Koiso Kenkichi, Akaza Hideyuki, Naito Seiji, Usami Michiyuki, Tsukamoto Taiji, Shimazaki Jun, Kotake Toshihiko, Yamanaka Hidetoshi, Oohashi Yasuo, Yoshinaka Ryoji, Onouchi Hitoshi, Yokokawa Kiyoshi
Senpo Tokyo Takanaka Hospital.
Hinyokika Kiyo. 2002 Dec;48(12):781-95.
A randomized, multicenter, double-blind, parallel-group study was conducted in order to evaluate the hormonal kinetics, pharmacokinetics, efficacy and safety of TAP-144-SR (3M) a three-month sustained-release injectable preparation of leuprorelin acetate, a highly active luteinizing hormone-releasing hormone (LH-RH) derivative by comparing the treatment with two subcutaneous doses of the test medication TAP-144-SR (3M) and the treatment with six subcutaneous doses of the reference medication TAP-144-SR (1M), a 1-month sustained-release injectable preparation. Study participants were 103 patients with prostate cancer in whom a stable anti-tumor effect had been obtained with Leuplin Injection 3.75. The hormonal kinetics revealed that the proportion of the patients "maintaining the castration level of serum testosterone (maximum serum testosterone level during treatment below the castration level [100 ng/dl])" was 100% in both treatment groups. With regard to the efficacy, the proportions of the patients in whom the anti-tumor effects (> or = Stable) of the baseline treatment prior to the initiation of the treatment with the study medication were maintained during the study treatment period (6 months) were comparable; 84.0% with TAP-144-SR (1M) and 80.4% with TAP-144-SR (3M). On evaluation of the pharmacokinetics, the mean value of AUC1-12w of the serum TAP-144 concentration (including the metabolite M-I) for the treatment with TAP-144-SR (3M) was 77.0% that of the treatment with TAP-144-SR (1M). Adverse events were similar in the subjects on TAP-144-SR (3M) and in those on TAP-144-SR (1M). There existed no big differences in kind, incidence or time of occurrence of adverse events between two groups. TAP-144-SR (3M) showed no clinically relevant findings in particular. These results indicate that one dose of TAP-144-SR (3M) is comparable to three doses of the already approved Leuplin injection 3.75 in serum testosterone level-inhibitory effect, efficacy and safety. Hence, it is considered that TAP-144-SR (3M) is a drug suitable for treatment of prostate cancer over a prolonged period of time.
为了评估TAP - 144 - SR（3M）（一种醋酸亮丙瑞林的三个月缓释注射制剂，醋酸亮丙瑞林是一种高活性促黄体生成激素释放激素（LH - RH）衍生物）的激素动力学、药代动力学、疗效和安全性，进行了一项随机、多中心、双盲、平行组研究，将试验药物TAP - 144 - SR（3M）的两个皮下注射剂量治疗与参比药物TAP - 144 - SR（1M）（一种一个月缓释注射制剂）的六个皮下注射剂量治疗进行比较。研究参与者为103例前列腺癌患者，这些患者使用亮丙瑞林注射液3.75已获得稳定的抗肿瘤效果。激素动力学显示，两个治疗组中“维持血清睾酮去势水平（治疗期间最大血清睾酮水平低于去势水平[100 ng/dl]）”的患者比例均为100%。关于疗效，在研究治疗期（6个月）内，维持研究药物治疗开始前基线治疗的抗肿瘤效果（≥稳定）的患者比例相当；TAP - 144 - SR（1M）组为84.0%，TAP - 144 - SR（3M）组为80.4%。在药代动力学评估中，TAP - 144 - SR（3M）治疗的血清TAP - 144浓度（包括代谢物M - I）的AUC1 - 12w平均值为TAP - 144 - SR（1M）治疗的77.0%。TAP - 144 - SR（3M）组和TAP - 144 - SR（1M）组受试者的不良事件相似。两组不良事件的种类、发生率或发生时间没有显著差异。TAP - 144 - SR（3M）尤其未显示出临床相关的发现。这些结果表明，一剂TAP - 144 - SR（3M）在血清睾酮水平抑制作用、疗效和安全性方面与已获批的亮丙瑞林注射液3.75的三剂相当。因此，认为TAP - 144 - SR（3M）是一种适合长期治疗前列腺癌的药物。
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