前立腺癌(未治療例)に対する3ヵ月徐放型LH-RH agonist,TAP-144-SR(3M)(リュープリンSR注射用キット11.25)の臨床効果の検討

Abstract

前立腺癌10例(平均73.1歳)を対象に, TAP-144-SR(3M)(TAP-144として11.25mg含有)を単回皮下投与した.因果関係が否定できない有害事象はなく, 忍容性に問題はなかった.血清中テストステロン濃度は投与2日後まで一過性に上昇したが, 3週後には去勢レベル以下となり, 12週後まで抑制された.血清中TAP-144濃度は, 投与3時間後にCmaxに達し, その後1～12週後まで0.2ng/mlで推移した.前立腺癌取り扱い規約中の「前立腺癌の非観血的治療効果判定基準」による総合評価の投与12週後の奏効率は, 100%であった.又, 血清中PSA濃度は, 投与12週後に9例で正常値となった.以上の成績をTAP-144-SR(1M)の3回投与試験と比較したところ, 安全性, ホルモン動態, 有効性とも同等であった

TAP-144-SR (3M) is a 3-month sustained releasing injection of a super-active agonist of luteinizing hormone releasing hormone (LH-RH), leuprorelin acetate. At the Department of Urology of Gunma University Hospital, TAP-144-SR (3M) was injected once subcutaneously into 10 prostatic cancer patients who had had no treatment in the past to investigate safety, serum testosterone levels, drug concentrations and efficacy. In safety, no problematic adverse reactions occurred, and the drug was well tolerated. Serum testosterone levels elevated temporarily up to 2 days after injection and then were reduced rapidly. The levels were reduced below the castration level (100 ng/dl) after 3 weeks and then remained reduced up to 12 weeks. Serum TAP-144 levels including metabolite M-I, elevated to maximal plasma concentration up to 3 hours after injection and then were maintained at about 0.2 ng/ml between 1 week and 12 weeks after injection. With respect to the anti-tumor effects, the response rate according to "criteria of prostate cancer" at 12 weeks after injection was 100% (stable response cases) and the ratio of PSA normalization at 12 weeks was 90%. These results showed that an injection of TAP-144-SR (3M) was well tolerated in prostate cancer patients having no prior treatment and inhibited serum testosterone persisting for at least 12 weeks so that TAP-144-SR (3M) was concluded to be safe and clinically effective for prostate cancer patients.