Triptorelin, a decapeptide (pGlu-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH2), is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. By causing constant stimulation of the pituitary, it decreases pituitary secretion of gonadotropins luteinizing hormone (LH) and follicle stimulating hormone (FSH). Like other GnRH agonists, triptorelin may be used in the treatment of hormone-responsive cancers such as prostate cancer or breast cancer, precocious puberty, estrogen-dependent conditions (such as endometriosis or uterine fibroids), and in assisted reproduction. Triptorelin is marketed under the brand names Decapeptyl (Ipsen) and Diphereline and Gonapeptyl (Ferring Pharmaceuticals). In the United States, it is sold by Watson as Trelstar.In Iran Triptorelin is marketed under the brand name Variopeptyl (Varian Darou Pajooh).
During the treatment of prostate cancer it does cause a surge of testosterone (an initial uplevel of testosterone levels), known as a flare effect. In men a reduction of serum testosterone levels into the range normally seen after surgical castration occurs approximately two to four weeks after initiation of therapy. In contrast, gonadotropin-releasing hormone antagonists do not cause a surge, but a sudden reduction of testosterone levels.
Systematic IUPAC Name: [d-Trp6]GnRH
- Lahlou N, Carel JC, Chaussain JL, Roger M (July 2000). "Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics". J Pediatr Endocrinol Metab. 13 Suppl 1: 723–37. PMID 10969915.