Fenn K M, Kalinsky K
Department of Medicine, Columbia University Irving Medical Center, New York, New York, USA.
Drugs Today (Barc). 2019 Sep;55(9):575-585. doi: 10.1358/dot.2019.55.9.3039669.
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.
一线治疗后病情进展的转移性三阴性乳腺癌（mTNBC）患者预后较差，治疗选择有限。戈沙妥珠单抗（SG）是一种新型抗体药物偶联物（ADC），在mTNBC中显示出有前景的疗效。SG由伊立替康的活性代谢产物SN-38组成，通过可水解连接子与靶向滋养层细胞表面抗原2（Trop-2）的人源化RS7抗体偶联，Trop-2是一种在许多上皮性实体瘤中高表达的糖蛋白。它已获得美国食品药品监督管理局（FDA）的突破性疗法认定，用于治疗经治的mTNBC患者。在本综述中，我们总结了关于SG的药理学、药代动力学、安全性和疗效的现有数据，并描述了正在进行的以及未来研究该药物的临床研究。
