抗人脑胶质瘤单克隆抗体─—阿霉素免疫交联物在荷瘤鼠体内药代动力学研究

Pharmacokinetics of adriamycin and antigliolna monoclonal antibodySZ-39 immunoconjugate in nude mice bearing human tumors

采用ＤｅｘｔｒａｎＴ－４０桥联法将抗人脑胶质瘤单克隆抗体ＳＺ－３９与肿瘤化疗药物氚标记阿霉素交联，制各成免疫交职物３Ｈ－Ａｄｒ（阿霉素）－ＰＡＤ（多醛葡聚糖）－ＭＡｂ（单克隆抗体）ＳＺ－３９．在荷瘤鼠体内研究免疫交联物药代动力学特征。结果显示Ａｄｒ－ＭＡｂＳＺ－３９在相关肿瘤内浓聚，发挥了单抗高选择性作用，为胶质瘤的治疗提供了高效低毒的新一代良药。但在肝内摄入较多，为其可能的副作用。血药浓度－时间曲线符合三室线性模型，Ｔ＿（１／２）长于游离Ａｄｒ，有效分布体积大于游离Ａｄｒ，以２周问隔多疗程治疗为佳。

?H-Adr-MAb SZ- 39 immunoconjugate was prepared by linking a murine anti-hu-man glioma monoclonal antibody,SZ-39,to an antitumor agent,￣3H-adriamycin,via a dextran T-40bridge, Its pharmacokinetics was studied in tumor-bearing nude mice. The results demonstratedthat the immunoconjugate localizes in relative tumor,and is high selective. But its high uptake inliver may be the main side-effect.Its pharmacokinetics fits three compartments model,and thera-py with several intervals of two weeks is favourable.