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| Therapy Name | I-BET151 |
| Synonyms | |
| Therapy Description |
I-BET151 is a small molecule that blocks Brd3/4 binding to chromatin, resulting in transcription inhibition and potentially leading to tumor cell death (PMID: 21964340, PMID: 30906568, PMID: 32603665). |
| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| I-BET151 | GSK1210151A | BRD3 Inhibitor 2 BRD4 Inhibitor 11 | I-BET151 is a small molecule that blocks Brd3/4 binding to chromatin, resulting in transcription inhibition and potentially leading to tumor cell death (PMID: 21964340, PMID: 30906568, PMID: 32603665). |
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| DNMT3A R882H NRAS G12D | acute myeloid leukemia | sensitive | I-BET151 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, an acute myeloid leukemia cell line harboring DNMT3A R882H and NRAS G12D mutations demonstrated reduced proliferation and downregulation of a DNMT3A R882H associated gene expression profile upon I-BET151 treatment in culture, and I-BET151 treatment delayed the onset of leukemia symptoms and improved survival in xenograft mouse models derived from these cells (PMID: 31164355). | 31164355 |
| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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