Heidelberg University Hospital, Department of Nuclear Medicine, INF 400, 69120 Heidelberg, Germany.
Heidelberg University, Institute of Pharmacy and Molecular Biotechnology, INF 364, 69120 Heidelberg, Germany.
Drug Discov Today. 2022 Oct;27(10):103311. doi: 10.1016/j.drudis.2022.06.011. Epub 2022 Jul 3.
Antibody-drug conjugates (ADCs) are on the brink of widespread use for the targeted treatment of cancer. ADCs manage the toxicity of drugs with unacceptable narrow therapeutic windows by guiding highly toxic compounds to the target cells, thereby sparing healthy cells. In this review, we describe approved ADCs and discuss their modes of action, together with medicinal chemical aspects, to evaluate the potential for improvement and to combat tumor-acquired resistance. A recent research focus has centered on the stimulation of immune responses to induce immunogenic cell death and the influence on the tumor microenvironment to enhance bystander effects.
抗体药物偶联物（ADCs）即将广泛用于癌症的靶向治疗。ADC 通过将高毒性化合物引导至靶细胞，从而使健康细胞免受损伤，以此控制具有不可接受的窄治疗窗口的药物的毒性。在这篇综述中，我们描述了已批准的 ADC，并讨论了它们的作用模式以及药物化学方面，以评估其改进潜力并对抗肿瘤获得性耐药性。最近的研究重点集中在刺激免疫反应以诱导免疫原性细胞死亡以及影响肿瘤微环境以增强旁观者效应上。
