Histone Deacetylase (HDAC) Inhibitors in Recent Clinical Trials for Cancer Therapy

  • Kristina Keller
  • Manfred Jung


Histone deacetylases are key enzymes of epigenetic regulation and are therefore involved in crucial cellular events like transcription, differentiation, apoptosis and cell division. The deacetylation of many non-histone substrates contributes to these phenomena as well. Thus, these enzymes are an attractive target for anticancer drug development, and first inhibitors are already approved for treatment of cutaneous T-cell lymphoma. About 10–15 inhibitors are currently in clinical trials for a variety of diseases but as single-agent response rates have so far been limited, esp. in solid tumours. There are many open questions, such as the relevance of subtype selectivity in enzyme inhibition, the clinical relevance of non-histone substrates and proper combination regimens. Still, histone deacetylase inhibitors are a promising class of new anticancer agents, and here we review their anticancer properties with a focus on clinical trials from the last 3 years.


Partial Response Stable Disease Valproic Acid HDAC Inhibitor Adenoid Cystic Carcinoma 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.



Two times daily




Complete response


Cutaneous T-cell lymphoma


Dose-limiting toxicity


Enzyme-inducing antiepileptic drugs


Food and Drug Administration


Histone deacetylase


Histone deacetylase inhibitor


Haematological improvement


Maximum tolerated dose


Monday, Wednesday, Friday


Overall response rate


Overall survival


Peripheral blood mononuclear cell


Progression free survival


Partial response


Once daily


Recommended phase II dose


Stable disease



The authors thank the Deutsche Forschungsgemeinschaft for funding (Ju 295/9-1 within the priority programme SPP1463 Epigenetic regulation of normal hematopoiesis and its dysregulation in myeloid neoplasia; coordinators M. Lübbert, Freiburg, C. Plass, Heidelberg).


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© Springer-Verlag Berlin Heidelberg 2014

Authors and Affiliations

  1. 1.Institute of Pharmaceutical SciencesAlbert-Ludwigs-Universität FreiburgFreiburgGermany

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