Drug intelligence / Profile preview

inobrodib + azacitidine

Development stage
Phase 2
Lead developer
CellCentric
Modality
Small Molecules
Administration
Oral, Intravenous, Subcutaneous
01

Overview

**Inobrodib + azacitidine** is an investigational combination therapy currently in clinical development for hematologic malignancies (including acute myeloid leukemia and high-risk myelodysplastic syndrome). Inobrodib is a potent, selective, orally bioavailable small-molecule inhibitor of the bromodomains of CBP and EP300, which are histone acetyltransferases crucial for transcriptional regulation of cancer-driving genes such as MYC and IRF4. Azacitidine is a hypomethylating agent and a pyrimidine nucleoside analog, which inhibits DNA methyltransferase, leading to DNA hypomethylation and reactivation of silenced genes involved in differentiation and apoptosis. The combination aims to enhance anti-tumor activity by simultaneously modulating chromatin structure, gene expression, and DNA methylation status.

Other names
inobrodibCCS1477CCS-1477CCS 1477azacitidine
02

Targets

CREBBP BD (Creb-binding protein bromodomain)DNMT1 (DNA (cytosine-5)-methyltransferase 1)EP300 BD (E1A Binding Protein p300 Bromodomain)CREBBP (CREB-binding protein)

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