Triptorelin Acetate & triptorelin pamoate
acetate: H-4075-GMP, 4008442
pamoate: H-4060-GMP, 4008634
What is triptorelin?
Triptorelin is a synthetic agonist analog of gonadotropin-releasing hormone (GnRH), repressing the expression of luteinizing hormone (LH) and follicle-stimulating hormone (FSH). First approved in 1986, the indications include prostate cancer, uterine fibroids, central precocious puberty, endometriosis, female infertility, and breast cancer. Triptorelin is a short peptide consisting of nine amino acids.
What is triptorelin used for?
Triptorelin is a synthetic analog of GnRH, a hormone naturally produced by the hypothalamus in the brain. GnRH plays a crucial role in regulating the production of sex hormones, specifically LH and FSH.
When triptorelin is applied as intramuscular injection, it initially stimulates the pituitary gland in the brain, much like natural GnRH. This stimulation prompts the pituitary gland to release LH and FSH, which are the messengers that signal the testes in males and the ovaries in females to produce sex hormones, such as testosterone and oestradiol.
However, as triptorelin injection treatment continues, a process known as “downregulation” occurs. This means that the pituitary gland becomes less responsive to the constant GnRH-like signals generated by triptorelin.
As a result of this desensitization, the production of LH and FSH by the pituitary gland decreases over time. Since LH and FSH are essential for stimulating the production of sex hormones, their reduction leads to a significant decrease in testosterone levels in males and oestradiol levels in females.
Ultimately, the diminished production of sex hormones leads to a state of hypogonadism, where the levels of testosterone or oestradiol in the body drops significantly below the normal range. This controlled reduction of sex hormones is the desired therapeutic outcome in various conditions. For example, in prostate cancer, lowering testosterone levels can slow the growth of cancer cells, while in conditions like endometriosis and uterine fibroids, it can reduce symptoms associated with excess oestradiol.
How is triptorelin administrated?
Triptorelin is available in two different salt forms, which are tritptorelin acetate and triptorelin pamoate. Triptorelin acetate is sold under different brand names, i.e. Decapeptyl®, Pamorelin® or Gonapeptyl® by the companies Ipsen and Ferring. Triptorelin pamoate or embonate, which has a longer acting release form and has been developed by Debiopharm, is commercialized under the brand names Decapeptyl®, Trelstar® and Triptodur® by Ipsen, Verity Pharm and Arbor Pharmaceuticals.
Both salt versions are administrated by intramuscular injection via a pre-filled syringe at different regimens:
- 75 mg for a monthly injection
- 25 mg for a 3-month period injection
- 5 mg for a 6-month period injection
Experience in GnRH analogs
With more than 20 years of experience in GMP-grade peptides, we manufacture and supply hundreds of kilograms of gonadorelin (LHRH) analogues or so-called relins each year. As a market leader, we see the importance of continuously improved processes for efficiency, robustness, and sustainability. With our strong expertise in gonadorelin analogs production, our customer benefit from an optimized process because of synergies in relins synthesis.
Bachem goes the extra mile
With over five decades of experience, we grew extensive regulatory expertise to deliver a comprehensive package of generic APIs tailored to your needs. Our services ensure a fast delivery of material on stock and faster registrations with available DMFs and CEPs. Our customers get regulatory support from our experienced teams and an all-around service with our extensive catalog of related impurities.
Whether you require just a few grams, multi-kilograms, or even tens of tons of generic APIs, we can accommodate your demands with timely delivery. Thanks to our in-house production of starting materials, we can guarantee a secure and sustainable supply chain.
Innovation is ingrained in our DNA, driving us to continuously enhance our processes, quality, and efficiency. We actively explore cutting-edge technologies to capitalize on emerging opportunities in the generic API sector, all while maintaining high quality, minimizing lead times, and ensuring cost-effectiveness.
List of impurities and related products:
|4033016||(D-Trp⁶)-GnRH, Triptorelin acetate salt, [DTrp6] LH-RH, amide||Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH₂||Acetate|
|4039648||Triptorelin pamoate salt||Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH₂||Pamoate|
|4026526||Triptorelin (free acid)||Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-OH||Trifluoroacetate|
|4029113||Triptorelin (1-6) amide||Pyr-His-Trp-Ser-Tyr-D-Trp-NH₂|
Bachem Regulatory Documentation
Acetate: (D-Trp6)-LHRH; (D-Trp6)-GnRH
Pamoate: (D-Trp6)-LHRH; Triptorelin Embonate
Acetate: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 acetate salt
Pamoate: Pyr-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2 pamoate salt
Relative Molecular Mass
57773-63-4 (net), 140194-24-7 (acetate), 124508-66-3 (pamoate)
-20 ± 5°C