C:科伦博泰/默沙东SKB264(首发适应症中国Ⅲ期,TNBC, EGFR突变NSCLC中国Ⅲ期,HER2-HR+ BC 中国Ⅲ期) Payload(有效载荷):拓扑异构酶I抑制剂在Trodelvy、DS-1062、和SKB-264中用作有效载荷,诱导DNA损伤并最终导致细胞凋亡。Trodelvy的有效载荷为伊立替康的活性代谢物SN-38。DS-1062有效载荷是Exatecan衍生物(DXd)。
进一步往深了想,DS-1062挑战IMMU-132本来胜算就相当大,后者著名的11h半衰期实在是不够稳定、导致高比例的血液毒性很明显限制了治疗窗(诚然它搭配上一个nmol级的弱毒性payload也不失为一种策略、最终也成药了),而前者以低亲和力抗体(好像也是nmol级)+ DS起家的linker和Dxd payload +DAR降回到4,在TROP2 ADC的成药...
作用:将抗体部分与细胞毒性药物部分连接起来,保证ADC在血液循环中稳定,并在肿瘤细胞内适时释放药物。 细胞毒性药物(Payload) 化学名称:Deruxtecan(一种拓扑异构酶I抑制剂)。 作用机制:在释放后,Deruxtecan通过抑制拓扑异构酶I,阻断DNA复制和转录,导致肿瘤细胞凋亡或死亡。 特点:Deruxtecan具有高效的抗肿瘤活性,能够在...
DS-1062, a TROP2 directed ADC, is one of three lead DXd ADCs in the oncology pipeline ofDaiichi Sankyo. ADCs are targeted cancer medicines that deliver cytotoxic chemotherapy (“payload”) to cancer cells via a linker attached to a monoclonal antibody that binds to a specific targ...
The amount of DXd payload released from TROP2-high tumor cells after the in vitro treatment with DS-1062a was higher than that of TROP2-low tumor cells. DNA damage and apoptosis were induced in TROP2-high tumor cells after the in vitro treatment with DXd and DS-1062a, but not with ...
细胞毒性药物(Payload) 化学名称:Deruxtecan(一种拓扑异构酶I抑制剂)。 作用机制:在释放后,Deruxtecan通过抑制拓扑异构酶I,阻断DNA复制和转录,导致肿瘤细胞凋亡或死亡。 特点:Deruxtecan具有高效的抗肿瘤活性,能够在低剂量下发挥显著的细胞毒性作用,提升ADC的整体治疗效果。
DS-1062, a TROP2 directed ADC, is one of three lead DXd ADCs in the oncology pipeline of Daiichi Sankyo. ADCs are targeted cancer medicines that deliver cytotoxic chemotherapy (payload) to cancer cells via a linker attached to a monoclonal antibody that binds to a specific target expressed on...
DS-1062 and patritumab deruxtecan (U3-1402) are two of three lead DXd ADCs in the oncology pipeline of Daiichi Sankyo. ADCs are targeted cancer medicines that deliver cytotoxic chemotherapy (payload) to cancer cells via a linker attached to a monoclonal antibody that binds to a specific targe...
DS-1062 and patritumab deruxtecan (U3-1402) are two of three lead DXd ADCs in the oncology pipeline of Daiichi Sankyo. ADCs are targeted cancer medicines that deliver cytotoxic chemotherapy (“payload”) to cancer cells via a linker attached to a monoclonal antibody that binds to a specific...