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目的:全面介绍新型抗癌药紫杉醇的全合成路线、药理作用机制、药效学、药动学、治疗应用和毒性作用。方法:查阅近期有关紫杉醇的大量文献。结果:紫杉醇不仅对治疗卵巢癌和乳腺癌有确切疗效,而且对抑制肺癌、头颈部癌、恶性黑色素瘤等多种实体癌显示了可喜的结果。紫杉醇的药动学行为似乎不是线性的,肝代谢和胆汁的清除是紫杉醇清除的主要途径。紫杉醇的剂量限制性毒性是中性粒细胞减少和外周神经病变。结论:紫杉醇是一个作用机理新颖的新型抗癌药,具有广谱抗癌活性,临床应用前景广阔。
OBJECTIVE: To introduce the full synthetic route of paclitaxel, a pharmacological action mechanism, pharmacodynamics, pharmacokinetics, therapeutic application and toxicity. Methods: Review of recent literature on paclitaxel. Results: Paclitaxel not only has the exact effect on the treatment of ovarian cancer and breast cancer, but also shows gratifying results on inhibiting various solid cancers such as lung cancer, head and neck cancer and malignant melanoma. The pharmacokinetic behavior of paclitaxel appears to be not linear, and hepatic metabolism and bile clearance are the main routes of paclitaxel clearance. Dose-limiting toxicity of paclitaxel is neutropenia and peripheral neuropathy. Conclusion: Paclitaxel is a novel anticancer drug with broad spectrum anticancer activity and broad prospects for clinical application.