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Mocetinostat + azacitidine
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral, Subcutaneous, Intravenous
01
Overview
MGCD0103 (mocetinostat) is an oral, isotype-selective histone deacetylase (HDAC) inhibitor that targets HDAC isoforms 1, 2, 3 (class I), and 11 (class IV), with minimal activity against class II enzymes. Azacitidine is a DNA methyltransferase inhibitor and hypomethylating agent approved for the treatment of myelodysplastic syndromes (MDS). The combination of MGCD0103 and azacitidine has been investigated in clinical trials for patients with acute myeloid leukemia (AML) and MDS due to their synergistic epigenetic effects—MGCD0103 modulates gene expression by inhibiting HDACs, while azacitidine induces DNA hypomethylation. Both drugs have demonstrated single-agent activity in MDS and AML; together they may offer enhanced efficacy compared to monotherapy. This combination has shown clinical responses in early-phase studies for advanced hematologic malignancies[5][6].
- Brand names
- Vidaza
- Other names
- azacitidine + MGCD-0103azacitidine + mocetinostat5-azacitidine + MGCD0103
02
Targets
HDAC11 (Histone Deacetylase 11)HDAC1 (Histone Deacetylase 1)DNMT1 (DNA (cytosine-5)-methyltransferase 1)
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