A focus on the preclinical development and clinical status of the histone deacetylase inhibitor, romidepsin (depsipeptide, Istodax(®)).

Abstract	Romidepsin (Istodax(®), depsipeptide, FR901228, FK228, NSC 630176) is a cyclic peptide, broad-spectrum, potent histone deacetylase inhibitor, with activity mainly against class I histone deacetylase enzymes. In this article, we give an overview of the putative modes of action, such as effects on gene expression, cell cycle regulation, apoptosis induction, DNA repair, protein acetylation and induction of autophagy. Romidepsin has mainly been developed as a therapy for hematologic malignancies and is approved by the US FDA for the treatment of cutaneous T-cell lymphomas. This report outlines the laboratory and clinical development of the compound as a single agent that has more recently been evaluated in combination with other anticancer therapeutics, such as proteasome inhibitors.
Authors	Simon J Harrison, Mark Bishton, Susan E Bates, Steven Grant, Richard L Piekarz, Ricky W Johnstone, Yun Dai, Becki Lee, Maria E Araujo, H Miles Prince
Journal	Epigenomics (Epigenomics) Vol. 4 Issue 5 Pg. 571-89 (Oct 2012) ISSN: 1750-192X [Electronic] England
PMID	23130838 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	Antineoplastic Agents Boronic Acids Depsipeptides HIF1A protein, human Histone Deacetylase Inhibitors Hypoxia-Inducible Factor 1, alpha Subunit Proteasome Inhibitors Pyrazines Bortezomib romidepsin HDAC6 protein, human Histone Deacetylase 6 Histone Deacetylases
Topics	Acetylation (drug effects) Animals Antineoplastic Agents (pharmacology) Apoptosis (drug effects) Autophagy Boronic Acids (pharmacology) Bortezomib Cell Line, Tumor Clinical Trials as Topic Depsipeptides (administration & dosage, pharmacology) Drug Evaluation, Preclinical Drug Synergism Histone Deacetylase 6 Histone Deacetylase Inhibitors (pharmacology) Histone Deacetylases (metabolism) Humans Hypoxia-Inducible Factor 1, alpha Subunit (antagonists & inhibitors, metabolism) Lymphoma, T-Cell, Cutaneous (drug therapy) Neovascularization, Pathologic Proteasome Inhibitors (pharmacology) Pyrazines (pharmacology)

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