Janssens Ann, Boogaerts Marc, Verhoef Gregor
Department of Hematology, University Hospitals Leuven, Campus Gasthuisberg, Leuven, Belgium.
Drug Des Devel Ther. 2009 Dec 29;3:241-52. doi: 10.2147/dddt.s5603.
Fludarabine is an antineoplastic agent used in the treatment of hematological malignancies, particularly chronic lymphocytic leukemia (CLL) and indolent B-cell lymphoma. Because of its immunosuppressive effects, fludarabine has been added to reduced intensity conditioning regimens. The oral formulation of fludarabine has become widely available. Pharmacokinetic studies have shown that an oral dose of 40 mg/m(2)/d would provide systemic drug exposure similar to the standard intravenous (IV) dose of 25 mg/m(2)/d. The oral dose can be taken once daily without any dietary restrictions. Dose adjustments are mandatory in patients with renal impairment to avoid increased toxicity. Several noncomparative trials in previously untreated and treated patients with CLL have shown that treatment with the oral formulation demonstrates similar efficacy compared to historical control groups treated with the IV formulation. The tolerability profile of oral fludarabine seems similar to that of the IV formulation. Myelosuppression and infectious complications are the most frequently reported adverse events. Gastrointestinal toxicity is more frequent with the oral formulation, but is usually of mild or moderate severity. Although oral fludarabine makes treatment more convenient, health care workers must be aware of the compliance behavior of each patient.
氟达拉滨是一种用于治疗血液系统恶性肿瘤，尤其是慢性淋巴细胞白血病（CLL）和惰性B细胞淋巴瘤的抗肿瘤药物。由于其免疫抑制作用，氟达拉滨已被添加到减低强度预处理方案中。氟达拉滨的口服制剂已广泛可得。药代动力学研究表明，口服剂量40mg/m²/d可提供与标准静脉注射（IV）剂量25mg/m²/d相似的全身药物暴露。口服剂量可每日服用一次，无需任何饮食限制。肾功能损害患者必须进行剂量调整以避免毒性增加。在既往未治疗和已治疗的CLL患者中进行的多项非对照试验表明，与接受IV制剂治疗的历史对照组相比，口服制剂治疗显示出相似的疗效。口服氟达拉滨的耐受性似乎与IV制剂相似。骨髓抑制和感染并发症是最常报告的不良事件。口服制剂的胃肠道毒性更常见，但通常为轻度或中度。虽然口服氟达拉滨使治疗更方便，但医护人员必须了解每位患者的依从行为。
