Fulton B, Spencer C M
Adis International Limited, Auckland, New Zealand.
Drugs. 1996 Jun;51(6):1075-92. doi: 10.2165/00003495-199651060-00011.
Docetaxel is a member of the taxoid class of antineoplastic agents. Its mechanism of action is primarily related to its ability to enhance microtubule assembly and to stabilise microtubules by preventing their depolymerisation, thus disrupting normal cell division. Docetaxel has significant cytotoxic activity against human breast cancer cell lines and freshly explanted human breast cancer cells in vitro. It has also shown activity in mice against mammary tumours and human mammary tumour xenografts. Docetaxel has been investigated in the treatment of patients with advanced and/or metastatic breast cancer in European and North American phase II trials using an initial dose of 100 mg/m2 infused over 1 hour every 3 weeks. As first-line treatment, monotherapy with docetaxel was associated with complete and partial response rates of 5 to 16% and 49 to 53%, respectively, with an overall (complete plus partial) response rate of 54 to 68%. The median overall survival time of patients in one study was > or = 71 weeks. Docetaxel monotherapy has shown impressive activity as second-line therapy in patients with metastatic breast cancer who had relapsed while receiving adjuvant therapy or who had progressive disease following previous treatment, with overall response rates of 53 and 58% reported in 2 studies. A number of issues need to be addressed before the ultimate place of docetaxel in the management of metastatic breast cancer is fully established. The efficacy of docetaxel compared with standard agents and in combination regimens and its effect on quality-of-life aspects require further evaluation. Nevertheless, docetaxel is a promising new agent which has produced impressive clinical results and should be considered an alternative second-line treatment of patients with metastatic breast cancer.
多西他赛是紫杉烷类抗肿瘤药物的一种。其作用机制主要与其增强微管组装以及通过防止微管解聚来稳定微管的能力有关，从而扰乱正常细胞分裂。多西他赛在体外对人乳腺癌细胞系和新鲜分离的人乳腺癌细胞具有显著的细胞毒活性。它在小鼠体内对乳腺肿瘤和人乳腺肿瘤异种移植瘤也显示出活性。在欧洲和北美的II期试验中，已对多西他赛用于治疗晚期和/或转移性乳腺癌患者进行了研究，初始剂量为100mg/m²，每3周静脉滴注1小时。作为一线治疗，多西他赛单药治疗的完全缓解率和部分缓解率分别为5%至16%和49%至53%，总体（完全加部分）缓解率为54%至68%。一项研究中患者的中位总生存时间≥71周。多西他赛单药治疗在接受辅助治疗时复发或先前治疗后病情进展的转移性乳腺癌患者的二线治疗中显示出令人印象深刻的活性，两项研究报告的总体缓解率分别为53%和58%。在多西他赛在转移性乳腺癌治疗中的最终地位完全确立之前，有许多问题需要解决。与标准药物和联合治疗方案相比，多西他赛的疗效及其对生活质量方面的影响需要进一步评估。尽管如此，多西他赛是一种有前景的新药剂，已产生了令人印象深刻的临床结果，应被视为转移性乳腺癌患者的替代二线治疗药物。
