Delving into the Latest Updates on ZEN-3365 with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

+ [1]

Target

BET

Mechanism

BET inhibitors(Bromodomain and extra terminal domain protein inhibitors)

Therapeutic Areas

NeoplasmsHemic and Lymphatic Diseases

Active Indication-

Inactive Indication

Refractory acute myeloid leukemiaRelapsing acute myeloid leukemia

Originator Organization

Zenith Epigenetics Ltd.

Active Organization-

Inactive Organization

Zenith Epigenetics Ltd.

Drug Highest PhaseDiscontinuedPhase 1

First Approval Date-

Regulation-

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AbstractModern cancer therapies increased the survival rates of acute myeloid leukemia (AML) patients tremendously. However, the complexity of the disease and the identification of new targets require the adaptation of treatment protocols to reduce side effects and increase benefit for the patients. One key regulator of leukemogenesis and chemotherapy resistance in AML is the Hedgehog (HH) signaling pathway. It is deregulated in numerous cancer entities and inhibition of its downstream transcription factors GLI translates into anti-leukemic effects. One major regulator of GLI is BRD4, a BET family member with epigenetic functions. We investigated the effect of ZEN-3365, a novel BRD4 inhibitor, on AML cells in regard to the HH pathway. We show that ZEN-3365 alone or in combination with GANT-61 reduced GLI promoter activity, cell proliferation and colony formation in AML cell lines and primary cells. Our findings strongly support the evaluation of the BRD4 inhibitor ZEN-3365 as a new therapeutic option in AML.

100 Deals associated with ZEN-3365

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Refractory acute myeloid leukemia	Phase 1	US	Zenith Epigenetics Ltd.	01 Oct 2014
Relapsing acute myeloid leukemia	Phase 1	US	Zenith Epigenetics Ltd.	01 Oct 2014