Drug intelligence / Profile preview

ipilimumab + decitabine

Development stage
Unknown
Lead developer
National Cancer Institute
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Ipilimumab + decitabine is a combination therapy investigated for the treatment of relapsed or refractory myelodysplastic syndrome (MDS) and acute myeloid leukemia (AML). Ipilimumab is a recombinant human monoclonal antibody that acts as an immune checkpoint inhibitor by binding to the Cytotoxic T-Lymphocyte-Associated Protein 4 (CTLA-4). By blocking CTLA-4, it prevents the inhibitory signal that normally downregulates T-cell activation, thereby enhancing the immune system's ability to attack tumor cells. Decitabine is a small molecule hypomethylating agent that functions as a DNA methyltransferase inhibitor. It incorporates into DNA and covalently binds to DNA methyltransferases, leading to their depletion and subsequent global DNA hypomethylation. This process can reactivate tumor suppressor genes that were silenced by hypermethylation. The combination is designed to leverage the epigenetic priming effects of decitabine to enhance the efficacy of CTLA-4 blockade in myeloid malignancies.

Brand names
YervoyDacogen
Other names
ipilimumab and decitabine
02

Targets

DNMT1 (DNA (cytosine-5)-methyltransferase 1)CTLA-4 (Cytotoxic t-lymphocyte–associated protein 4)DNMT3A (DNA methyltransferase 3 alpha)

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