Efficacy and safety of leuprolide acetate 6-month depot for suppression of testosterone in patients with prostate cancer.
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.
South Orange County Medical Research Center, Laguna Hills, CA, USA.
A
A
Spitz
J M
JM
Young
L
L
Larsen
C
C
Mattia-Goldberg
J
J
Donnelly
K
K
Chwalisz
D000368:Aged; D000369:Aged, 80 and over; D000726:Androgen Antagonists / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D000740:Anemia / Q000097:blood / Q000139:chemically induced; D018931:Antineoplastic Agents, Hormonal / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D014408:Biomarkers, Tumor / Q000097:blood; D001786:Blood Glucose; D002626:Chemistry, Pharmaceutical; D006454:Hemoglobins / Q000378:metabolism; D006801:Humans; D016729:Leuprolide / Q000009:adverse effects / Q000493:pharmacokinetics / Q000627:therapeutic use*; D007986:Luteinizing Hormone / Q000097:blood; D008297:Male; D008875:Middle Aged; D017430:Prostate-Specific Antigen / Q000097:blood; D011471:Prostatic Neoplasms / Q000097:blood / Q000188:drug therapy*; D013739:Testosterone / Q000097:blood; D016896:Treatment Outcome
D000726:Androgen Antagonists; D018931:Antineoplastic Agents, Hormonal; D014408:Biomarkers, Tumor; D001786:Blood Glucose; D006454:Hemoglobins; D013739:Testosterone; D007986:Luteinizing Hormone; D017430:Prostate-Specific Antigen; D016729:Leuprolide