Fields S M, Koeller J M
University of Texas Health Science Center, San Antonio 78284.
DICP. 1991 May;25(5):505-17. doi: 10.1177/106002809102500511.
Because of its in vitro activity in leukemic cell lines and Phase I studies of acute leukemia, Phase II and III clinical trials with idarubicin hydrochloride were conducted in patients with acute lymphocytic leukemia or acute nonlymphocytic leukemia. In the Phase III comparative trials between the combinations of idarubicin and cytarabine and daunorubicin hydrochloride and cytarabine, the idarubicin/cytarabine combination resulted in significantly greater complete remission rates and longer overall survival in two of three studies conducted in the US. As a result, the Food and Drug Administration approved intravenous idarubicin with a Class 1A rating in September 1990 for use in combination with other antileukemic drugs (e.g., cytarabine) for the treatment of acute myelogenous leukemia in adults. The recommended dose of idarubicin is 12 mg/m2 daily for three days by slow intravenous injection in combination with cytarabine. Although idarubicin causes myelosuppression similar to that described with daunorubicin, the incidence of cardiotoxicity in animal models is lower. Idarubicin also has the advantage of oral administration, but the oral formulation of the drug remains investigational. The use of idarubicin in pediatric patients also remains to be established.
由于其在白血病细胞系中的体外活性以及急性白血病的I期研究，开展了盐酸伊达比星针对急性淋巴细胞白血病或急性非淋巴细胞白血病患者的II期和III期临床试验。在美国进行的三项研究中的两项里，在盐酸伊达比星与阿糖胞苷联合用药和柔红霉素与阿糖胞苷联合用药的III期对比试验中，伊达比星/阿糖胞苷联合用药产生了显著更高的完全缓解率和更长的总生存期。因此，美国食品药品监督管理局于1990年9月批准静脉注射伊达比星，评定等级为1A类，用于与其他抗白血病药物（如阿糖胞苷）联合治疗成人急性髓性白血病。伊达比星的推荐剂量是与阿糖胞苷联合使用时，每日12 mg/m²，缓慢静脉注射，连用三天。虽然伊达比星引起的骨髓抑制与柔红霉素类似，但在动物模型中其心脏毒性的发生率较低。伊达比星还具有口服给药的优势，但该药物的口服制剂仍处于研究阶段。伊达比星在儿科患者中的应用也有待确定。
