Arnon R, Hurwitz E, Sela M
Recent Results Cancer Res. 1980;75:236-45. doi: 10.1007/978-3-642-81491-4_37.
Daunomycin conjugates to antitumor antibodies prepared either by direct binding or by binding via dextran retain both the antibody and the drug activity. Thus, the exert specific cytotoxicity in vitro toward tumor cells that the antibodies recognize. The macromolecular conjugates are able to penetrate the cells and concentrate in or on the nuclei. In vivo, the antitumor antibodies accumulate preferentially at the tumor metastases. Daunomycin-antibody conjugates are more active than the free drug in prolongation of survival of mice transplanted with the YAC lymphoma cells.
通过直接结合或经由葡聚糖结合制备的柔红霉素与抗肿瘤抗体的缀合物保留了抗体和药物活性。因此,它们在体外对抗体所识别的肿瘤细胞发挥特异性细胞毒性。大分子缀合物能够穿透细胞并在细胞核内或核上聚集。在体内,抗肿瘤抗体优先在肿瘤转移灶处蓄积。柔红霉素 - 抗体缀合物在延长移植了YAC淋巴瘤细胞的小鼠生存期方面比游离药物更具活性。