抗体偶联药物的有关进展

The Coupling Methods of Antibody-Immunoconjugated Drugs

化疗肿瘤治疗的常规手段之一,但由于细胞毒药物没有明显的靶向性,导致其副作用十分显著。因此免疫偶联药物由于其良好的靶向性及抗癌活性就成为了研究的热点。文章综述了细胞毒药物与单克隆抗体偶联的各种常用方法,包括使用偶联剂进行偶联、利用肽链进行偶联、利用二硫键进行偶联和利用大分子技术进行偶联,以及抗体偶联药物的研究现状。抗体偶联药物有细胞毒药物、抗体和偶联剂组成,利用各种偶联手段将单克隆抗体与细胞毒药物偶联,不仅可以将细胞毒药物特异性地靶向于肿瘤细胞,而且可以降低细胞毒药物对于正常细胞的杀伤,同时还可以具备缓释、提高药物抗肿瘤活性等效果,是未来肿瘤靶向治疗的发展方向之一。同时文章还结合作者的自身工作,对抗体偶联药物的未来发展方向提出了建议。

Traditional chemotherapy has become one of essential treatments of cancer. However, cymtoxic agents are not tumor specific, which would cause serious side effects. Antibody- Immunoconjugated drugs, also called immunoconjugates, belong to the ＂targeted chemotherapeutics＂ category of anti - cancer drugs. Immunoconjugates are composed of three components： including the cytotoxic drug, the monoclonal antibody, and the linker connecting the drug to the antibody. With the special - binding between antibody and antigen expressed on the surface of targeted cancer cells, immunoconjugates provide a method to achieve the excellent localization of drug at the desired Site in the body. This review summarizes the coupling methods of immunoconjugates including the coupling reagents, disulfide linkage, and macromolecular linkage, and the advances of immunoconjugates. In the mean time, it also put forward some advices about the future of immunoconjugates.