Sacituzumab govitecan:抗体-药物结合物在三阴性乳腺癌和其他实体肿瘤中的应用。

K. Fenn, K. Kalinsky
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引用次数: 29

摘要

经一线治疗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。Sacituzumab govitecan (SG)是一种新型抗体-药物偶联物(ADC),在mTNBC中显示出有希望的疗效。SG由伊立替康的活性代谢物SN-38组成,通过可水解的连接物偶联到靶向滋养细胞表面抗原2 (Trop-2)的人源化RS7抗体,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,用于治疗预先治疗的mTNBC患者。在这篇综述中,我们总结了关于SG的药理学、药代动力学、安全性和有效性的现有数据,并描述了正在进行的和未来的临床研究。
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Sacituzumab govitecan: antibody-drug conjugate in triple-negative breast cancer and other solid tumors.
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.
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