Verweij J, Clavel M, Chevalier B
Dept. of Medical Oncology, Rotterdam Cancer Institute, The Netherlands.
Ann Oncol. 1994 Jul;5(6):495-505. doi: 10.1093/oxfordjournals.annonc.a058903.
Paclitaxel and docetaxel are the two presently clinically available representatives of the new class of taxane drugs. They share major parts of their structures and mechanisms of action, but differ in several other aspects. For instance, there is a difference in their tubulin polymer generation, and docetaxel appears twice as active in depolymerization inhibition. In vitro docetaxel also tends to be more potent in different cell lines and investigational models. While in vitro and in vivo studies suggest that prolonged exposure to paclitaxel is better than a brief exposure, no such tendency is seen for docetaxel, indicating it to be a schedule-independent drug. Clinical studies have not confirmed an advantage for prolonged exposure to paclitaxel; but do show differences in the toxicity profiles of the two drugs. These topics will be addressed in detail.
紫杉醇和多西他赛是目前临床上可获得的紫杉烷类新药的两类代表药物。它们在结构和作用机制上有大部分相同之处，但在其他几个方面存在差异。例如，它们在微管蛋白聚合物生成方面存在差异，多西他赛在抑制解聚方面的活性是紫杉醇的两倍。在体外，多西他赛在不同细胞系和研究模型中往往也更具效力。虽然体外和体内研究表明，长时间接触紫杉醇比短时间接触效果更好，但多西他赛没有这种趋势，这表明它是一种给药方案不依赖的药物。临床研究尚未证实长时间接触紫杉醇有优势；但确实显示出这两种药物在毒性方面存在差异。这些主题将详细阐述。
