Efficacy and safety of leuprolide acetate 6-month depot for suppression of testosterone in patients with prostate cancer

• Published in: Prostate cancer and prostatic diseases Vol. 15; no. 1; pp. 93 - 99
• Main Authors: Spitz, A, Young, J M, Larsen, L, Mattia-Goldberg, C, Donnelly, J, Chwalisz, K
• Format: Journal Article
• Language: English
• Published: London Nature Publishing Group UK 01.03.2012; Nature Publishing Group
• Subjects: Aged; Aged, 80 and over; Androgen Antagonists - adverse effects; Androgen Antagonists - pharmacokinetics; Androgen Antagonists - therapeutic use; Anemia - blood; Anemia - chemically induced; Antineoplastic Agents, Hormonal - adverse effects; Antineoplastic Agents, Hormonal - pharmacokinetics; Antineoplastic Agents, Hormonal - therapeutic use; Biomarkers, Tumor - blood; Biomedical and Life Sciences; Biomedicine; Blood Glucose; Cancer Research; Care and treatment; Chemistry, Pharmaceutical; Development and progression; Dosage and administration; Hemoglobins - metabolism; Humans; Leuprolide; Leuprolide - adverse effects; Leuprolide - pharmacokinetics; Leuprolide - therapeutic use; Luteinizing Hormone - blood; Male; Middle Aged; Original; original-article; Patient outcomes; Prostate cancer; Prostate-Specific Antigen - blood; Prostatic Neoplasms - blood; Prostatic Neoplasms - drug therapy; Testosterone - blood; Treatment Outcome; United States; gonadotropin-releasing hormone analog; leuprolide acetate; testosterone; LH-RH; PSA
• ISSN: 1365-7852; 1476-5608
• DOI: 10.1038/pcan.2011.50

Background: This open-label study evaluated the efficacy and safety of a new leuprolide acetate 45 mg 6-month depot formulation in 151 men with prostate cancer who received 2 intramuscular injections administered 24 weeks apart. Methods: The primary efficacy measurement was the proportion of patients achieving suppression of serum testosterone to ⩽50 ng dl −1 from week 4 through week 48. Adverse events (AEs) and hormonal and safety laboratory values were monitored. Results: The primary efficacy end point was achieved in 93.4% of subjects (95% confidence interval (89.2%, 97.6%)). There were nine escapes from testosterone suppression during the study, none of which were accompanied by a rise in PSA. By week 4, mean testosterone concentration was suppressed below castrate levels to 15.9 ng dl −1 ; suppression was maintained for the entire 24-week duration of each depot injection. No mean increase in testosterone was observed after the second injection. Mean PSA levels were maintained below 3 ng ml −1 from week 14 through the 48-week treatment period. The most frequent AE was flushing (58.3%). Injection site reactions were reported in 24.5% of patients. Conclusions: Leuprolide acetate 45 mg 6-month depot demonstrated rapid and sustained testosterone suppression through 12 months and was well tolerated. This 6-month leuprolide acetate depot will decrease the number of annual injections in the treatment of prostate cancer.