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Docetaxel

多西他賽
Mechanism of action:
Docetaxel 是一種半合成紫杉醇類(semisynthetic taxane)衍生物,源自歐洲紅豆杉(Taxus baccata)的天然前驅物 10-去乙醯巴卡亭III(10-deacetylbaccatin III)。Docetaxel 可與 β-微管蛋白(β-tubulin)高親和力結合,促進游離微管蛋白聚合形成微管。Docetaxel 藉由穩定微管結構,阻止其正常的解聚合(depolymerization),導致微管無法動態重組。細胞有絲分裂時期的紡錘體(mitotic spindle)主要由微管組成,docetaxel 的作用會導致紡錘體無法正常形成,使細胞停滯於中期(metaphase),最終誘發細胞凋亡。
Reference(s):
1. Kenmotsu H et al. (2015). Pharmacokinetics, dynamics and toxicity of docetaxel: Why the Japanese dose differs from the Western dose. Cancer Sci.
2. Hendrikx JJ et al. (2013). Quantification of docetaxel and its metabolites in human plasma by liquid chromatography/tandem mass spectrometry. Rapid Commun Mass Spectrom.
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