靶向Trop-2的抗体偶联药物:戈沙妥珠单抗

Trop-2-targeted antibody-drug conjugate:sacituzumab govitecan

戈沙妥珠单抗是全球首款由抗人滋养层细胞表面抗原2(Trop-2)h RS7 IgG1κ抗体与拓扑异构酶Ⅰ抑制剂SN-38(伊立替康的活性代谢物)通过专有的可水解连接子偶联而成的抗体偶联药物。其于2020年和2021年分别获美国食品和药物管理局批准用于三阴性乳腺癌和尿路上皮癌患者的治疗,并于2022年6月获我国药品监督管理局批准,用于既往至少接受过两种系统治疗(其中至少一种治疗针对转移性疾病)的不可切除的局部晚期或转移性三阴性乳腺癌成人患者。临床研究表明,戈沙妥珠单抗在多种上皮癌患者中均具有较好的抗癌疗效,且安全性良好。

Sacituzumab govitecan(SG)is the world's first antibody-drug conjugate composed of an antitrophoblast cell-surface antigen 2(Trop-2)hRS7 IgGlk antibody coupled to topoisomerase Iinhibitor SN-38(the active metabolite of irinotecan),through a proprietary hydrolyzable linker.SG was approved by the U.S.Food and Drug Administration in the treatment of triple negative breast cancer and urothelial cancer patients in 2020 and 2021.And it was also approved by the National Medical Product Administration for treating unresectable locally advanced or metastatic triple negative breast cancer adult patients who have received two or more kinds of systemic therapies(at least one of which for metastatic disease)in June,2022.Clinical studies have shown that SG has good anticancer efficacy and safety in a variety of epithelial cancer patients.