而Trastuzumab Deruxtecan(T-DXd 和DS-8201)是一种新型抗体药物偶联物(antibody-drug conjugate,ADC),是HER2靶向抗体和DNA拓扑异构酶Ⅰ抑制剂德卢替康(deruxtecan,DXd)的结合物。它设计独特,药物与抗体的比例高达大约8:1,并保持稳定,从而提供了强大的细胞毒性载荷,被癌细胞中过度表达的溶酶体内化并选择性地裂——...
Trastuzumab emtansine是一种抗体偶联药物 (ADC),是HER2 靶向药物曲妥珠单抗以及微管抑制剂 DM1 的结合药物,目前是HER2阳性,先前接受过曲妥珠单抗联合紫杉醇治疗后出现疾病进展的乳腺癌患者的一线治疗手段。Trastuzumab deruxtecan(T-DXd)是一种新...
randomized trial to compare the efficacy and safety of trastuzumab deruxtecan(a HER2 antibody-drug conjugate)with those of trastuzumab emtansine in patients with HER2-positive metastatic breast cancer previously treated with trastuzumab and a taxane.The primary end point was progression-free survival(as...
Trastuzumab deruxtecan (T-DXd) demonstrated significantly improved efficacy over trastuzumab emtansine (T-DM1) in DESTINY-Breast03 (median follow-up, 28 months). We report updated efficacy and safety analyses, including secondary and exploratory efficacy
针对T-DM1 (Emtansine)不敏感/耐受的肿瘤使用DS-8201a(DXd)可以展示良好的抗肿瘤活性,其原因可能一部分归因于能否裂解的Linker,一部分归因于Payload抑制活性的高低。 随着“万物皆可偶联”概念的兴起,与Tz偶联的Payload不再局限于细胞毒性药物开始扩展到放射性核素[13]、荧光染料[14]、Toll样受体激动剂[15]等,随之...
Trastuzumab deruxtecan versus trastuzumab emtansine in patients with HER2-positive metastatic breast cancer: updated results from DESTINY-Breast03, a randomised, open-label, phase 3 trial. PMID: 36495879Trastuzumab Deruxtecan: First Approval. PMID: 32144719...
此外,还有ADC药物trastuzumab emtansine(T-DM1)和HER2激酶抑制剂lapatinib,用于进一步的治疗。HER2的过度表达和突变同样也是非小细胞肺癌(NSCLC)和结直肠癌的致病因素,然而,迄今为止,在这些适应症还没有批准的HER2靶向治疗。 Trastuzumab deruxtecan(T-DXd)(DS-8201;ENHERTU®) 是由第一三共和阿斯利康合作开发的...
此外,还有ADC药物trastuzumab emtansine(T-DM1)和HER2激酶抑制剂lapatinib,用于进一步的治疗。HER2的过度表达和突变同样也是非小细胞肺癌(NSCLC)和结直肠癌的致病因素,然而,迄今为止,在这些适应症还没有批准的HER2靶向治疗。 Trastuzumab deruxtecan(T-DXd)(DS-8201;ENHERTU?) 是由第一三共和阿斯利康合作开发的新型...
When we compared JIMT-1 and L-JIMT-1 sensitivity to three HER2-targeting antibody-drug conjugates (ADCs) trastuzumab emtansine (T-DM1), trastuzumab deruxtecan (T-DXd), and disitamab vedotin (DV) in vitro, JIMT-1 cells were resistant T-DXd, partially sensitive to T-DM1, and sensitive ...
Abstract OT1-02-03: Trastuzumab deruxtecan (T-DXd; DS-8201) vs trastuzumab emtansine (T-DM1) in high-risk patients with HER2-positive, residual invasive early breast cancer after neoadjuvant therapy: A randomized, phase 3 trial (DESTINY-... Trastuzumab deruxtecan (T-DXd; DS-8201) vs ...