Zittoun R, Marie J P, Delanian S, Suberville A M, Thevenin D
Semin Oncol. 1987 Jun;14(2 Suppl 1):269-75.
In vitro uptake and retention of 3H-cytosine arabinoside (ara-C) was studied in 68 acute myelogenous leukemia (AML) patients (ten were studied twice) treated with a regimen containing conventional (54 patients) or high doses (24) of ara-C. Drug uptake and retention after four hours were measured following 30 minutes exposure to 1 and 50 micrograms/mL of ara-C. A good correlation was observed between high uptake in the acid soluble (AS) fraction (P less than .01), or high retention in the acid insoluble (Al) fraction (P less than .03) of 1 microgram, but not 50 micrograms, of the drug and obtainment of complete remission (CR) in patients treated with conventional doses of ara-C. Patients with a high percentage of ara-C retained in the AS fraction (greater than 26%) have a significantly longer CR duration than patients with a lower level of retention (P less than .02). In 17 patients who achieved a CR in spite of a low tritiated ara-C uptake, the clonogenic leukemic (CFU-L) cells were especially sensitive to drugs (15 of 17 v three of 11 among resisting patients).
对68例接受含常规剂量（54例）或高剂量（24例）阿糖胞苷（ara-C）方案治疗的急性髓性白血病（AML）患者（其中10例接受了两次研究）进行了3H-阿糖胞苷（ara-C）的体外摄取和保留研究。在暴露于1和50微克/毫升阿糖胞苷30分钟后，测量4小时后的药物摄取和保留情况。在接受常规剂量阿糖胞苷治疗的患者中，1微克（而非50微克）药物在酸溶性（AS）部分的高摄取（P<0.01）或在酸不溶性（Al）部分的高保留（P<0.03）与完全缓解（CR）的获得之间观察到良好的相关性。阿糖胞苷在AS部分保留百分比高（>26%）的患者的CR持续时间明显长于保留水平低的患者（P<0.02）。在17例尽管氚标记阿糖胞苷摄取低但仍实现CR的患者中，克隆形成性白血病（CFU-L）细胞对药物特别敏感（17例中有15例，而耐药患者中11例中有3例）。
