▴ Leuprorelin (leuprolide acetate) is a luteinizing hormone-releasing hormone agonist used in the palliative treatment of advanced prostate cancer. This subcutaneous depot formulation of leuprorelin is available for administration as 7.5, 22.5, or 30mg once every 1, 3, or 4 months, respectively.
▴ The efficacy of leuprorelin 7.5mg once monthly for 6 months, 22.5mg every 3 months for 6 months, or 30mg every 4 months for 8 months has been investigated in three multicenter, noncomparative studies (n = 90–119). Mean serum testosterone levels transiently increased following initial administration of leuprorelin (days 2–3) and then decreased to below castration levels (<50 ng/ dL).
▴ In these three trials, serum testosterone levels <50 ng/dL occurred in approximately 20% of patients after 14 days and in >98% of patients at study completion (6–8 months).
▴ Mean testosterone levels ranged from 6.1 to 12.4 ng/dL after 6–8 months of leuprorelin 7.5 mg/mo, 22 mg/3mo, or 30 mg/4mo.
▴ Mean serum prostate-specific antigen levels decreased following leuprorelin administration. There were no significant changes in WHO performance status scores or patient-assessed bone pain, urinary pain, or urinary symptoms in any of the studies.
▴ Adverse effects were predominantly mild to moderate in severity and typical of testosterone suppression. The most frequently reported adverse effect was hot flashes.