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Triptorelin is a synthetic hormone used primarily in the treatment of hormone-sensitive conditions, such as advanced prostate cancer, endometriosis, and precocious puberty.
It is a gonadotropin-releasing hormone (GnRH) agonist that works by suppressing the production of sex hormones like testosterone and estrogen [1]. By reducing these hormone levels, Triptorelin helps slow the progression of hormone-dependent diseases.
Molecular Formula: C64H82N18O13
Sequence: H-Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2
Molecular Weight: 1311.4 g/mol
View the HPLC Certificate here.
Source: PubChem
Buy Triptorelin Peptide Vial here – Available in 2mg
Triptorelin is a gonadotropin-releasing hormone (GnRH) agonist that works by interacting with the endocrine system to regulate hormone production. Normally, GnRH is released in pulses from the hypothalamus, signalling the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH). These, in turn, stimulate the production of sex hormones—like testosterone in men and oestrogen in women.
Scientists have found that Triptorelin mimics natural GnRH but delivers continuous stimulation to the pituitary gland. Initially, this causes a temporary surge in LH and FSH, leading to a rise in sex hormone levels. However, with ongoing exposure, the pituitary gland becomes desensitized and stops producing these hormones. This suppression of LH and FSH leads to significantly reduced levels of testosterone and oestrogen in the body [2].
By lowering sex hormone production, Triptorelin is effective in managing hormone-sensitive conditions such as advanced prostate cancer, endometriosis, and precocious puberty, helping to alleviate symptoms and slow disease progression [3].
Buy Triptorelin Nasal Spray from PharmaLabGlobal . Available in 15ml and 30ml bottles.
Scientists investigating the effects of Triptorelin peptide have identified the following potential uses:
Reduces hormone levels
Triptorelin reduces hormone levels by acting as a gonadotropin-releasing hormone GnRH agonist. It imitates the natural GnRH produced by the body, but instead of being released in regular pulses, it provides continuous stimulation to the pituitary gland [2]. This persistent activation initially causes a surge in the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), temporarily increasing sex hormone levels like testosterone and estrogen. However, research has found that with prolonged exposure, the pituitary gland becomes desensitized and stops producing LH and FSH. This suppression halts the production of testosterone and estrogen, effectively lowering hormone levels to manage hormone-sensitive medical conditions.
Slow the progression of Prostate Cancer
Health care professionals have demonstrated that Triptorelin helps slow the progression of prostate cancer by significantly reducing testosterone levels, a hormone that fuels the growth of prostate cancer cells [4]. The desensitizing of the pituitary gland after continuous stimulation, halts the production of luteinizing hormone (LH), which in turn stops the testes from producing testosterone [5]. With testosterone levels greatly diminished, the growth and spread of hormone-sensitive prostate cancer cells are restricted. This form of hormone therapy provides an effective strategy for managing advanced prostate cancer, alleviating symptoms, and improving patient outcomes by curbing disease progression [3].
Helps alleviate symptoms of endometriosis
Triptorelin helps reduce the symptoms of endometriosis by suppressing estrogen production, a hormone essential for the growth of endometrial tissue. As a gonadotropin-releasing hormone (GnRH) agonist, Triptorelin delivers continuous stimulation to the pituitary gland, which initially triggers a rise in estrogen levels [6]. However, prolonged exposure desensitizes the pituitary gland, halting the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This suppression leads to a significant decrease in oestrogen levels, slowing the growth and activity of endometrial tissue. By reducing inflammation and related symptoms like pelvic pain, Triptorelin offers effective relief and improves the quality of life for patients [7].
Delays early onset puberty
Clinical trials have identified Triptorelin as an effective treatment for delaying early puberty, also known as central precocious puberty [8]. It works by regulating the body’s endocrine activity as a gonadotropin-releasing hormone (GnRH) agonist. Under normal circumstances, GnRH stimulates the pituitary gland to release gonadotropins—luteinizing hormone (LH) and follicle-stimulating hormone (FSH)—which, in turn, trigger the production of sex hormones like testosterone and estrogen. These hormones are responsible for the physical and hormonal changes that signify puberty.
By using Triptorelin to mimic the body’s GnRH administered continuously, overstimulating and desensitizing the pituitary gland. This leads to a significant reduction in LH and FSH production, effectively halting the hormonal cascade that drives early puberty. By suppressing this process, Triptorelin not only delays the onset of physical changes like growth spurts and secondary sexual characteristics but also helps reduce emotional and social challenges often faced by children experiencing early signs of puberty [9].
The treatment of hormone sensitive breast cancer
Triptorelin plays a pivotal role in treating hormone-sensitive breast cancer by reducing estrogen levels, which fuels cancer growth in some cases. Acting as a gonadotropin-releasing hormone (GnRH) agonist, it suppresses ovarian function, effectively lowering estrogen production. This makes it a valuable option for premenopausal women with hormone receptor-positive breast cancer, often used alongside other treatments by health professionals. Triptorelin helps in delaying disease progression, reducing recurrence risks, and improving survival outcomes. Its targeted approach helps manage cancer with fewer invasive procedures, offering patients a well-tolerated solution when monitored closely by healthcare providers for side effects and treatment response [10].
Triptorelin 2mg peptide is also available in a convenient Pre-Mixed Peptide pen. Refill cartridges containing Triptorelin and Bacteriostatic water are also available from PharmaLabGlobal .
[1] LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012-. Gonadotropin Releasing Hormone (GnRH) Analogues. [Updated 2018 Mar 20].
[2] Kumari R, Muneshwar KN, Pathade AG, Yelne S. Unveiling the Effects of Triptorelin on Endocrine Profiles: Insights From Healthy, Polycystic Ovary Syndrome, and Hypothalamic Amenorrhea Women. Cureus. 2023 Sep 5;15(9):e44752.
[3] 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.
[4] Michaud JE, Billups KL, Partin AW. Testosterone and prostate cancer: an evidence-based review of pathogenesis and oncologic risk. Ther Adv Urol. 2015 Dec;7(6):378-87.
[5] 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.
[6] 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.
[7] Agneta Bergqvist, Thorbjörn Bergh, Lars Hogström, Silvia Mattsson, Fredrik Nordenskjöld, Carsten Rasmussen, Effects of Triptorelin Versus Placebo on the Symptoms of Endometriosis 11Supported by Ferring Läkemedel AB, Malmö, Sweden., Fertility and Sterility, Volume 69, Issue 4, 1998, Pages 702-708
[8] Martínez-Aguayo A, Hernández MI, Beas F, Iñiguez G, Avila A, Sovino H, Bravo E, Cassorla F. Treatment of central precocious puberty with triptorelin 11.25 mg depot formulation. J Pediatr Endocrinol Metab. 2006 Aug;19(8):963-70.
[9] Jean-Claude Carel, Marc Roger, Simona Ispas, Françoise Tondu, Najiba Lahlou, Joelle Blumberg, Jean-Louis Chaussain, Final Height after Long-Term Treatment with Triptorelin Slow Release for Central Precocious Puberty: Importance of Statural Growth after Interruption of Treatment, The Journal of Clinical Endocrinology & Metabolism, Volume 84, Issue 6, 1 June 1999, Pages 1973–1978.
[10] Ferraro E, Trapani D, Marrucci E, Curigliano G. Evaluating triptorelin as a treatment option for breast cancer. Expert Opin Pharmacother. 2019 Oct;20(15):1809-1818.
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Is Triptorelin approved for human consumption?
Triptorelin is approved for human use by the FDA in many countries, but its approval depends on the specific medical condition being treated and the regulatory body in each region. It is commonly used as a prescription medication for conditions like hormone-sensitive cancers (e.g., prostate cancer), endometriosis, precocious puberty, and certain fertility-related issues. Please note products sold by PharmaLabGlobal are for medical research use only.
Are there any potential side effects associated with Triptorelin?
Triptorelin, while medically beneficial, can cause a range of adverse effects. Common side effects include dizziness, hot flashes, headaches, fatigue, decreased libido, and injection site reactions such as redness, hives or swelling. Some patients may also experience mood changes or musculoskeletal pain. Serious but less frequent but possible side effects include bone density loss with extended use, cardiovascular complications like changes in heart rhythm, and severe allergic reactions such as swelling or difficulty breathing.
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