蒽环霉素

Q3 Pharmacology, Toxicology and Pharmaceutics WikiJournal of Medicine Pub Date : 2018-12-06 DOI:10.15347/wjm/2018.001
Alison Cheong, Sean McGrath, S. Cutts
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引用次数: 0

摘要

蒽环类药物是临床上重要的一类抗肿瘤药物,用于治疗多种实体癌和血癌。第一个被描述的蒽环类药物,柔红霉素,最早是在20世纪60年代初从一株纯净链霉菌中分离出来的。临床上应用最广泛的是阿霉素、柔红霉素及其半合成衍生物表红霉素和依甲红霉素。它们主要通过插入DNA和抑制拓扑异构酶II起作用,导致DNA断裂和取消DNA合成。使用蒽环类药物最严重的副作用是累积剂量依赖性心脏毒性,将推荐的最大终生治疗限制在400450mg /m2。几种阿霉素脂质体制剂正在使用中,具有延长保留率同时降低游离药物的血浆浓度峰值的好处。一些装载了蒽环类药物的纳米颗粒的临床试验目前正在进行中。
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Anthracyclines
Anthracyclines are a clinically important class of antineoplastic agents used to treat a wide variety of solid and blood cancers. The first described anthracycline, daunorubicin, was first isolated from a strain of Streptomyces peucetius in the early 1960s. Clinically the most widely used are doxorubicin, daunorubicin and their semisynthetic derivatives epirubicin and idarubicin. They primarily act by intercalating with DNA and inhibiting topoisomerase II, resulting in DNA breaks and abrogated DNA synthesis. The most serious side effect of anthracycline use is cumulative dose-dependent cardiotoxicity, limiting recommended maximum lifetime treatment to 400450 mg/m2. Several liposomal formulations of doxorubicin are in use, having the benefits of prolonging retention rate while reducing peak plasma concentration of free drug. Several clinical trials of anthracycline-loaded nanoparticles are currently underway.
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来源期刊
WikiJournal of Medicine
WikiJournal of Medicine Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
0.80
自引率
0.00%
发文量
6
审稿时长
4 weeks
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