Pharmacogenomics and histone deacetylase inhibitors

Andrew KL Goey, Tristan M. Sissung, Cody J. Peer, William D. Figg*

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

25 Scopus citations


The histone deacetylase inhibitor valproic acid (VPA) has been used for many decades in neurology and psychiatry. The more recent introduction of the histone deacetylase inhibitors (HDIs) belinostat, romidepsin and vorinostat for treatment of hematological malignancies indicates the increasing popularity of these agents. Belinostat, romidepsin and vorinostat are metabolized or transported by polymorphic enzymes or drug transporters. Thus, genotype-directed dosing could improve pharmacotherapy by reducing the risk of toxicities or preventing suboptimal treatment. This review provides an overview of clinical studies on the effects of polymorphisms on the pharmacokinetics, efficacy or toxicities of HDIs including belinostat, romidepsin, vorinostat, panobinostat, VPA and a number of novel compounds currently being tested in Phase I and II trials. Although pharmacogenomic studies for HDIs are scarce, available data indicate that therapy with belinostat (UGT1A1), romidepsin (ABCB1), vorinostat (UGT2B17) or VPA (UGT1A6) could be optimized by upfront genotyping.

Original languageEnglish
Pages (from-to)1807-1815
Number of pages9
Issue number16
StatePublished - Nov 2016
Externally publishedYes


  • HDAC inhibitors
  • UGT1A1
  • belinostat
  • panobinostat
  • pharmacogenomics
  • romidepsin
  • valproic acid
  • vorinostat


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