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pracinostat + azacitidine
- Development stage
- Discontinued
- Lead developer
- Helsinn
- Modality
- Small Molecules
- Administration
- Oral, Intravenous, Subcutaneous
01
Overview
**Pracinostat + azacitidine** is a combination of two drugs: pracinostat, a potent oral pan-histone deacetylase (HDAC) inhibitor, and azacitidine, a DNA methyltransferase (DNMT) inhibitor classified as a hypomethylating agent. The combination is intended to provide synergistic antitumor activity by epigenetically reactivating silenced tumor suppressor and regulatory genes in the treatment of acute myeloid leukemia (AML) in patients ineligible for intensive chemotherapy. Pracinostat inhibits class I, II, and IV HDACs, thereby altering gene expression, while azacitidine causes DNA hypomethylation and cytotoxicity in abnormal hematopoietic cells. This combination has shown clinical activity in early-phase studies, especially in older or unfit newly diagnosed AML patients, achieving notable remission and survival rates. However, a large phase 3 trial failed to demonstrate a survival benefit over azacitidine monotherapy, and development for this indication has been discontinued[1][2][3][4][5].
- Brand names
- Pracinostat
- Other names
- Pracinostat + azacitidine
02
Targets
DNMT1 (DNA (cytosine-5)-methyltransferase 1)
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