Romidepsin (Istodax, NSC 630176, FR901228, FK228, Depsipeptide): A Natural Product Recently Approved for Cutaneous T-Cell Lymphoma

UNCG Author/Contributor (non-UNCG co-authors, if there are any, appear on document)
Nicholas Oberlies, Patricia A. Sullivan Distinguished Professor of Chemistry (Creator)
Cedric J Pearce, Adjunct Professor (Creator)
The University of North Carolina at Greensboro (UNCG )
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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.

Additional Information

Journal of Antibiotics, 2011, 64, 525-531. PMID: 21587264; PMCID: PMC3163831; doi: 10.1038/ja.2011.35
Language: English
Date: 2011
Chromobacterium violaceum, cutaneous T-cell lymphoma, depsipeptide, histone deacetylase inhibitor, Istodax, romidepsin

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