Initial testing (stage 1) of eribulin, a novel tubulin binding agent, by the pediatric preclinical testing program
Initial testing (stage 1) of eribulin, a novel tubulin binding agent, by the pediatric preclinical testing program
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DOI：
10.1002/pbc.24517
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发表时间：
2013-08-01
影响因子：
3.2
通讯作者：
Smith, Malcolm A.
中科院分区：
文献类型：
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作者：
Kolb, E. Anders;Gorlick, Richard;Smith, Malcolm A.
背景抗分裂药物是治疗儿童急性白血病和许多实体瘤的重要药物。灯盏花素是一种不同于长春花碱和紫杉烷的新型药物，它与微管蛋白聚合物的结合方式不同。方法：在第21天重复q4dx3程序，以0.1 nM至1.0M的浓度与PPTP体外细胞系小组进行对比试验，并以1 mg/kg(实体瘤)或1.5 mg/kg(所有模型)的剂量与体内异种移植小组进行对照。结果灯盏花素体外具有细胞毒作用，其相对IC50值的中位数为0.27 nM(范围
Background Antimitotic agents are essential components for curative therapy of pediatric acute leukemias and many solid tumors. Eribulin is a novel agent that differs from both Vinca alkaloids and taxanes in its mode of binding to tubulin polymers. Procedures Eribulin was tested against the PPTP in vitro cell line panel at concentrations from 0.1nM to 1.0M and against the PPTP in vivo xenograft panels at a dose of 1mg/kg (solid tumors) or 1.5mg/kg (ALL models) using a q4dx3 schedule repeated at Day 21. Results In vitro eribulin demonstrated cytotoxic activity, with a median relative IC50 value of 0.27nM, (range