[Clinical effect of slow release (depot) formulation of the LH-RH analogue ICI 118630 (Zoladex) in patients with prostatic carcinoma].
The antitumor effect and safety and endocrinological effect of a depot formulation of luteinizing hormone-releasing hormone (LH-RH) analogue ICI 118630 (Zoladex) were studied. Each depot containing 3.6 mg of ICI 118630 (corresponding to the average daily release of 120 micrograms) was subcutaneously injected 3 times at 4 week intervals to 12 prostate cancer patients in total at 4 centers from August 1984 to March 1985. Of the 12 patients, 7 showed an objective clinical response (1 CR and 6 PR patients), 3 showed no change and the remaining 2 showed PD. Overall subjective improvement was obtained in 8 of 10 patients (80.0%). Serum hormone levels (LH, FSH, and testosterone) increased immediately after injection of depot and then significantly decreased during and after 2 weeks of treatment. These changes seen in 100% of the patients were attributable to the pharmacological action of the drug. Medical castration was attained in 3.1 +/- 0.9 weeks on average. Observed side effects included gynecomastia in 1 and hyperlipidemia in 2 patients which were all mild. The trial was continued in the patients who required no special medical treatment. Changes in blood Zoladex concentrations suggested no accumulation. These findings demonstrate the safety and useful endocrinological and antitumor effects of Zoladex in prostate cancer through its pharmacological action, that is, LH-RH agonistic action.
D000368:Aged; D002064:Buserelin / Q000031:analogs & derivatives* / Q000627:therapeutic use; D003692:Delayed-Action Preparations; D004334:Drug Administration Schedule; D004341:Drug Evaluation; D005640:Follicle Stimulating Hormone / Q000097:blood; D017273:Goserelin; D006801:Humans; D007986:Luteinizing Hormone / Q000097:blood; D008297:Male; D008875:Middle Aged; D011471:Prostatic Neoplasms / Q000097:blood / Q000188:drug therapy* / Q000473:pathology; D013739:Testosterone / Q000097:blood
D003692:Delayed-Action Preparations; D017273:Goserelin; D013739:Testosterone; D007986:Luteinizing Hormone; D005640:Follicle Stimulating Hormone; D002064:Buserelin