Combination of the novel BET inhibitor BI 894999 with CDK9 inhibition suggests a promising regimen for the treatment of AML

An abstract of the study of Tontsch-Grunt et al. about BET inhibitor BI 894999 with CDK9 inhibition suggests a promising regimen for the treatment of AML. Among other things bromodomain and extra-terminal (BET) protein inhibitors comprising the family members BRD2, 3, 4 and T are being extensively s...

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Bibliographic Details
Published in:European journal of cancer (1990) 2016-12, Vol.69, p.S89-S89
Main Authors: Tontsch-Grunt, U, Savarese, F, Baum, A, Scharn, D, Gerlach, D, Hofmann, M.H, Popow, J, Schweifer, N, Engelhardt, H, Musa, H, Lee, C.P, Munzert, G.M, Kraut, N
Format: Article
Language:English
Subjects:
Biomarkers
Blood diseases
Clinical trials
Elongation
Hematology
Hematology, Oncology and Palliative Medicine
Inhibition
Inhibitors
Medical research
Medical treatment
Myc protein
Proteins
Robustness (mathematics)
Studies
Transcription elongation
Tumors
Xenografts
Xenotransplantation
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Summary:An abstract of the study of Tontsch-Grunt et al. about BET inhibitor BI 894999 with CDK9 inhibition suggests a promising regimen for the treatment of AML. Among other things bromodomain and extra-terminal (BET) protein inhibitors comprising the family members BRD2, 3, 4 and T are being extensively studied as treatment options in human hematological malignancies as well as in solid cancers. BRD4 is a key epigenetic regulator of transcriptional elongation, particularly of oncogenes including MYC. BI 894999 shows remarkable synergy with CDK9 inhibition in vitro and in xenograft models. BI 894999 is a novel, potent and selective orally bloavailable inhibitor of the BET family. This compound is in clinical trials (NCT02516553). BET bromodomain inhibitor BI 894999 shows potent antiproliferative effect in hematological cell lines, primary human malignant cells and in in vivo tumor models. Synergy with CDK9i leads to remarkable tumor regressions. HEXIM1 is described as a robust PD biomarker.
ISSN:0959-8049
1879-0852
DOI:10.1016/S0959-8049(16)32862-3