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EP31670
- Development stage
- Phase 1
- Lead developer
- Epigenetix
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
EP31670 (also known as NEO2734) is an orally bioavailable, first-in-class small molecule that acts as a dual inhibitor of the bromodomains of the BET (bromodomain and extra-terminal) family proteins and the histone acetyltransferase paralogs CREB binding protein (CBP) and p300. By targeting both epigenetic "readers" (BET proteins) and "writers" (CBP/p300), EP31670 disrupts oncogenic transcriptional programs critical for cancer cell survival. Preclinical studies have demonstrated potent antitumor activity in hematologic malignancies such as lymphomas, leukemias, myelofibrosis, as well as in solid tumors including prostate cancer and NUT midline carcinoma. The drug is currently being evaluated in Phase 1 clinical trials for advanced solid tumors and hematological malignancies[1][2][3][4][5][7][8].
- Other names
- NEO2734NEO-2734NEO 2734
02
Targets
CREBBP BD (Creb-binding protein bromodomain)EP300 (Histone acetyltransferase p300)BRD4 (Bromodomain-containing protein 4)
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