Rowlinson-Busza G, Epenetos A A
Department of Clinical Oncology, Royal Postgraduate Medical School, Hammersmith Hospital, London, UK.
Curr Opin Oncol. 1992 Dec;4(6):1142-8. doi: 10.1097/00001622-199212000-00020.
This review summarizes several strategies under investigation for targeted delivery of antineoplastic agents to tumor cells, which avoids normal tissue damage. Monoclonal antibodies remain the molecules of choice for targeted therapy, and several improvements to immunotargeting are discussed. These improvements include the use of novel radioisotopes, cytokines, new linkers for chemotherapeutic drugs, more potent drugs, and improved immunotoxins. Bifunctional antibodies, in which one antigen-binding site recognizes a tumor-associated antigen and the other an antineoplastic agent, have been investigated for radioimmunotherapy and for the activation of cytotoxic cells for targeted immunotherapy. The activation of relatively nontoxic prodrugs by antibody-enzyme conjugates is increasingly being investigated in an effort to reduce the systemic toxicity associated with conventional chemotherapy. Finally, the use of liposomes as carriers of drugs or as activators of macrophages is described.
本综述总结了正在研究的几种将抗肿瘤药物靶向递送至肿瘤细胞的策略,这些策略可避免对正常组织造成损伤。单克隆抗体仍是靶向治疗的首选分子,并讨论了免疫靶向的一些改进措施。这些改进包括使用新型放射性同位素、细胞因子、化疗药物的新连接体、更强效的药物以及改良的免疫毒素。双功能抗体,其中一个抗原结合位点识别肿瘤相关抗原,另一个识别抗肿瘤药物,已被研究用于放射免疫治疗和激活细胞毒性细胞以进行靶向免疫治疗。为了降低与传统化疗相关的全身毒性,人们越来越多地研究抗体 - 酶偶联物对相对无毒前药的激活作用。最后,描述了使用脂质体作为药物载体或巨噬细胞激活剂的情况。