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May 17, 2026Science Advances0 citationsOpen Access

P300/CBP inhibition with inobrodib in combination with gilteritinib and venetoclax targets leukemia stem cells in epigenetic mutant AML

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MGMelanie L. GoetzJRJennifer S. Romer-SeibertAVAmanda M. Versace

Key Points

  • The study aims to determine the effectiveness of a triplet therapy targeting leukemia stem cells in acute myeloid leukemia (AML).
  • Preclinical model used was of DNMT3A/FLT3-mutant AML.
  • Combination therapy included inobrodib, venetoclax, and gilteritinib.
  • Focus on evaluating reduction of leukemia stem cells and related oncogenic factors.
  • The combination treatment virtually eliminates leukemia stem cells in the model.
  • Significant impairment of pro-oncogenic survival and proliferation factors was observed.
  • Demonstrated efficacy in blocking leukemogenesis in the preclinical setup.

Abstract

Acute myeloid leukemia (AML) is a fatal blood cancer with cytotoxic chemotherapy offering at best 25% 5-year survival. While targeted BCL2 and FLT3 inhibitors venetoclax and gilteritinib are used upfront in the treatment of a subset of adult patients with AML and help to extend the survival of some patients, a curative treatment combination with minimal side effects has yet to be discovered. We find that use of the dual histone acetyltransferase p300/CBP bromodomain inhibitor CCS1477 (inobrodib), together with venetoclax and gilteritinib, virtually eliminates leukemia stem cells in an aggressive preclinical model of DNMT3A/FLT3 -mutant AML by impairing pro-oncogenic survival and proliferation factors to effectively block leukemogenesis. This work identifies potential clinical utility of a targeted, triplet combination therapy for treatment of AML.

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Cite This Study

Goetz et al. (2026) studied this question.

synapsesocial.com/papers/6a095bdd7880e6d24efe1af8https://doi.org/10.1126/sciadv.aec9305
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