Antibody-drug conjugates-A new wave of cancer drugs
Antibody-drug conjugates-A new wave of cancer drugs
复制标题
DOI：
10.1016/j.bmcl.2014.10.021
复制
发表时间：
2014-12-01
影响因子：
2.7
通讯作者：
Garcia-Echeverria, Carlos
中科院分区：
文献类型：
--
作者：
Bouchard, Herve;Viskov, Christian;Garcia-Echeverria, Carlos
抗体-药物偶联物（adc）由细胞毒性药物与单克隆抗体共价连接而成，这些单克隆抗体针对肿瘤细胞中差异过表达的抗原。这些装载的抗体有望选择性地向肿瘤细胞递送致命的货物，并为预先选择的癌症患者提供持续的临床益处，同时最大限度地减少全身毒性。尽管不能完全避免靶上不良事件，这些创新药物的真正功效仍需要进一步澄清，但在临床环境中，含有calicheamicin、auristatin或基于美坦辛的细胞毒性有效载荷的免疫偶联物已经获得了概念验证。在这篇文章中，我们回顾了前面的细胞毒性平台的特点和它们的化学偶联方法。(C) 2014年Elsevier Ltd.出版这是一篇基于CC BY-NC-ND许可的开放获取文章
Antibody-drug conjugates (ADCs) consist of cytotoxic drugs covalently linked to monoclonal antibodies directed to antigens differentially overexpressed in tumor cells. These loaded antibodies are expected to selectively deliver lethal cargoes to tumor cells and provide sustained clinical benefit to pre-selected cancer patients while, at the same time, minimizing systemic toxicity. Although on-target adverse events are not completely avoided and the true efficacy of these innovative agents still requires further clarification, proof-of-concept has already been achieved in clinical settings with immunoconjugates containing calicheamicin, auristatin or maytansine-based cytotoxic payloads. In this present article we review the characteristics of the preceding cytotoxic platforms and their chemical conjugation approaches. (C) 2014 Published by Elsevier Ltd. This is an open access article under the CC BY-NC-ND license