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伊立替康(irinotecan,CPT-11)是喜树碱类衍生物,属拓扑异构酶Ⅰ(Topo Ⅰ)抑制剂,最早由日本研制开发,1987年开始Ⅰ期临床实验,1998年获得美国FDA批准,用于标准化疗方案治疗失败后转移性结直肠癌的一线治疗。其作用机制在于,通过与DNA Topo Ⅰ结合,阻碍DNA的复制和RNA转录,从而发挥抗肿瘤作用。肿瘤细胞中Topo Ⅰ的浓度越
The irinotecan (CPT-11) is a camptothecin derivative. It belongs to the topoisomerase Ⅰ (Topo Ⅰ) inhibitor and was first developed in Japan. Phase Ⅰ clinical trial started in 1987 and obtained FDA Approved for first-line treatment of metastatic colorectal cancer following failure of standard chemotherapy regimens. Its mechanism of action is to exert anti-tumor effects by binding to DNA Topo I, hindering DNA replication and RNA transcription. The higher the concentration of Topo I in tumor cells