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Trop-2 蛋白作为治疗靶点:基于 Trop-2 的抗体药物偶联物及其预测性生物标志物的综述。

Trop-2 protein as a therapeutic target: A focused review on Trop-2-based antibody-drug conjugates and their predictive biomarkers.

机构信息

College of Medicine, QU Health, Qatar University, Doha, Qatar; Biomedical and Pharmaceutical Research Unit, QU Health, Qatar University, Doha, Qatar.

Department of Pathology, University of Oklahoma College of Medicine, Oklahoma City, Oklahoma, United States.

出版信息

Bosn J Basic Med Sci. 2022 Feb 1;22(1):14-21. doi: 10.17305/bjbms.2021.6100.

Abstract

Antibody-drug conjugates (ADCs) represent a new class of highly potent antineoplastic drugs built by attaching a small molecule of an anticancer drug (payload) or another therapeutic agent to an antibody recognizing an epitope on the targeted cells. Trophoblast cell-surface antigen-2 (Trop-2) was originally described in trophoblasts and fetal tissues, but subsequently, its overexpression has been demonstrated in various solid malignancies. Sacituzumab govitecan, a conjugate of anti-Trop-2 antibody and SN-38 payload (an active metabolite of irinotecan), is the first in the class that has been clinically validated and approved by the Food and Drug Administration for the treatment of metastatic triple-negative breast (2020) and urothelial carcinomas (2021). In the current review, we summarize and critically appraise the most recent advances with Sacituzumab govitecan, emphasizing the predictive biomarker analysis.

摘要

抗体药物偶联物 (ADC) 代表了一类新型的高效抗肿瘤药物,它们是通过将小分子抗癌药物(有效载荷)或其他治疗剂连接到识别靶细胞上表位的抗体上而构建的。滋养细胞表面抗原-2(Trop-2)最初在滋养细胞和胎儿组织中被描述,但随后在各种实体恶性肿瘤中证明了其过度表达。Sacituzumab govitecan 是一种抗 Trop-2 抗体和 SN-38 有效载荷(伊立替康的活性代谢物)的偶联物,是该类别中第一个经临床验证并获得美国食品和药物管理局批准用于治疗转移性三阴性乳腺癌(2020 年)和尿路上皮癌(2021 年)的药物。在当前的综述中,我们总结并批判性地评价了 Sacituzumab govitecan 的最新进展,强调了预测性生物标志物分析。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4724/8860310/078388744585/BJBMS-22-14-g001.jpg

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