Dowsett M, Jacobs S, Aherne J, Smith I E
Department of Biochemistry, Royal Marsden Hospital, London, U.K.
Clin Ther. 1992;14 Suppl A:97-103.
Premenopausal Study. Twenty-five pre- or perimenopausal patients with advanced breast cancer were treated with leuprorelin acetate 3.75 mg (n = 9) or 7.5 mg (n = 16) every 4 weeks. Serum levels of gonadotrophins and oestrogens were suppressed markedly by both doses and there was no indication that the lower dose was less effective as an oestrogen suppressant. There were four objective responders to the 3.75 mg dose and six to the 7.5 mg dose. Toxicity was confined almost entirely to hot flushes, which occurred in 17 patients. Leuprorelin acetate is therefore an effective agent in the treatment of premenopausal breast cancer patients. There appears to be no major detriment to the use of 3.75 mg rather than the 7.5 mg dose. Postmenopausal Study. Fifteen postmenopausal patients with advanced breast cancer were treated with monthly injections of leuprorelin acetate 7.5 mg to assess the clinical activity and endocrine responses to treatment. None of the 15 patients showed an objective response to treatment, although four patients had stable disease for at least 6 months. Endocrine effects after 4 weeks' treatment included major suppression of serum gonadotrophins to below 10% of pretreatment values and decreases in the level of serum testosterone in 12 of 14 patients. In this group there were no changes in oestradiol levels, although we had previously observed suppression in postmenopausal patients treated with goserelin. In common with other gonadotrophin-releasing hormone analogues, leuprorelin acetate cannot be recommended as a treatment for postmenopausal breast cancer.
绝经前研究。25例绝经前或围绝经期晚期乳腺癌患者接受醋酸亮丙瑞林治疗，每4周注射3.75mg（n = 9）或7.5mg（n = 16）。两种剂量均能显著抑制血清促性腺激素和雌激素水平，没有迹象表明低剂量作为雌激素抑制剂效果较差。3.75mg剂量组有4例客观缓解者，7.5mg剂量组有6例。毒性几乎完全局限于潮热，17例患者出现潮热。因此，醋酸亮丙瑞林是治疗绝经前乳腺癌患者的有效药物。使用3.75mg而非7.5mg剂量似乎没有太大危害。绝经后研究。15例绝经后晚期乳腺癌患者每月注射7.5mg醋酸亮丙瑞林，以评估治疗的临床活性和内分泌反应。15例患者中无一例对治疗有客观反应，尽管有4例患者病情稳定至少6个月。治疗4周后的内分泌效应包括血清促性腺激素大幅抑制至低于治疗前值的10%，14例患者中有12例血清睾酮水平下降。该组雌二醇水平无变化，尽管我们之前在接受戈舍瑞林治疗的绝经后患者中观察到了抑制作用。与其他促性腺激素释放激素类似物一样，醋酸亮丙瑞林不能推荐用于治疗绝经后乳腺癌。
