About Epigene Therapeutics

Epigene Therapeutics Inc. was created by the NEOMED Institute in December 2017. The Epigene Therapeutics team is dedicated to advancing novel epigenetic modulators for the targeted treatment of cancer. Epigene Therapeutics has generated six distinct chemical series/scaffolds from which a portfolio of novel epigenetic modulators is advancing through preclinical development. The lead molecule, NEO2734, currently in late pre-IND stage of development, is an orally-bioavailable, first-in-class dual Bromodomain and Extra-Terminal domain (BET) and Cyclic AMP response element binding protein (CREB)-binding protein (CBP) and E1A interacting protein of 300 kDa (EP300 or P300) [CBP/P300] inhibitor. The activity of NEO2734 in a spectrum of hematological malignancies and solid tumors, relative to that of traditional BET inhibitors, have been presented at EHA (European Hematology Association) and ESMO (European Society for Medical Oncology) 2018, with a forthcoming presentation at ASH (American Society of Hematology) in December 2018. Initial clinical studies of NEO2734 in patients with cancer are planned for 2019.

NEO2734's Targets

The Bromodomain (BRD) and Extra-Terminal domain (BET) family of proteins are key regulators of epigenetic control. Modulation of epigenetic 'readers' such as BRDs is a recognized developmental therapeutics priority. Cyclic AMP response element binding protein (CREB)-binding protein (CBP) and E1A interacting protein of 300 kDa (EP300 or P300) (P300/CBP) are highly homologous BRD-containing transcriptional co-activators ('writers') that regulate a number of important cellular events through their acetyltransferase activity. Inhibitors of BETs are in development, being studied alone1, or in combination with other class inhibitors (eg, tyrosine kinase inhibitor2; BCL-2 inhibitor3). The synergistic effect of JQ1 (a prototypic BET inhibitor) and a CBP/P300 inhibitor has been demonstrated.4

1. Lin et al, 800/10, AACR 2018
2. Liu et al., Mol Cancer Ther; 13 (5) May, 2014
3. Cai et al, LB-261/5, AACR 2018
4. Picaud et al., Cancer Res; 75(23) Dec 1, 2015

We have developed a series of molecules that exhibit dual inhibition of both BET and CBP/P300 from which NEO2734 has emerged as lead clinical candidate. In addition to NEO2734, the Epigene Therapeutics pipeline includes a second (chemically distinct from NEO2734) dual BET and CBP/P300 inhibitor (NEO1132) and a CBP/P300 inhibitor lead generation program.