Triptorelin (GnRH) (2mg)

What is the Triptorelin (GnRH) Peptide?

Triptorelin is a gonadotropin-releasing hormone analog that has been studied in clinical settings to treat advanced prostate cancer as part of a multifaceted approach to androgen deprivation therapy. Like luteinizing hormone-releasing hormone, Triptorelin appears to work as an inhibitor—a synthesis of testosterone and estrogen with long-term continuous dosing. In the UK, Triptorelin is studied for its potential to suppress the synthesis of testosterone and estrogen in transgender people. This peptide is also studied for its potential to treat hormone receptor-positive breast cancer in premenopausal women.

Specifications

AKA: Decapeptyl, TRP(6)-LHRH, Trelstar, Triptoreline, Decapeptyl, Gonapeptyl

MOLECULAR FORMULA: C₆₄H₈₂N₁₈O₁₃

MOLECULAR WEIGHT: 1311.473 g/mol

CAS NUMBER: 57773-63-4

SEQUENCE: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly

PUBCHEM: CID 25074470

RECONSTITUTION: Required

Triptorelin (GnRH) Research

Triptorelin and Testosterone Secretion
Studies have suggested that Triptorelin may raise testosterone levels early in long-term treatment regimens and may also suppress production only after chronic exposure. This is known as a testosterone flare and has been observed in Triptorelin studies within the first few weeks. This suggests that GnRH, when given at the right time and the right dose, may help raise testosterone levels in some men.

Triptorelin and Administration Dependency
Triptorelin is an analog of gonadotropin-releasing hormone (GnRH). It appears to stimulate the anterior pituitary gland to release follicle-stimulating hormone (FSH) and luteinizing hormone (LH). The exact levels of FSH and LH appear to depend on the size and frequency of GnRH pulses and, therefore, on the size and frequency of Triptorelin administration. However, administration of Triptorelin in a steady-state rather than a pulse may ultimately suppress LH and FSH secretion, and testosterone and estrogen production. Most of the research on Triptorelin focuses on the long-term and widespread potential of the peptide to suppress the production of sex hormones. Most of the research focuses on sex hormones in oncology and cancer progression.

Triptorelin and GnRH Research, Breast Cancer
One of the modern breast cancer treatments is hormone suppression to treat cancers sensitive to hormone levels. Tamoxifen is currently the most widely used substance in its class. Tamoxifen is a selective estrogen receptor modulator (SERM) used to treat and prevent cancer in certain patients. Tamoxifen reduces the risk of breast cancer recurrence by approximately 40% – 50% in postmenopausal women and 30% – 50% in premenopausal women. It is also used to shrink tumors before surgery. Tamoxifen also exhibits side effects, and over time, tumors may become more resistant to it. The search for Tamoxifen alternatives and excipients has led scientists to investigate the role of Triptorelin in breast cancer. Recent Phase 3 clinical trials have observed that Triptorelin combined with Zoledronic acid or Letrozole may be more effective than Tamoxifen (alone) in increasing 5-year disease-free survival in premenopausal females.^[1] The researchers conclude that “HOBOE study shows that in premenopausal patients with early breast cancer undergoing ovarian function suppression with triptorelin, ZL significantly improves DFS, while worsening compliance and toxicity, as compared with tamoxifen.” Similar studies also suggest the addition of Triptorelin to Tamoxifen treatment in early-stage breast cancer may improve and increase disease control and increase survival rates, especially in high-risk patients who have already received chemotherapy.^[2]

Triptorelin and Prostate Cancer
Triptorelin is primarily studied for its potential to treat prostate cancer via its apparent growth-inhibiting effect. By lowering testosterone levels, researchers observe that Triptorelin may reduce 10-year mortality to less than 5% in hormone-sensitive prostate cancer.^[3] It also appears to reduce the need for surgical intervention. New studies suggest that the combination of Triptorelin and radiation therapy may have the same benefits as complete androgen deprivation without as many debilitating side effects. Studies further suggest that Triptorelin may help relieve lower urinary tract infection symptoms. In one study, severe symptoms from prostate cancer appeared to be reduced from ~54% to 12%.^[4] The researchers conclude that “A reduction of LUTS is observed in patients with locally advanced or metastatic prostate cancer treated with triptorelin in routine practice. This is in agreement with similar observational studies of triptorelin conducted in other countries.” The results of these studies were supported by similar studies in China, Belgium, South Korea, and elsewhere. These results suggest that Triptorelin may also be useful in treating benign prostatic hyperplasia and other conditions that affect urinary function in men.

Triptorelin and Fertility
One of the potential side effects of chemotherapy, especially in young people, is loss of fertility. A small clinical study of the use of Triptorelin in young women receiving chemotherapy, observed that the peptides could maintain a significant proportion of patients giving birth. Similar studies have suggested that Triptorelin may reduce the onset of premature menopause in patients receiving chemotherapy by almost 17%.^[5]
Triptorelin appears to have the benefit of increased fertility in most test subjects, not just those receiving chemotherapy. Studies on women with adenomyosis include Triptorelin therapy. The peptide appeared to increase the rate of spontaneous pregnancies and improve the outcome of the illnesses. Similar effects were seen in research with women with endometriosis.

Triptorelin and Endometriosis
Studies suggest that Triptorelin may help to relieve pain associated with endometriosis by decreasing the number of diseased nodules. Triptorelin has been studied for its potential to be an effective preoperative treatment in reducing bleeding and other complications.^[6]  Preliminary studies suggest that Triptorelin may improve the outcome of endometriosis laparoscopic surgery.^[7] It appeared to be especially effective with increasing pregnancy rates after surgery. Triptorelin may have a profound effect on women with colorectal endometriosis, with studies reporting the peptide to relieve almost 80% of patients’ pain and almost 60% of diarrhea over a study duration of 3 months. Prolonging Triptorelin therapy may further improve results.

Triptorelin and Immune Function
Studies on rats suggest that LHRH is important due to its apparent regulatory ability in the thymus and certain aspects of the immune system. Aging leads to a decrease in the LHRH agonist binding sites on the Thymus. This causes the amount of thymus to increase by the 50% over time and also may lead to age-related immunodeficiencies, such as increased susceptibility to colds and the flu.^[8] Administration of LHRH agonists, such as Triptorelin, have been studied for their potential to improve intrathymic growth and offset the effects of aging. Supplementation with Triptorelin may help to prevent age-related changes. The amount of thymus appears to correlate to the immune system’s performance. The peptide may be used both therapeutically and prophylactically. Experimental studies report Triptolerin to exhibit moderate side effects, low oral and excellent subcutaneous bioavailability in mice. The dose per kg of mice is not tailored for humans.

References