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紫杉醇(泰素)和多西他赛(泰索帝):肺癌的有效化疗药物。

Paclitaxel (Taxol) and docetaxel (Taxotere): active chemotherapeutic agents in lung cancer.

作者信息

Francis P A, Kris M G, Rigas J R, Grant S C, Miller V A

机构信息

Department of Medicine, Memorial Sloan-Kettering Cancer Center, New York, NY, USA.

出版信息

Lung Cancer. 1995 Apr;12 Suppl 1:S163-72. doi: 10.1016/0169-5002(95)00432-z.

Abstract

Paclitaxel (Taxol), the prototype of a new class of plant-derived antineoplastic compounds, is a natural product isolated from the Pacific yew. Docetaxel (Taxotere) is a hemisynthetic product derived from the European yew. These agents share a unique mechanism of cytotoxic action by promoting assembly of microtubules and rendering the microtubules resistant to depolymerization. In vitro studies suggest a possible role for radiation sensitization. In Phase I trials, the dose-limiting toxicity was neutropenia for both agents. Other toxicities include infusion-related hypersensitivity reactions, alopecia, neurotoxicity, mucositis, diarrhoea and myalgias. To prevent infusion-related reactions, routine premedication is recommended. Noncumulative cardiac toxicity has been observed with paclitaxel. Fluid retention and rash have been reported with docetaxel. In Phase II studies of paclitaxel in advanced non-small cell lung cancer, response rates of 21% and 24% were observed. In Phase II studies of docetaxel in similar patients, response rates ranging from 28-38% were reported, including patients previously treated with cisplatin. The most common toxicity in these studies was neutropenia. Combination studies with cisplatin and other agents are in progress. Paclitaxel and docetaxel are among the most active chemotherapeutic agents for non-small cell lung cancer patients. Their testing will dominate trials of new therapies in this disease for years to come.

摘要

紫杉醇(泰素)是一类新型植物源抗肿瘤化合物的原型,是从太平洋紫杉中分离出的一种天然产物。多西他赛(泰索帝)是一种从欧洲紫杉衍生而来的半合成产物。这些药物具有独特的细胞毒性作用机制,可促进微管组装并使微管抵抗解聚。体外研究表明其可能具有放射增敏作用。在Ⅰ期试验中,两种药物的剂量限制性毒性均为中性粒细胞减少。其他毒性包括输注相关的过敏反应、脱发、神经毒性、粘膜炎、腹泻和肌痛。为预防输注相关反应,建议进行常规预处理。已观察到紫杉醇有非累积性心脏毒性。多西他赛有液体潴留和皮疹的报道。在晚期非小细胞肺癌患者中进行的紫杉醇Ⅱ期研究中,观察到的缓解率分别为21%和24%。在类似患者中进行的多西他赛Ⅱ期研究中,报道的缓解率为28% - 38%,包括先前接受顺铂治疗的患者。这些研究中最常见的毒性是中性粒细胞减少。与顺铂及其他药物的联合研究正在进行中。紫杉醇和多西他赛是治疗非小细胞肺癌患者最有效的化疗药物之一。在未来几年,它们的试验将主导该疾病新疗法的试验。

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