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|Therapy Name||DS-3201b + Trastuzumab deruxtecan|
|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|DS-3201b||DS-3201|Valemetostat Tosylate||EZH1 inhibitor 5 EZH2 inhibitor 19||DS-3201b inhibits EZH1 and EZH2, resulting in decreased H3K27 trimethylation and potentially leading to decreased tumor growth (Blood 2017 130:2073, PMID: 30658046).|
|Trastuzumab deruxtecan||Enhertu||DS-8201|DS8201a|T-DXd|DS-8201|fam-trastuzumab deruxtecan-nxki|DS-8201a||HER2 (ERBB2) Antibody 64 HER2 (ERBB2) Antibody-Drug Conjugate 24||Enhertu (trastuzumab deruxtecan) is an antibody-drug conjugate (ADC) comprising an anti-ERBB2 (HER2) antibody linked to a derivative of the topoisomerase inhibitor DX-8951, which delivers the cytotoxic agent to ERBB2 (HER2)-expressing tumor cells, potentially resulting in decreased growth of tumors, including tumors with low ERBB2 (HER2) expression (PMID: 27026201). Enhertu (fam-trastuzumab deruxtecan-nxki) is FDA approved for use in patients with ERBB2 (HER2)-positive breast cancer who have received two or more anti-HER2 therapies previously, in patients with ERBB2 (HER2)-low (IHC 1+ or IHC 2+/ISH -) breast cancer received prior chemotherapy, in patients with locally advanced or metastatic HER2-positive gastric or gastroesophageal (GEJ) adenocarcinoma who have received prior trastuzumab-based therapy, and in patients with non-small cell lung cancer harboring ERBB2 (HER2) activating mutations who have received prior systemic therapy (FDA.gov).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|
|NCT05633979||Phase I||DS-3201b DS-3201b + Trastuzumab deruxtecan||Phase 1b Study of EZH1/2 Inhibitor Valemetostat in Combination With Trastuzumab Deruxtecan in Subjects With HER2 Low/Ultra-low/Null Metastatic Breast Cancer||Recruiting||USA||0|