Muggia F M, Green M D
Department of Medicine, University of Southern California, Los Angeles 90033.
Crit Rev Oncol Hematol. 1991;11(1):43-64. doi: 10.1016/1040-8428(91)90017-7.
Doxorubicin is an essential component of the treatment of aggressive lymphoma, childhood solid tumors, bone and soft tissue sarcomas, and breast cancer and additional indications are emerging. On the other hand, daunorubicin has occupied the central position of interest in the treatment of acute leukemia. Epirubicin has a spectrum very similar to doxorubicin but lesser toxicity. The ability to protect against cardiotoxicity with ICRF-187 further enhances clinical interest in exploiting modifications in doze intensity to therapeutic advantage. Idarubicin has at least equivalent activity to daunorubicin and doxorubicin in leukemia. New areas of research in relation to anthracycline antibiotics include introduction of new the analogs, insight into mechanisms of resistance, the reversal of multidrug resistance in vitro, the protection of cardiac toxicity, and the study of other important biochemical reactions relevant to cytotoxicity. Orally active anthracyclines such as idarubicin and compounds which lack cross-resistance with the parent drugs or have other mechanisms for cytotoxicity are being developed. It is likely that these modifications will lead to an expanding therapeutic spectrum for these already widely useful drugs.
多柔比星是侵袭性淋巴瘤、儿童实体瘤、骨与软组织肉瘤及乳腺癌治疗的重要组成部分,且新的适应证不断涌现。另一方面,柔红霉素在急性白血病治疗中占据着核心地位。表柔比星的光谱与多柔比星非常相似,但毒性较小。用ICRF - 187预防心脏毒性的能力进一步增强了人们对利用剂量强度调整来获得治疗优势的临床兴趣。伊达比星在白血病治疗中的活性至少与柔红霉素和多柔比星相当。与蒽环类抗生素相关的新研究领域包括新型类似物的引入、耐药机制的深入了解、体外多药耐药的逆转、心脏毒性的保护以及与细胞毒性相关的其他重要生化反应的研究。正在研发口服活性蒽环类药物,如伊达比星以及与母体药物无交叉耐药或具有其他细胞毒性机制的化合物。这些改进很可能会使这些已广泛应用的药物治疗谱得到拓展。