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|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|I-BET151||GSK1210151A||BRD3 Inhibitor 2 BRD4 Inhibitor 9||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|
|KMT2A - AFF1||acute lymphoblastic leukemia||sensitive||I-BET151||Preclinical - Pdx & cell culture||Actionable||In a preclinical study, treatment with I-BET151 in acute lymphoblastic leukemia cell lines harboring a KMT2A-AFF1 fusion resulted in growth inhibition, cell cycle arrest, increased apoptosis, and down-regulation of BRD4 targets CDK6, c-MYC, and BCL2 in culture, and resulted in reduced leukemic engraftment and decreased disease burden in a patient-derived xenograft (PDX) model and prolonged survival and reduced cellularity in a cell line xenograft model (PMID: 29748211).||29748211|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status||Covered Countries||Other Countries|