国际肿瘤学杂志

国际肿瘤学杂志 ›› 2017, Vol. 44 ›› Issue (2): 136-138.doi: 10.3760/cma.j.issn.1673422X.2017.02.015

• 综述 • 上一篇    下一篇

伊曲康唑抗肿瘤作用机制

樊则英,张晓东,陈红清   

  1. 523112 东莞，广东省泗安医院皮肤二科
  • 出版日期:2017-02-08 发布日期:2017-01-04
  • 通讯作者: 陈红清，Email: hongqing_chen@hotmail.com E-mail:hongqing_chen@hotmail.com

The mechanism of itraconazole as an anticancer agent

Fan Zeying, Zhang Xiaodong， Chen Hongqing   

  1. Second Department of Dermatology, Guangdong Provincial Si′an Hospital, Dongguan 523112, China
  • Online:2017-02-08 Published:2017-01-04
  • Contact: Chen Hongqing E-mail:hongqing_chen@hotmail.com

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摘要： 体内外实验及临床试验都证实标准治疗剂量的伊曲康唑具有抗肿瘤活性，但其精确作用机制迄今未明，推测与其抑制血管生成、抑制Hedgehog信号传导通路、诱导自噬和逆转多药抗药性有关。伊曲康唑因疗效确切、安全性高、药代动力学明晰，极有可能成为肿瘤临床治疗中“老药新用”的范例。

关键词: 伊曲康唑, 血管生成抑制剂, 信号传导, 抗药性, 多药

Abstract: Itraconazole has potent anticancer activity at the standard therapeutic doses, which is proved in vitro and in vivo preclinical studies, even in active clinical trials. The precise mode of action of itraconazole for its anticancer activity has not been elucidated, however multiple putative mechanisms are proposed, such as antiangiogenesis, inhibition of Hedgehog pathway, autophagy induction and reversal of multidrug resistance. Its high efficacy, known toxicity and wellestablished pharmacokinetics make this generic drug a strong candidate for repurposing as an oncological treatment.

Key words: Itraconazole； Angiogenesis inhibitors； Signal transduction, Drug resistance, multiple