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Romidepsin is a histone deacetylase (HDAC) inhibitor used to treat cutaneous T-cell lymphoma. A chemotherapy agent used to treat cancers affecting specific types of white blood cells.
- Mechanism
- Curator reviewed
Romidepsin is a prodrug, where it becomes active once taken up into the cell. The active metabolite has a free thiol group, which interacts with zinc ions in the active site of class 1 and 2 HDAC enzymes, resulting in inhibition of its enzymatic activity. Certain tumors have over expressed HDACs and downregulated/mutated histone acetyltransferases. This imbalance of HDAC relative to histone acetyltransferase can lead to a decrease in regulatory genes, ensuing tumorigenesis. Inhibition of HDAC may restore normal gene expression in cancer cells and result in cell cycle arrest and apoptosis.
- Primary indication
- Romidepsin is indicated for the treatment of cutaneous T-cell lymphoma (CTCL) in adult patients who have received at least one prior systemic therapy.Curator reviewed · 1 structured indication
- Formula / weight
- C24H36N4O6S2 · 540.69 g/mol (avg)
- First approval
- Canada, 2024 · United States, 2009
- Also known as
- Depsipeptide
- Code names
- FK-228 · FR-901228 · NSC-630176
- Brand names
- Istodax
Resolves to
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Which drugs share a target with Romidepsin, and which of those have an active Phase 3 trial?