by the size and frequency of GnRH pulses, mirrored in the size and frequency of triptorelin doses. Conversely, continuous steady-state administration of triptorelin suppresses both LH and FSH secretion, consequently resulting in reduced production of testosterone and estrogen. The mode of triptorelin administration in research settings significantly impacts its resultant effects.

The primary focus of research on triptorelin has centered on its long-term use in suppressing the production of sex hormones, particularly within the field of oncology, where the role of sex hormones in cancer progression is being closely examined. Recently, there has been a growing interest in exploring the potential of triptorelin to restore sexual function, fertility, and testosterone levels. However, it's important to note that research in this area is still in its early stages.

Triptorelin Research and Breast Cancer

Triptorelin, a gonadotropin-releasing hormone analogue, has been the subject of extensive research about breast cancer. The primary focus has been its use in managing hormone-sensitive breast cancers, particularly in premenopausal women.

Triptorelin functions by suppressing the production of sex hormones, which play a significant role in the progression of certain types of breast cancers. By reducing the levels of these hormones, triptorelin can help slow down the growth of hormone-sensitive tumors.

Several studies have explored the impact of triptorelin on chemotherapy-induced early menopause in premenopausal women with breast cancer. This is significant as early menopause can lead to a variety of health issues, including an increased risk of cardiovascular disease and osteoporosis.

In conjunction with adjuvant breast cancer chemotherapy, triptorelin has been studied for its effects on long-term ovarian function, pregnancies, and disease-free survival. Some research suggests no statistically significant difference in disease-free survival for women assigned to triptorelin.

Furthermore, triptorelin has been compared to other treatments like degarelix in premenopausal patients who receive letrozole for locally advanced endocrine-responsive breast cancer. Some studies suggest that patients respond better to a combination of degarelix and letrozole than triptorelin and letrozole.

Research is also being conducted on triptorelin's potential cytotoxic activity in in vitro models of triple-negative breast cancers (TNBC), a particularly aggressive form of the disease.

Triptorelin Protects Fertility

Studies have shown that triptorelin can be administered to postpubertal female individuals with cancer who are receiving chemotherapy to help preserve their fertility. This is because chemotherapy can often result in early menopause and infertility in women.

However, it's important to note that while triptorelin may help in fertility preservation, it can also cause impotence and affect fertility. Therefore, individuals planning to start a family should discuss this with their doctor.

Research has also been conducted on the effects of varying doses of triptorelin on hormone serum levels and the outcomes of in vitro fertilization. One study demonstrated that halving the daily dose of triptorelin at the start of ovarian stimulation didn't negatively impact the outcome of in vitro fertilization.

Furthermore, other studies have suggested that triptorelin administration in the luteal phase can improve the results of ovulation induction, which is significant for women undergoing fertility treatments.

Triptorelin Is Not Associated with Alzheimer's Disease

Its implications for Alzheimer's disease have been a focus of several studies due to its role in androgen deprivation therapy (ADT), a treatment for prostate cancer.

Some research suggests there might be an association between ADT and an increased risk of Alzheimer's disease. However, it's important to note that these findings do not necessarily implicate triptorelin directly in this increased risk. The potential link could be due to the overall hormonal changes induced by ADT rather than triptorelin specifically.

Contrary to these findings, other studies have found no increased risk of Alzheimer's disease associated with anti-androgens like triptorelin (source). A patent also discloses the application of triptorelin, stating that the drug has shown potential in improving cognitive function, though more research is needed to confirm these findings.

While triptorelin is primarily used in hormone-related conditions, it's not typically used in the treatment of Alzheimer's disease. Current treatments for Alzheimer's primarily involve drugs like galantamine that aim to improve thinking ability.

While there is some conflicting research regarding the relationship between triptorelin and Alzheimer's disease, the majority of studies suggest that there is no direct association between the two.

Triptorelin Research and Endometriosis

Endometriosis is a condition where tissue similar to the lining of the womb starts to grow in other places, such as the ovaries and fallopian tubes. Triptorelin can help manage the symptoms of endometriosis by reducing the production of sex hormones, which may slow down the growth of endometrial tissue.

One study investigated the effects of prolonged use of triptorelin depot on patients with endometriosis, concluding that administering four doses of triptorelin depot 3.75 mg was effective.

In terms of long-term use, a single-center, single-arm, open-label study found that long-long term use of Triptorelin, combined with Tibolone as supportive therapy in premenopausal women that have issues with chronic cyclical pelvic pain (CCPP) and endometriosis hasn’t demonstrated any significant side effects.

Additionally, a randomized controlled trial assessed two formulations of triptorelin in Chinese patients with endometriosis. 

Finally, a clinical trial evaluated the combination of laparoscopic surgery and triptorelin acetate for treating patients with endometriosis and infertility.

Triptorelin Research and Immune Function

Triptorelin has been researched for its potential effects on immune function.

One study found that Triptorelin and Cetrorelix can induce immune responses and affect uterine development and expressions of genes and proteins of ESR1, LHR, and FSHR in mice. It was observed that immunity could reduce the expression of pituitary GnRH levels and cause changes in reproductive behaviors.

Another research focused on the manifestation of CD68+ and Ki67 cells in red bone marrow monocyte sprouts, under the influence of triptorelin within the hypothalamic-pituitary-testis regulatory system. The study suggested that triptorelin administration induces a hormonal imbalance in the system.

A phase I study evaluated the safety of triptorelin in combination with nivolumab, an anti–PD–1 drug, in melanoma patients who had been pretreated with anti–PD–1. The results showed that adding triptorelin to nivolumab did not significantly increase immune-related toxicity.

In the context of breast cancer treatment, research has been conducted on the potential benefits of adding triptorelin or other LH-RH analogues to endocrine treatment in the adjuvant setting.

A study was also conducted on how immunocompetent liver cells respond to chemical castration in male rats, a process triggered by the administration of triptorelin acetate.The research suggested that triptorelin acetate could cause changes in the immune system of the liver cells.

Further, an investigation on Cetrorelix and Triptorelin active immunization revealed that it could improve ovarian growth, increase receptor expressions of ovaries in mice, and enhance expression levels of FSHR and LHR proteins.

Article Autho

The above literature was researched, edited and organized by Dr. Logan, M.D. Dr. Logan holds a doctorate degree from Case Western Reserve University School of Medicine and a B.S. in molecular biology.

Scientific Journal Author

Prof. Dr. Axel S. Merseburger is the chairman of the Department of Urology, Campus Lübeck, University Hospital Schleswig-Holstein, Germany. Professor Merseburger obtained his medical degree from Hannover Medical School in 2002 after a one-year academic research programme in Washington DC, USA, where he completed his MD thesis. In 2008, he accepted a staff position in Hannover and was promoted to associate professor in 2009; he obtained full professorship in 2012.

Professor Merseburger is board certified in urology and is a member of numerous national and international urological and oncological associations. In addition to serving as a reviewer and member of the editorial board of many journals, Professor Merseburger is the associate editor of the World Journal of Urology and Editor-in-Chief of the “Advanced Prostate Cancer Resource Centre”. Part of his studies pertained to the examination of Triptorelin's ability to induce androgen deprivation in order to treat prostate cancer.

Furthermore, he is a member of the European Association of Urology (EAU) Guideline Groups on Renal Cell Cancer. He serves as national and international principal investigator in several phase II/III clinical trials. Professor Merseburger has won multiple awards, stipends and prizes for his molecular and clinical research and has authored and co-authored more that 200 publications.

Dr. Axel S. Merseburger is being referenced as one of the leading scientists involved in the research and development of Triptorelin. In no way is this doctor/scientist endorsing or advocating the purchase, sale, or use of this product for any reason. There is no affiliation or relationship, implied or otherwise, between Peptide Shop and this doctor. The purpose of citing the doctor is to acknowledge, recognize, and credit the exhaustive research and development efforts conducted by the scientists studying this peptide.

ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATONAL AND EDUCATIONAL PURPOSES ONLY.

The products offered on this website are furnished for in-vitro studies only. In-vitro studies (Latin: in glass) are performed outside of the body.  These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease.  Bodily introduction of any kind into humans or animals is strictly forbidden by law.

Sources

https://www.mayoclinic.org/drugs-supplements/triptorelin-intramuscular-route/side-effects/drg-20066536?p=1

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC10556375/

https://my.clevelandclinic.org/health/drugs/19231-triptorelin-pamoate-injection-suspension-prostate-cancer

https://aacrjournals.org/cancerres/article/78/4_Supplement/P1-10-06/541923

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8686727/

https://journals.lww.com/jpho-online/abstract/2018/05000/triptorelin_for_fertility_preservation_in.2.aspx

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5070576/

https://pubmed.ncbi.nlm.nih.gov/30480255/

https://www.sciencedirect.com/science/article/abs/pii/S0301211514005466

https://www.hkmj.org/system/files/hkm0009p260.pdf

https://link.springer.com/article/10.1186/s12958-020-00586-z

https://www.tandfonline.com/doi/abs/10.3109/08923973.2016.1168432

https://iej.zaslavsky.com.ua/index.php/journal/article/view/1308

https://aacrjournals.org/clincancerres/article-abstract/29/5/858/716606/Phase-I-Study-of-Androgen-Deprivation-Therapy-in

https://www.tandfonline.com/doi/abs/10.1080/14656566.2019.1650020

https://www.sciencedirect.com/science/article/abs/pii/S1214021X15000447

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