摘要
小细胞肺癌 (SCLC)治疗新药盐酸拓扑替康 (topotecan)属喜树碱类 ,为拓扑异构酶Ⅰ抑制剂 ,它能导致DNA复制叉断裂 ,该作用方式决定其不易产生耐药性。其剂量限制毒性 (DLT)为中性粒细胞减少和腹泻 ,肝肾功能下降会降低最大耐受剂量 (MTD)。拓扑替康对SCLC最常用的有效剂量是 1.5mg·m-2 ·d-1× 5d。临床前实验发现 ,拓扑替康对耐药SCLC细胞株NCL H82rasH的杀瘤作用比单独使用顺铂的作用强 2 5 0倍 ,与顺铂或VP16有协同作用。临床试验结果亦证明 ,拓扑替康是有效的一线及二线抗肿瘤药 ,尤其对于既往化疗敏感而又复发处于进展期的患者及对颅内转移的症状和体征有明显的缓解作用。
Topotecan,a new agent for SCLC treatment,is a topo is onerase inhibitor.It can induce the fragmentation of DNA replication fork,theref ore it is not easy to produce drug resistance.The dose limiting toxicity(DLT) o f it was neutropenia and diarrhea.Its maximum tolerance dose(MTD) may be reduced by elevated liver or kidney function.The usual dose for SCLC treatment is 1.5 m g·m -2 ·d -1 ×5d.Pre clinical trials indicated that the cancer killi ng effect of topotecan is as potent as 250 times of cisplatin for drug resistanc e cancer strain of NCL H82rasH,and it has a synergetic effect with cisplatin or VP16.Clinical trials indicated that topotecan is an anticancer agent of first o r second choice,especially for patients who are sensitive to anticancer agent in the past and replicated now.The agent can significantly relief the symptoms and signs of brain metastasis of lung cancer.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2001年第10期743-746,共4页
Chinese Journal of New Drugs