Department of Hematology, Medical University of Lodz and Copernicus Memorial Hospital, Ul. Ciolkowskiego 2, 93-510, Lodz, Poland.
Drug Saf. 2019 Feb;42(2):295-314. doi: 10.1007/s40264-018-0775-7.
Antibody-drug conjugates are monoclonal antibodies attached to biologically active drugs through chemical linkers that deliver and release cytotoxic agents at the tumor site, reducing the likelihood of systemic exposure and therefore toxicity. Currently, there are about 110 ongoing studies implementing antibody-drug conjugates in the treatment of multiple human malignancies. Antibody-drug conjugates carry a feature of the specificity of a monoclonal antibody and the anti-neoplastic potential of a cytotoxin. The first antibody-drug conjugate was approved in 2001, and the field of antibody-drug conjugates has expanded since then with three more antibody-drug conjugates being added to the market. The complex structure of the antibody-drug conjugate poses a challenge in designing a clinically adequate molecule. Antibody-drug conjugates are usually well tolerated with some predictable adverse reactions, as well as new medical issues, that need careful approach. This review provides an outline of the current status of the efficacy and safety of antibody-drug conjugates in malignant diseases.
抗体药物偶联物是通过化学连接子将单克隆抗体与生物活性药物连接起来的，在肿瘤部位输送并释放细胞毒性药物，降低了全身暴露的可能性，从而降低了毒性。目前，大约有 110 项正在进行的研究将抗体药物偶联物用于治疗多种人类恶性肿瘤。抗体药物偶联物具有单克隆抗体的特异性和细胞毒素的抗肿瘤潜力。第一个抗体药物偶联物于 2001 年获得批准，此后，抗体药物偶联物领域不断发展，又有 3 种抗体药物偶联物进入市场。抗体药物偶联物的复杂结构给临床充分分子的设计带来了挑战。抗体药物偶联物通常具有良好的耐受性，有一些可预测的不良反应，以及新的医疗问题，需要谨慎处理。本文综述了抗体药物偶联物在恶性疾病中的疗效和安全性的现状。
