ADC composed of the HER2-targeting monoclonal antibody (mAb) trastuzumab, atopoisomeraseI inhibitor conjugate deruxtecan, and a novel GGFG quadripeptide-based cleavable moiety. Recently, the FDA has approved trastuzumab deruxtecan for the treatment of unresectable or metastatic HER2+ breast cancer...
a HER2 antibody-drug conjugate, in patients with HER2-mutant NSCLC have not been examined extensively. In an international, multi-center, phase-II clinical trial, trastuzumab deruxtecan (6.4 mg/
Trastuzumab deruxtecan (T-DXd) in patients withHER2-mutant metastatic non–small cell lung cancer (mNSCLC): Final analysis results of DESTINY-Lung02.doi:10.1200/JCO.2024.42.16_suppl.854338543#Background:In the DESTINY-Lung02 primary analysis (data cutoff, Dec 23, 2022), T-DXd 5.4 mg/kg ...
4.Nakada, T., et al., Nakada, T., et al.,The latest research and development into the antibody–drug conjugate,[fam-] trastuzumab deruxtecan (DS-8201a), for HER2 cancer therapy.Chemical and Pharmaceutical Bulletin, 2019.67(3): p. 173-185. 5.Staudacher, A.H. and M.P. Brown, Stau...
In summary, published data suggest that, despite their large molecular size, ADCs may achieve relevant clinical activity in brain metastases, potentially due to a partially disrupted BBB at the metastatic site. Trastuzumab deruxtecan was shown to harbor substantial extracranial activity in heavily pretr...
DESTINY-CRC01 (NCT03384940) was a multicenter, open-label, phase 2 trial assessing the efficacy and safety of trastuzumab deruxtecan (T-DXd) in patients with HER2-expressing metastatic colorectal cancer (mCRC) that progressed after ≥2 prior regimens; results of the primary analysis are publishe...
4. Nakada, T., et al., The latest research and development into the antibody–drug conjugate,[fam-] trastuzumab deruxtecan (DS-8201a), for HER2 cancer therapy. Chemical and Pharmaceutical Bulletin, 2019.67(3): p. 173-185. 5. Staudacher, A.H. and M.P. Brown, Antibody drug conjugates...
Deruxtecan is much more potent topoisomerase I inhibitor than SN-38. The bystander effect for T-DXd is felt to be fundamental to its efficacy in the low HER2 protein expression environment, however for SG given the high level of Trop-2 expression the importance of the bystander effect is ...
DS-8201(又称Enhertu®、T-DXd、德曲妥珠单抗、Trastuzumab deruxtecan)是一种靶向人表皮生长因子2(HER2)的新型抗体药物偶联物(ADC),由新型有效的喜树碱类似物拓扑异构酶I抑制剂(DXd)、新开发的酶切割连接子、人源化的抗HER2抗体三部分组成,可同时杀伤目标肿瘤细胞及邻近肿瘤细胞。
Summary Trastuzumab deruxtecan is an antibody used to treat certain types of unresectable or metastatic HER2 positive breast cancer. Brand Names Enhertu Generic Name Trastuzumab deruxtecan DrugBank Accession Number DB14962 Background Trastuzumab deruxtecan is a HER2-directed antibody attached to a to...