Orditura Michele, Quaglia Fabiana, Morgillo Floriana, Martinelli Erika, Lieto Eva, De Rosa Giuseppe, Comunale Daniela, Diadema Maria Rosaria, Ciardiello Fortunato, Catalano Giuseppe, De Vita Ferdinando
Division of Medical Oncology, F. Magrassi-A. Lanzara Department of Clinical and Experimental Medicine and Surgery, Second University of Naples School of Medicine, Via S. Pansini 5, 80131 Naples, Italy.
Oncol Rep. 2004 Sep;12(3):549-56.
Anthracyclines are among the most active antineoplastic drugs developed to date, used both in the treatment of solid cancers, such as breast and ovarian cancer and sarcomas, and of hematologic cancers. However, their clinical use is limited by cardiotoxicity, which is observed at a range of 0.4-41%. The risk of this side effect can be minimized by using cardioprotective agents, planning dosing schedules to lower the anthracycline peak plasma concentration, identifying and monitoring high-risk patients, keeping in mind that early anthracycline-induced histologic changes may be identified successfully by cardiac biopsy. Nonetheless, the challenge to increase the tumor response to chemotherapy while keeping low the cardiac risk may be now met by the use of a recently introduced polyethylene glycol-coated (pegylated) liposomal doxorubicin (PLD). Here, we review the pharmacologic properties of PLD as well as the results of phases I, II and III trials demonstrating activity and low cardiac toxicity associated with the use of this novel drug.
蒽环类药物是迄今为止研发出的最有效的抗肿瘤药物之一,可用于治疗实体癌,如乳腺癌、卵巢癌和肉瘤,以及血液系统癌症。然而,它们的临床应用受到心脏毒性的限制,心脏毒性的发生率在0.4%至41%之间。使用心脏保护剂、规划给药方案以降低蒽环类药物的血浆峰值浓度、识别和监测高危患者,可将这种副作用的风险降至最低,同时要记住,早期蒽环类药物引起的组织学变化可通过心脏活检成功识别。尽管如此,目前使用最近推出的聚乙二醇包被(聚乙二醇化)脂质体阿霉素(PLD)可能应对在保持低心脏风险的同时提高肿瘤对化疗反应的挑战。在此,我们综述了PLD的药理特性以及I期、II期和III期试验的结果,这些试验证明了使用这种新药具有活性且心脏毒性低。