Omoto S, Kondo S, Fukatsu S, Takeuchi T, Umezawa K, Tsuchiya T, Umezawa S
Meiji Seika Kaisha, Ltd., Tokyo, Japan.
Drugs Exp Clin Res. 1988;14(7):435-9.
ME2303 (FAD-104) is a new anthracycline antibiotic whose structure is characterized by the presence of a 2'-fluoro atom and the lack of a 3'-amino group in the sugar moiety. Its cytocidal activity is superior to or equal to that of adriamycin (ADM). The LD50 value of ME2303 was about 140 mg/kg i.v. in mice and this value was about 7-fold higher than that of ADM. ME2303 was administered intravenously to Golden strain hamsters at doses of 25, 50, 75 and 150 mg/kg and the ECG was examined. From ECG changes, it seems that ME2303 did not show any effect on the heart in acute toxicity. Mutagenicity was recognized as with ADM in the back-mutation test.
ME2303(FAD - 104)是一种新型蒽环类抗生素,其结构特点是在糖部分存在2'-氟原子且缺少3'-氨基。其杀细胞活性优于或等同于阿霉素(ADM)。ME2303在小鼠体内静脉注射的半数致死量(LD50)约为140mg/kg,该值比阿霉素高约7倍。以25、50、75和150mg/kg的剂量给金黄仓鼠静脉注射ME2303,并检查心电图。从心电图变化来看,ME2303在急性毒性中似乎对心脏没有任何影响。在回复突变试验中,ME2303与阿霉素一样具有致突变性。