Therapy Detail
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| Therapy Name | DS-3201b + Trastuzumab deruxtecan |
| Synonyms | |
| Therapy Description | |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| DS-3201b | DS-3201|Valemetostat Tosylate | EZH1 inhibitor 5 EZH2 inhibitor 20 | 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 72 HER2 (ERBB2) Antibody-Drug Conjugate 27 | 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). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT06244485 | Phase I | DS-3201b + Trastuzumab deruxtecan Datopotamab deruxtecan + DS-3201b | A Study of Valemetostat in Combination With DXd ADCs in Subjects With Solid Tumors | Recruiting | USA | 0 |
| 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 |
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