Casazza A M, Pratesi G, Giuliani F, Di Marco A
Tumori. 1980 Oct 31;66(5):549-64. doi: 10.1177/030089168006600503.
4-demethoxydaunorubicin was tested against experimental mouse leukemias, in comparison with doxirubicin and daunorubicin. 4-demethoxydaunorubicin, administered ip to mice bearing ascitic L1210 or P388 leukemia was 5 times more potent than daunorubicin and 10 times more potent than doxorubicin (potency established in relation to optimal antitumor doses). At the optimal doses, 4-demethoxydaunorubicin was as active as daunorubicin and less active than doxorubicin. 4-demethoxydaunorubicin, administered iv was 8 times more potent than daunorubicin and 4-5 times more potent than doxorubicin. At the optimal doses, 4-demethoxydaunorubicin was markedly more active than daunorubicin or doxorubicin in mice injected iv with 10(5) L1210 leukemia cells (early or late leukemia) or with 10(2) Gross leukemia cells. In mice given 2 X 10(6) Gross leukemia cells iv, 4-demethoxydaunorubicin was as active as doxorubicin when treatment was given iv on days 1, 5 and 9 for 4-demethoxydaunorubicin, and on days 1, 3 and 6 for daunorubicin and doxorubicin. 4-demethoxydaunorubicin administered orally was highly active against ascitic P388 leukemia and against L1210 and Gross leukemia inoculated iv.
将4-去甲氧基柔红霉素与阿霉素和柔红霉素进行比较，对实验性小鼠白血病进行了测试。给患有腹水型L1210或P388白血病的小鼠腹腔注射4-去甲氧基柔红霉素，其效力比柔红霉素高5倍，比阿霉素高10倍（效力是相对于最佳抗肿瘤剂量确定的）。在最佳剂量下，4-去甲氧基柔红霉素与柔红霉素活性相当，但比阿霉素活性低。静脉注射4-去甲氧基柔红霉素的效力比柔红霉素高8倍，比阿霉素高4 - 5倍。在最佳剂量下，对于静脉注射10(5)个L1210白血病细胞（早期或晚期白血病）或10(2)个格罗斯白血病细胞的小鼠，4-去甲氧基柔红霉素比柔红霉素或阿霉素的活性明显更高。对于静脉注射2×10(6)个格罗斯白血病细胞的小鼠，当4-去甲氧基柔红霉素在第1、5和9天静脉给药，柔红霉素和阿霉素在第1、3和6天静脉给药时，4-去甲氧基柔红霉素与阿霉素活性相当。口服4-去甲氧基柔红霉素对腹水型P388白血病以及静脉接种的L1210和格罗斯白血病具有高活性。
