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Advances in antibody-drug conjugates: A new era of targeted cancer therapy.
Drug Discovery Today ( IF 7.4 ) Pub Date : 2017-06-13 , DOI: 10.1016/j.drudis.2017.05.011
Samaresh Sau 1 , Hashem O Alsaab 2 , Sushil Kumar Kashaw 3 , Katyayani Tatiparti 1 , Arun K Iyer 4
Affiliation  

Antibody-drug conjugates (ADCs), a potent class of anticancer therapeutics, comprise a high-affinity antibody (Ab) and cytotoxic payload coupled via a suitable linker for selective tumor cell killing. In the initial phase of their development, two ADCs, Mylotarg®, and Adcetris® were approved by the US Food and Drug Administration (FDA) for treating hematological cancer, but the real breakthrough came with the discovery of the breast cancer-targeting ADC, Kadcyla®. With advances in bioengineering, linker chemistry, and potent cytotoxic payload, ADC technology has become a more powerful tool for targeted cancer therapy. In addition, ADCs with improved safety using humanized Abs with a unified 'drug:antibody ratio' (DAR) have been achieved. Concomitantly, there has been a significant increase in the number of clinical trials with anticancer ADCs with high translation potential.

中文翻译:

抗体-药物偶联物的进展:靶向癌症治疗的新时代。

抗体-药物偶联物(ADC)是一类有效的抗癌治疗药物,包含高亲和力抗体(Ab)和通过合适的接头偶联的细胞毒性有效载荷,以选择性杀伤肿瘤细胞。在开发的最初阶段,Mylotarg®和Adcetris®这两个ADC已获美国食品药品管理局(FDA)批准用于治疗血液学癌症,但真正的突破是针对乳腺癌的ADC的发现, Kadcyla®。随着生物工程,接头化学和有效的细胞毒性有效载荷的发展,ADC技术已成为靶向癌症治疗的更强大工具。此外,已经实现了使用具有统一“药物:抗体比率”(DAR)的人源化Abs改善了安全性的ADC。同时,
更新日期:2017-06-13
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