Schneider M R, Schiller C D, Humm A, von Angerer E
Institut of Pharmazie, Universität Regensburg, Federal Republic of Germany.
J Cancer Res Clin Oncol. 1991;117(1):33-6. doi: 10.1007/BF01613193.
The anti-oestrogen zindoxifene was originally developed as a drug for the treatment of hormone-dependent mammary carcinomas. Experiments with rats bearing androgen-dependent prostatic tumours revealed anti-neoplastic activity of zindoxifene on these tumours also. Therefore, the inhibitory effect of this drug was studied in various prostatic tumour models in comparison to the anti-oestrogen tamoxifen and to castration. The growth of the hormone-dependent Dunning R3327 H tumour was strongly inhibited by zindoxifene (4 mg/kg), which was more effective than tamoxifen (43% T/C vs 87% T/C, the ratios of tumour weights in control and drug-treated rats). Zindoxifene was able to delay the relapse of these tumours by 7 weeks in comparison to castration. The experiments with Noble Nb-R prostatic tumours showed that administration of zindoxifene (5 mg) is superior to castration (5% T/C vs 52% T/C). The growth of tumours in castrated rats was completely inhibited by administration of zindoxifene. Therefore a peripheral mode of action has to be assumed.
抗雌激素药物津多昔芬最初是作为一种治疗激素依赖性乳腺癌的药物开发的。对患有雄激素依赖性前列腺肿瘤的大鼠进行的实验表明，津多昔芬对这些肿瘤也具有抗肿瘤活性。因此，与抗雌激素他莫昔芬和去势相比，在各种前列腺肿瘤模型中研究了这种药物的抑制作用。津多昔芬（4mg/kg）强烈抑制激素依赖性邓宁R3327H肿瘤的生长，其效果比他莫昔芬更显著（对照组与药物治疗组大鼠肿瘤重量之比为43%T/C对87%T/C）。与去势相比，津多昔芬能够将这些肿瘤的复发延迟7周。对诺布尔Nb-R前列腺肿瘤的实验表明，给予津多昔芬（5mg）优于去势（5%T/C对52%T/C）。给去势大鼠给药津多昔芬可完全抑制肿瘤生长。因此，必须假定其作用方式为外周作用。
