Triptorelin (acetate or palmoate) is a gonadotropin releasing hormone agonist (GnRH agonist). 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® (Ferring Pharmaceuticals) and Diphereline® and Gonapeptyl®.
Triptorelin is sold by Pfizer in the United States as Trelstar®.
During the treatment of prostate cancer it does cause a surge of testosteron (an initial uplevel of testosterone levels). In men a reduction of serum testosterone levels into the range normally seen after surgical castration occurs appr. 2 to 4 weeks after initiation of therapy. In contrast gonadotropin releasing hormone Receptor antagonists does not cause a surge, but a sudden shut-down of testosterone level.
Systematic IUPAC Name: [d-Trp6]GnRH
- Pharmacokinetics and pharmacodynamics of GnRH agonists: clinical implications in pediatrics. J Pediatr Endocrinol Metab. 2000 Jul;13 Suppl 1:723-37. Review. PMID 10969915
- GnRH analogues—agonists and antagonists A.M. Padula,
University of Melbourne 
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