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azacitidine + romidepsin
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
- Administration
- Intravenous, Subcutaneous
01
Overview
Azacitidine + romidepsin is a combination therapy of two small molecule drugs used primarily in the treatment of relapsed or refractory peripheral T-cell lymphoma (PTCL) and other T-cell malignancies. Azacitidine is a DNA methyltransferase inhibitor (a hypomethylating agent), while romidepsin is a histone deacetylase (HDAC) inhibitor. Together, they act as epigenetic modifiers that synergistically inhibit cancer cell proliferation and induce apoptosis by altering gene expression through DNA demethylation and increased histone acetylation. This combination has shown higher efficacy in PTCL compared to B-cell lymphomas and demonstrates particular activity in patients with T-follicular helper cell phenotype. The regimen is under investigation in phase 2 clinical trials for PTCL[1][2][3][4][5][6].
- Other names
- azacitidine + romidepsinCC-486 + romidepsinoral 5-azacitidine + romidepsin
02
Targets
HDAC (HDAC family)DNMT (DNA methyltransferase)
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