Triptorelin (Trelstar)
Overview
Triptorelin is a synthetic decapeptide analogue of gonadotropin-releasing hormone (GnRH) that functions as a long-acting GnRH agonist. Following an initial stimulatory phase, chronic administration leads to downregulation of pituitary GnRH receptors, resulting in suppression of luteinizing hormone and follicle-stimulating hormone secretion and subsequent reduction in sex steroid production. This mechanism provides therapeutic benefit in hormone-sensitive conditions including advanced prostate cancer, endometriosis, and central precocious puberty. The peptide incorporates amino acid substitutions at positions 6 and 10 to enhance receptor affinity and metabolic stability.
Key Research Findings
Triptorelin received FDA approval in 2000 for palliative treatment of advanced prostate cancer, with pivotal trials demonstrating effective castration in over 90% of patients maintained on depot formulations. Comparative studies have shown equivalent efficacy to other GnRH agonists such as leuprolide and goserelin in achieving and maintaining testosterone suppression. Long-term extension studies have confirmed durability of response with acceptable tolerability profiles across approved depot formulations (1-month, 3-month, and 6-month).
Intramuscular injection
FDA Approved
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