Hermentin P, Seiler F R
Research Laboratories of Behringwerke AG, Marburg, W. Germany.
Behring Inst Mitt. 1988 Apr(82):197-215.
The development of monoclonal antibody-drug (anthracycline) conjugates (immunocytostatics) that has emerged during the last decade is briefly reviewed. Stress is layed on the various procedures that have been employed for the chemical attachment of daunorubicin (daunomycin) and doxorubicin (adriamycin) to spacers, high-molecular weight carrier molecules, and immunoglobulins. Anthracycline conjugates that have proved effective in mice with respect to the treatment of cancer are especially evaluated. Also a new method developed for the conjugation of rhodosaminyl anthracyclinones via a hydrolysable spacer, developed in our laboratories, is briefly communicated. Finally, import aspects for further developments of monoclonal antibody-drug conjugates are discussed.
本文简要回顾了过去十年中出现的单克隆抗体-药物（蒽环类）偶联物（免疫细胞抑制剂）的发展情况。重点介绍了将柔红霉素（柔毛霉素）和多柔比星（阿霉素）化学连接到间隔物、高分子量载体分子和免疫球蛋白上所采用的各种方法。特别评估了在小鼠癌症治疗中已证明有效的蒽环类偶联物。此外，还简要介绍了我们实验室开发的一种通过可水解间隔物将玫瑰胺基蒽环酮偶联的新方法。最后，讨论了单克隆抗体-药物偶联物进一步发展的重要方面。
