Histone deacetylase inhibitors in cancer therapy

Curr Opin Oncol. 2008 Nov;20(6):639-49. doi: 10.1097/CCO.0b013e3283127095.


Purpose of review: The purpose of this review is to provide an overview of recent advances in the development of histone deacetylase inhibitors (HDACi) for the treatment of cancer.

Recent findings: Recently, there has been a dramatic expansion of HDACi clinical investigation. There are now 11 HDACi in clinical trial, including inhibitors with a broad spectrum of HDAC isoform inhibitory activity as well as drugs with isoform selectivity. Over 70 combination therapy trials are in progress. Major areas of progress covered include the entry of new HDAC inhibitors into clinical development, recent progress in understanding of molecular mechanisms of HDACi anticancer activity, and a preclinical and clinical update on HDACi in combination.

Summary: In the period under review there have been advances in understanding of HDACi mechanisms of action, identification of rational combinations that address increased efficacy and overcoming resistance, and greatly expanded clinical development of pan-HDAC-inhibitory and isoform-selective inhibitors in monotherapy and combination therapy protocols.

Publication types

  • Research Support, N.I.H., Intramural
  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Antineoplastic Agents / therapeutic use*
  • Apoptosis
  • Chemistry, Pharmaceutical / methods
  • Chemistry, Pharmaceutical / trends
  • Clinical Trials as Topic
  • Drug Design
  • Enzyme Inhibitors / therapeutic use
  • Histone Deacetylase Inhibitors*
  • Histones / metabolism
  • Humans
  • Immune System
  • Medical Oncology / methods
  • Medical Oncology / trends
  • Models, Chemical
  • Neoplasms / drug therapy*
  • Neoplasms / pathology*
  • Neoplastic Stem Cells
  • Protein Isoforms


  • Antineoplastic Agents
  • Enzyme Inhibitors
  • Histone Deacetylase Inhibitors
  • Histones
  • Protein Isoforms