Department of Pharmacokinetics, Dynamics and Metabolism, Pfizer Inc, Pearl River, New York.
Ann N Y Acad Sci. 2014 Aug;1321:41-54. doi: 10.1111/nyas.12499.
Antibody-drug conjugates (ADCs) offer promise as a therapeutic modality that can potentially reduce the toxicities and poor therapeutic indices caused by the lack of specificity of conventional anticancer therapies. ADCs combine the potency of cytotoxic agents with the target selectivity of antibodies by chemically linking a cytotoxic payload to an antibody, potentially creating a synthetic molecule that will deliver targeted antitumor therapy that is both safe and efficacious. The ADC repertoire contains a range of payload molecules, antibodies, and linkers. Two ADC molecules, Kadcyla® and Adcetris®, have been approved by the FDA, and many more are currently in clinical development.
抗体偶联药物(ADCs)作为一种治疗方式具有很大的潜力,它可以减少传统抗癌疗法缺乏特异性而导致的毒性和治疗指数低的问题。ADCs 通过将细胞毒性有效载荷与抗体化学连接,将细胞毒性药物的效力与抗体的靶向选择性结合在一起,从而有可能创造出一种既能安全又能有效的靶向抗肿瘤治疗的合成分子。ADC 库包含一系列有效载荷分子、抗体和连接子。两种 ADC 药物 Kadcyla®和 Adcetris®已被 FDA 批准,目前还有更多的 ADC 药物正在临床开发中。