Centre de Recherches en Cancérologie de Toulouse (CRCT), UMR1037 INSERM, Université Toulouse III: Paul-Sabatier, ERL5294 CNRS, Université de Toulouse, Toulouse, France.
Hématologie Clinique, Hôpital Le Bocage-CHU Dijon, 14 rue Paul Gaffarel, 21079, Dijon Cedex, France.
Target Oncol. 2018 Jun;13(3):287-308. doi: 10.1007/s11523-018-0558-1.
Antibody-drug conjugates (ADCs) are an emerging class of therapeutic agents that bring new opportunities for the treatment of hematological malignancies by meeting unmet medical needs. These drugs consist of a cytotoxic agent connected by a linker to a human, humanized, or chimeric antibody targeting a surface antigen specifically expressed by tumor cells. These ADCs are being developed to specifically deliver the cytotoxic agent into tumor cells. The cytotoxic payload is released from the ADC after internalization and cleavage of the linker, ultimately triggering the death of the cancer cell. Second- and even third-generation ADCs are currently being developed and have more stable linkers and more potent payloads, which should improve ADC efficacy even further. In this review, we analyze the results for the main ADCs currently developed and discuss the advantages and drawbacks of this therapeutic option.
抗体药物偶联物 (ADC) 是一类新兴的治疗药物,通过满足未满足的医疗需求为治疗血液系统恶性肿瘤带来了新的机会。这些药物由通过连接子连接的细胞毒性药物和靶向肿瘤细胞特异性表达的表面抗原的人源化、人源或嵌合抗体组成。这些 ADC 被开发用于将细胞毒性药物特异性递送至肿瘤细胞。细胞毒性有效载荷在连接子内化和切割后从 ADC 中释放,最终触发癌细胞死亡。目前正在开发第二代甚至第三代 ADC,它们具有更稳定的连接子和更有效的有效载荷,这应该会进一步提高 ADC 的疗效。在这篇综述中,我们分析了目前开发的主要 ADC 的结果,并讨论了这种治疗选择的优缺点。
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