Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma.
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VanderMolen KM, McCulloch W, Pearce CJ, Oberlies NH
Romidepsin (Istodax, NSC 630176, FR901228, FK228, depsipeptide): a natural product recently approved for cutaneous T-cell lymphoma.
J Antibiot (Tokyo). 2011 Aug;64(8):525-31. doi: 10.1038/ja.2011.35. Epub 2011 May 18.
- PubMed ID
- 21587264 [ View in PubMed]
- Abstract
Romidepsin (Istodax), a selective inhibitor of histone deacetylases (HDACs), was approved for the treatment of cutaneous T-cell lymphoma in November 2009 by the US Food and Drug Administration. This unique natural product was discovered from cultures of Chromobacterium violaceum, a Gram-negative bacterium isolated from a Japanese soil sample. This bicyclic compound acts as a prodrug, its disulfide bridge being reduced by glutathione on uptake into the cell, allowing the free thiol groups to interact with Zn ions in the active site of class I and II HDAC enzymes. Due to the synthetic complexity of the compound, as well as the low yield from the producing organism, analogs are sought to create synthetically accessible alternatives. As a T-cell lymphoma drug, romidepsin offers a valuable new treatment for diseases with few effective therapies.
DrugBank Data that Cites this Article
- Drugs
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Romidepsin Histone deacetylase 1 Protein Humans YesAntagonistInhibitorDetails Romidepsin Histone deacetylase 2 Protein Humans YesAntagonistInhibitorDetails Romidepsin Histone deacetylase 4 Protein Humans NoInhibitorDetails Romidepsin Histone deacetylase 6 Protein Humans NoInhibitorDetails - Drug Reactions
Reaction Details
