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Histone deacetylase (HDAC) inhibitors

Epigenetic drugs that block histone deacetylases, reopening silenced genes; vorinostat and romidepsin treat cutaneous T-cell lymphoma.

Updated

What they are

Histone deacetylases remove acetyl groups from histones and other proteins, compacting chromatin and silencing genes, including tumour suppressors. HDAC inhibitors reverse this. Vorinostat (oral) and romidepsin (intravenous) are used in cutaneous T-cell lymphoma; panobinostat and belinostat in other blood cancers.

Mechanism of action

They bind the zinc ion in the active site of HDACs. Acetylated histones and transcription factors accumulate, chromatin opens and genes that stop the cell cycle or trigger differentiation and apoptosis are expressed again.

Target: Histone deacetylases (zinc-dependent enzymes)

Drugs in this class

Others in the class

  • panobinostat
  • belinostat

Test yourself

Think of the answer, then tap the question to see it.

What does an HDAC inhibitor do to chromatin?

It keeps histones acetylated, so chromatin stays open and silenced genes can be expressed.

Which lymphoma do vorinostat and romidepsin treat?

Cutaneous T-cell lymphoma.

Which electrolytes are checked before an HDAC inhibitor and why?

Potassium and magnesium, because these drugs can cause ECG changes and QT prolongation.

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Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.

Sources: Vorinostat: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); Romidepsin Injection: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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