
NCBI . NLM . NIH . GOV {
}
Title[redir]:
The DOT1L inhibitor pinometostat reduces H3K79 methylation and has modest clinical activity in adult acute leukemia - PMC
Description:
Pinometostat demonstrates first evidence of DOT1L target inhibition and clinical responses in a subset of MLL-r advanced leukemia patients. The observed safety profile of pinometostat shows potential for exploration of combination therapies in ...
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Keywords {๐}
patients, pinometostat, day, leukemia, dotl, study, treatment, patient, doi, pubmed, google, scholar, inhibition, clinical, mllr, mgm, mll, infusion, data, civ, pmc, acute, cell, hkme, article, dose, levels, blood, response, plasma, desc, disease, drug, failure, free, safety, doses, days, figure, activity, target, methyltransferase, cycle, cancer, treated, methylation, histone, phase, aml, achieved,
Topics {โ๏ธ}
mann-whitney 2-tailed student class small-molecule inhibitor high-risk myelodysplastic syndrome short ฮฑ-elimination phase pmc beta search blood web site leukaemia stem-cell development relapsed/refractory hematologic malignancies /mll-ptd restricted/expansion phase calm-af10-mediated transformation relapsed/refractory acute leukemias pinometostat concentrationโtime profile human mll-af4 leukemias disease-specific response criteria biopsy-documented leukemia cutis small-molecule inhibitor common terminology criteria approximately dose-proportional fashion mll-rearranged leukemia cells supplementary materials included dose-expansion multicenter study national cancer institute page charge payment fusion protein targets enabled full identification mll-af9-mediated leukemogenesis 11q23/mll acute leukemia quantitative hox expression apparent steady-state level increased blast count open-label dose-escalation postdose time points small cohort sizes license information pmcid validated methods performed acute hematologic malignancies received research funding advanced acute leukemias small molecule inhibitors bone marrow consistent included intracranial hemorrhage steady-state concentration leukemia cell lines h3k79 methylation results polymerase chain reaction electrocardiogram qt prolonged received funding support bone marrow aspiration chip-seq analysis receives research funding
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