Sacituzumab govitecan: antibody-drug conjugate in triple-negative breast cancer and other solid tumors.
Sacituzumab govitecan: antibody-drug conjugate in triple-negative breast cancer and other solid tumors.
复制标题
DOI：
10.1358/dot.2019.55.9.3039669
复制
发表时间：
2019-09
期刊：
影响因子：
1.8
通讯作者：
Kathleen M. Fenn;Kevin Kalinsky
中科院分区：
文献类型：
--
作者：
Kathleen M. Fenn;Kevin Kalinsky
一线治疗后进展的转移性三阴性乳腺癌 (mTNBC) 患者预后不良，治疗选择有限。 Sacituzumab govitecan (SG) 是一种新型抗体药物偶联物 (ADC)，在 mTNBC 中显示出良好的疗效。 SG 由伊立替康的活性代谢物 SN-38 组成，通过可水解接头与靶向滋养层细胞表面抗原 2 (Trop-2) 的人源化 RS7 抗体缀合，Trop-2 是一种在许多上皮实体瘤中高水平表达的糖蛋白。它已获得美国食品和药物管理局 (FDA) 的突破性治疗地位，用于治疗已接受过治疗的 mTNBC 患者。在这篇综述中，我们总结了有关 SG 的药理学、药代动力学、安全性和有效性的现有数据，并描述了正在进行和未来调查该药物的临床研究。
Patients with metastatic triple-negative breast cancer (mTNBC) that has progressed on first-line therapy have a poor prognosis with limited therapeutic options. Sacituzumab govitecan (SG) is a novel antibody-drug conjugate (ADC) that has shown promising efficacy in mTNBC. SG is comprised of SN-38, the active metabolite of irinotecan, conjugated via a hydrolyzable linker to the humanized RS7 antibody targeting trophoblast cell surface antigen 2 (Trop-2), a glycoprotein that is expressed at high levels in many epithelial solid tumors. It has received breakthrough therapy status by the U.S. Food and Drug Administration (FDA) for the treatment of patients with pretreated mTNBC. In this review, we summarize available data regarding the pharmacology, pharmacokinetics, safety and efficacy of SG and describe ongoing and future clinical studies investigating this agent.