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Sacituzumab govitecan: antibody-drug conjugate in triple-negative breast cancer and other solid tumors

机译:Sacituzumab Govitecan:三阴性乳腺癌和其他实体瘤中的抗体 - 药物缀合物

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摘要

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.
机译:在一线治疗中进行的转移性三阴性乳腺癌(MTNBC)的患者具有有限的治疗选择预后差。 Sacituzumab Govitecan(SG)是一种在MTNBC中显示出有希望的疗效的新型抗体 - 药物缀合物(ADC)。 SG由Sn-38组成,通过可水解连接器与人源化的RS7抗体缀合的氨基丙二烷的活性代谢物组成,靶向滋养细胞表面抗原2(TOP-2),糖蛋白在许多上皮固体瘤中以高水平表达。 它已获得美国食品和药物管理局(FDA)的突破治疗状况,用于治疗预处理MTNBC患者。 在本文中,我们总结了SG的药理学,药代动力学,安全性和功效的可用数据,并描述了调查该试剂的持续和未来的临床研究。

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