Drug intelligence / Profile preview

CC-90011 + venetoclax + azacitidine

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

CC-90011 + venetoclax + azacitidine is an investigational **combination regimen** under clinical evaluation for the treatment of hematologic malignancies, notably acute myeloid leukemia (AML) and related disorders. - **CC-90011** is a potent, oral, selective, and reversible inhibitor of lysine-specific demethylase 1 (LSD1, also known as KDM1A), which is being developed for multiple cancers including AML and neuroendocrine tumors[1][3][4]. It reversibly inhibits LSD1, modulating epigenetic repression, inducing tumor differentiation, and suppressing tumor-promoting gene expression[1][3][5]. - **Venetoclax** is a selective, oral small-molecule inhibitor of B-cell lymphoma 2 (BCL-2) protein, promoting apoptosis in malignant cells. - **Azacitidine** is a DNA methyltransferase inhibitor and nucleoside analog that causes hypomethylation of DNA and direct cytotoxicity, reactivating tumor suppressor genes and inducing apoptosis in abnormal hematopoietic cells. This triplet combination is currently being investigated in clinical research settings for its synergistic antitumor activity, particularly in AML, where epigenetic modification, inhibition of anti-apoptotic signaling, and cytotoxic effects may provide enhanced efficacy over standard regimens[4].

02

Targets

BCL-2 (BCL-2 family)DNMT (DNA methyltransferase)KDM1A (LSD1)

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