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抗体药物偶联物在癌症治疗中的应用。

Antibody Drug Conjugates for Cancer Therapy.

机构信息

Department of Molecular Oncology, Genentech, South San Francisco, California

出版信息

Pharmacol Rev. 2016 Jan;68(1):3-19. doi: 10.1124/pr.114.009373.

Abstract

Antibody drug conjugates (ADCs) constitute a family of cancer therapeutics designed to preferentially direct a cytotoxic drug to cells expressing a cell-surface antigen recognized by an antibody. The antibody and drug are linked through chemistries that enable release of the cytotoxic drug or drug adduct upon internalization and digestion of the ADC by the cell. Over 40 distinct ADCs, targeting an array of antigens and utilizing a variety of drugs and linkers, are undergoing clinical evaluation. This review primarily covers ADCs that have advanced to clinical investigation with a particular emphasis on how the individual targets, linker chemistries, and appended drugs influence their behavior.

摘要

抗体药物偶联物 (ADC) 是一类癌症治疗药物,旨在将细胞毒性药物优先靶向表达细胞表面抗原的细胞,该抗原由抗体识别。抗体和药物通过化学连接,使 ADC 被细胞内化和消化后,能够释放出细胞毒性药物或药物加合物。目前正在进行临床评估的有 40 多种不同的 ADC,针对一系列抗原,并利用各种药物和连接子。本篇综述主要涵盖了已进入临床研究的 ADC,并特别强调了各个靶点、连接子化学和附加药物如何影响它们的行为。

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