Scher H I, Sternberg C, Heston W D, Watson R C, Niedzwiecki D, Smart T, Hollander P, Yagoda A
Cancer Chemother Pharmacol. 1986;18(1):24-6. doi: 10.1007/BF00253058.
Etoposide, a semisynthetic derivative of podophyllotoxin, was evaluated concurrently in vitro against a human derived hormone-resistant cell line, PC-3, and in vivo in bidimensionally measurable hormone-resistant human prostatic cancer. In vitro, a dose-response relationship was observed, with 74% inhibition at 10 micrograms/ml (1 h incubation) and greater than 99% inhibition at 90 micrograms/ml, both in the range of clinically achievable concentrations. In vivo, 1 PR (5%, 95% confidence limits 0-12%) of 18+ months was observed in 20 adequately treated patients. The results confirm the limited role of etoposide in hormone-refractory disease and the need for new model systems for evaluation of potential chemotherapeutic compounds in this disease.
依托泊苷是鬼臼毒素的半合成衍生物,同时在体外对人源激素抵抗性细胞系PC-3进行了评估,并在体内对二维可测量的激素抵抗性人类前列腺癌进行了评估。在体外,观察到剂量反应关系,在10微克/毫升(孵育1小时)时抑制率为74%,在90微克/毫升时抑制率大于99%,两者均在临床可达到的浓度范围内。在体内,20例接受充分治疗的患者中有1例出现部分缓解(5%,95%置信区间0-12%),缓解期超过18个月。结果证实了依托泊苷在激素难治性疾病中的作用有限,以及需要新的模型系统来评估该疾病中潜在化疗化合物的必要性。