Drug intelligence / Profile preview

IACS-70654

Development stage
Preclinical
Lead developer
University of Texas MD Anderson Cancer Center
Modality
Small Molecules
Administration
Oral
01

Overview

IACS-70654 is a selective small-molecule inhibitor of the CREB-binding protein (CBP) and E1A-associated protein p300 (EP300) bromodomains (BRD). Developed by the Institute for Applied Cancer Science (IACS) at the University of Texas MD Anderson Cancer Center, IACS-70654 targets the epigenetic reader function of CBP/P300. In preclinical models of triple-negative breast cancer (TNBC), particularly those enriched with tumor-associated neutrophils (TANs), IACS-70654 has been shown to reduce immunosuppressive TAN accumulation, inhibit abnormal myelopoiesis in the bone marrow, and stimulate antitumor immunity by inducing interferon (IFN) responses and major histocompatibility complex class I (MHCI) expression. It also enhances the efficacy of standard-of-care therapies, such as docetaxel and immune checkpoint blockade.

02

Targets

CREBBP BD (Creb-binding protein bromodomain)CREBBP (CREB-binding protein)EP300 (Histone acetyltransferase p300)

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