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Sacituzumab govitecan:一种新型抗体药物偶联物的过去、现在和未来及未来展望。

Sacituzumab govitecan: past, present and future of a new antibody-drug conjugate and future horizon.

机构信息

German Breast Group, Neu-Isenburg, 63263, Germany.

Medical Faculty Mannheim, Heidelberg University, Universitätsfrauenklinik, Mannheim, 68167, Germany.

出版信息

Future Oncol. 2022 Sep;18(28):3199-3215. doi: 10.2217/fon-2022-0407. Epub 2022 Sep 7.

Abstract

Sacituzumab govitecan (SG) is a new antibody-drug conjugate directed against the cell-surface antigen Trop-2. Characteristics of the linker connecting the payload SN-38 to the antibody allows SG to kill tumor cells expressing Trop-2 and also the adjacent tumor cells (bystander effect). SG showed efficacy and safety in several epithelial tumors. The phase III ASCENT trial led to the approval of SG (10 mg/kg, d1,8 q3w) in patients with advanced or metastatic triple-negative breast cancer (TNBC) who have received ≥2 prior systemic therapies, including ≥1 for metastatic disease. The phase III TROPiCS-02 trial in heavily pretreated advanced hormone receptor (HR)-positive breast cancer has recently shown an improvement in progression-free survival for patients treated with SG compared to single-agent chemotherapy. The phase III post-neoadjuvant SASCIA study in early high-risk TNBC and HR-positive breast cancer is currently recruiting patients.

摘要

沙库巴曲缬沙坦(Sacituzumab govitecan,SG)是一种新型抗体药物偶联物,针对细胞表面抗原 Trop-2。连接有效载荷 SN-38 与抗体的连接子的特性允许 SG 杀死表达 Trop-2 的肿瘤细胞和相邻的肿瘤细胞(旁观者效应)。SG 在几种上皮肿瘤中显示出疗效和安全性。III 期 ASCENT 试验导致 SG(10mg/kg,d1,8 q3w)在接受过≥2 种系统治疗(包括≥1 种转移性疾病治疗)的晚期或转移性三阴性乳腺癌(TNBC)患者中的批准。在预处理的晚期激素受体(HR)阳性乳腺癌中进行的 III 期 TROPiCS-02 试验最近表明,与单药化疗相比,SG 治疗的患者无进展生存期得到改善。目前正在招募患者的 III 期新辅助后 SASCIA 研究在早期高危 TNBC 和 HR 阳性乳腺癌中进行。

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