Drug intelligence / Profile preview

inobrodib + azacitidine + venetoclax

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

Overview

This is a combination therapy comprised of three small-molecule drugs: **inobrodib**, **azacitidine**, and **venetoclax**. - **Inobrodib** is a first-in-class, orally available small molecule inhibitor of the epigenetic regulators p300 and CBP, proteins that are important for transcriptional activation in cancer cells. By inhibiting these proteins, inobrodib modulates gene expression critical for cancer cell survival, showing activity in multiple cancer types including hematologic malignancies. - **Azacitidine** is a hypomethylating agent (antimetabolite) that incorporates into DNA and RNA, leading to DNA hypomethylation and direct cytotoxicity, especially in abnormal hematopoietic cells. - **Venetoclax** is a selective inhibitor of BCL-2, an anti-apoptotic protein; by inhibiting BCL-2, venetoclax restores apoptosis in cancer cells, particularly in certain hematological malignancies. The combination of these three drugs is under early-phase investigation, primarily for hematologic malignancies such as multiple myeloma and potentially other blood cancers. The combination exploits complementary mechanisms to target malignant cells: epigenetic disruption (inobrodib), reversal of DNA methylation (azacitidine), and promotion of apoptosis (venetoclax).

02

Targets

BCL-2 (BCL-2 family)CREBBP BD (Creb-binding protein bromodomain)DNMT (DNA methyltransferase)EP300 BD (E1A Binding Protein p300 Bromodomain)CREBBP (CREB-binding protein)

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