拓扑替康在临床应用的研究进展

拓扑替康 (topotecan ,TPT)是新的喜树碱衍生物。TPT是DNA拓扑异构酶Ⅰ抑制剂。 1996年FDA批准治疗小细胞肺癌 (SCLC)和卵巢癌(OVC)。临床试验表明 ,TPT与顺铂和紫杉醇无交叉耐药性。TPT单药治疗SCLC的效果与目前的一线治疗方案相当。TPT单药治疗OVC的效果相同或好于紫杉醇 ,TPT单药或结合治疗作为一线药物 ,治疗SCLC和OVC进行了很多研究并得到肯定的结果。TPT是少有的能进入血脑屏障的药物之一 ,口服TPT与静脉注射效果相同 ,但有低的骨髓抑制毒性。TPT单药或结合治疗也对白血病、非何杰金病、骨髓异常增生症、选择性胰腺癌有效

Progress of clinical trial study of topotecan

Topotecan(TPT) is a novel derivative of comptothecin. TPT is DNA topoisomerase I inhibitor. FDA approved TPT as a treatment drug for small cell lung cancer(SCLC) and ovarian cancer(OVC) in 1996. Clinical non cross resistance had been demonstrated between TPT and cisplatin or paclitaxel. The TPT single agent was as active as first line therapy regiments in SCLC. Single TPT was as well as or better than paclitaxel for OVC. Single agent TPT or TPT based combination regiments were under investigation in numerous studies for first line therapy in SCLC and OVC and clinical results demonstrated that TPT was good active. TPT is one of the very few chemotherapy drugs that cross the blood brain barrier. Oral TPT is similar in efficacy to intravenous TPT and has less hematologic toxicity than the intravenous TPT. Clinical trials show that both single agent TPT and TPT based combination agents are effective in treatment of leukemias, non Hodgkin's lymphomas,myelodysplastic syndrome and selected pediatric cancer.