Bromodomain inhibitor against cancer


Acute leukemia, breast cancer, glioblastoma, lung cancer, lymphoma, melanoma, mesothelioma, neuroblastoma, ovarian cancer, pancreatic cancer, prostate cancer

Mode Of Action

Dual inhibitor of BET and CBP/P300

Main Advantages

  • Selective for bromodomain family of targets
  • Bromodomain (BRD) compounds inhibit epigenetic reader proteins that modulate transcription of genes associated with disease states
  • Additional activity at CREBBP and EP300 synergizes with BET activity providing enhanced efficacy resulting in a larger therapeutic window
  • NEO#### exhibits both cytotoxic and immuno-oncological properties


Epigenetix Inc., Florida, USA


How NEO#### Works

Bromodomains (BRDs) are key modulators of epigenetic control – this control is abnormal in some cancers. BRD4 inhibitors can treat cancer by restoring epigenetic control.
Much support has been accumulating for BRDs as cancer targets. NEO#### demonstrates a broad spectrum of in-vitro activity against a variety of cancer types and will be explored in priority indications which will be chosen based on data from our extensive pre-clinical collaborations.
Synergistically inhibiting both BRD4 and CBP/P300 may explain the observed enhanced efficacy as compared to other compounds in development.

Safety has been demonstrated in rodents, dogs and non-human primates in several non-GLP studies. In vitro and in vivo studies have shown at least 10-fold better cell membrane penetration and anti-tumor potency than other inhibitors in development while maintening a good safety profile.

Compounds were identified from 4 different chemical series with distinct scaffolds. Due to its superior in-vivo efficacy NEO#### was the selected lead candidate.

For more information

Bill Brown

Project Director

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