Martini A, Donelli N G, Mantovani A, Pacciarini M A, Fogar-Ottaviano E F, Morasca L, Garattini S, Spreafico F S
Oncology. 1977;34(4):173-8. doi: 10.1159/000225216.
In C57B1/6 mice bearing the intramuscular Lewis lung carcinoma, single intravenous doses of Adriamycin showed an higher antineoplastic effectiveness on the primary tumor and its lung metastasis than equal doses of its analog Daunomycin. The in vitro cell-binding of Daunomycin to these tumor cells was higher than that of Adriamycin, but no differences in cytotoxicity were found between the two agents. Pharmacokinetic studies revealed that Adriamycin (and/or its metabolites) accumulated in the neoplastic tissue more promptly, in significantly greater quantities and for longer periods than Daunomycin. The possible importance of these findings in explaining the greater therapeutic activity of Adriamycin in experimental animals is discussed.
在携带肌肉内Lewis肺癌的C57B1/6小鼠中,单剂量静脉注射阿霉素对原发性肿瘤及其肺转移的抗肿瘤效果高于同等剂量的类似物柔红霉素。柔红霉素与这些肿瘤细胞的体外细胞结合率高于阿霉素,但两种药物的细胞毒性没有差异。药代动力学研究表明,与柔红霉素相比,阿霉素(和/或其代谢物)在肿瘤组织中积累得更快、数量更多、时间更长。讨论了这些发现对于解释阿霉素在实验动物中具有更大治疗活性的可能重要性。