Huennekens F M
Department of Molecular and Experimental Medicine, Scripps Research Institute, La Jolla, CA 92037.
Trends Biotechnol. 1994 Jun;12(6):234-9. doi: 10.1016/0167-7799(94)90122-8.
Selective delivery of lethal levels of drugs to tumors, without concomitant damage to normal tissues, is a major challenge in cancer chemotherapy. Prodrugs used in conjunction with enzyme-monoclonal antibody conjugates that can target tumors and convert prodrugs to their active drug forms in situ, offer exceptional promise in achieving this objective. Synthesis of prodrugs, acquisition of appropriate enzymes and monoclonal antibodies, and manufacture of conjugates afford considerable flexibility in experimental design.
在不损害正常组织的情况下,将致死剂量的药物选择性地输送到肿瘤部位,是癌症化疗中的一项重大挑战。与酶-单克隆抗体偶联物联合使用的前药可以靶向肿瘤,并在原位将前药转化为其活性药物形式,为实现这一目标提供了巨大的前景。前药的合成、合适酶和单克隆抗体的获取以及偶联物的制造,在实验设计中提供了相当大的灵活性。