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多聚(L-谷氨酸)-紫杉醇偶合物在抗癌治疗中的新进展

宋依凝, 张双庆*, 张振清*   

  1. 北京毒物药物研究所 药物代谢与药代动力学实验室, 北京 100850
  • 收稿日期:2009-06-05 修回日期:2009-08-10 出版日期:2009-09-15 发布日期:2009-09-15
  • 通讯作者: 张双庆*, 张振清*

New progress in the study of poly (L-glutamic acid)-paclitaxel conjugates for cancer treatment

Yi-Ning Song, Shuang-Qing Zhang*, Zhen-Qing Zhang*   

  1. Laboratory of Drug Metabolism and Pharmacokinetics, Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China
  • Received:2009-06-05 Revised:2009-08-10 Online:2009-09-15 Published:2009-09-15
  • Contact: Shuang-Qing Zhang*, Zhen-Qing Zhang*

摘要: 抗癌药物-聚合物偶合物的应用是抗癌治疗的一个有效发展方向。抗癌药物-聚合物偶合物是将适合的聚合物载体、生物可降解的连接体以及具有生物学活性的抗癌药物连接在一起, 形成了新型抗癌药物的发展方向。多聚(L-谷氨酸)-紫杉醇偶合物(PG-PTX), 将传统抗癌药物紫杉醇和多聚谷氨酸接连起来, 是抗癌药物-聚合物偶合物中极具代表性的药物。PG-PTX偶合物能够提高紫杉醇的抗癌活性, 增强紫杉醇治疗的安全性和效能, 以及改善单独应用紫杉醇引起的不良药动学特性等。因此, PG-PTX偶合物的应用对于许多人类恶性肿瘤的临床治疗都起到了重要的促进作用。

关键词: 紫杉醇, 多聚(L-谷氨酸)-紫杉醇偶合物, 药代动力学

Abstract: The preparation of polymer-anticancer drug conjugates is an effective way to improve the efficacy and decrease the toxicity of anticancer drugs. Polymer-drug conjugates, which were made by combining a suitable polymeric carrier, a biodegradable linker and a bioactive anticancer agent, could form the basis of a new generation of anticancer agents. Poly (L-glutamic acid)-paclitaxel conjugate is a polymer-drug conjugate that links anticancer agent paclitaxel (PTX) to poly (L-glutamic acid) (PG). PG-PTX conjugate can improve the anticancer activity, enhance the safety and efficacy, and improve the pharmacokinetic properties of PTX. Therefore, the application of PG-PTX facilitates the clinical therapy of a variety of human cancers.

Key words: Paclitaxel, Paclitaxel, Poly (L-glutamic acid)-paclitaxel conjugate, Poly (L-glutamic acid)-paclitaxel conjugate, Pharmacokinetics, Pharmacokinetics

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Supporting:

Foundation items: National Key Technologies R & D Program for New Drugs (Grant No. 2009ZX09301-002, 2009ZX09304-004).
*Corresponding authors. Tel.: 86-10-66874610; e-mail: zhangshq@hotmail.com (Shuang-Qing Zhang, Ph.D.)
Tel.: 86-10-66930632; e-mail: zqzhang55@yahoo.com (Zhen-Qing Zhang, Prof.)