Advances in antibody-drug conjugates: A new era of targeted cancer therapy

作者：Sau Samaresh; Alsaab Hashem O; Kashaw Sushi Kumar; Tatiparti Katyayani; lyer Arun K^*

来源：Drug Discovery Today, 2017, 22(10): 1547-1556.

DOI：10.1016/j.drudis.2017.05.011

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 (R), and Adcetrise (R) 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 (R). 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.

• 出版日期2017-10