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Vorinostat

  • Histone deacetylase (HDAC) inhibitorsHistone deacetylase (HDAC) inhibitors
  • High alertAn error with this medicine can cause serious harm: double checks and protocols are used.

Oral histone deacetylase inhibitor for cutaneous T-cell lymphoma. Watch for dehydration, high blood sugar, low platelets and blood clots.

Updated

Also called: SAHA (suberoylanilide hydroxamic acid)

Quick facts

Group
Histone deacetylase (HDAC) inhibitors
Target
Histone deacetylases (class I HDAC1, 2 and 3, and HDAC6)
Used for
Cutaneous T-cell lymphoma
Key effects
Diarrhoea · Fatigue · Taste changes
Monitor
Complete blood count · Electrolytes · Signs of clots
ATC
L01XH01

No doses: the clinician sets them by the current guideline.

Mechanism of action

The crystal structure shows vorinostat in the active site of human HDAC2, with its hydroxamic acid holding the catalytic zinc ion.

Target in 3D: Histone deacetylases (class I HDAC1, 2 and 3, and HDAC6). PDB structure 4LXZ (RCSB PDB, public domain). View the structure at RCSB PDB

Vorinostat binds the active site of histone deacetylases and chelates the zinc ion there. HDAC1, 2, 3 and 6 are inhibited, so acetylated histones and other acetylated proteins, including transcription factors needed for differentiation, accumulate. Gene expression changes, and some cancer cells stop the cell cycle or undergo apoptosis.

  1. Vorinostat enters the HDAC active site
  2. Its hydroxamic acid chelates the zinc ion
  3. Acetylated histones accumulate and chromatin opens
  4. Silenced genes return: arrest or apoptosis

Indications

Adverse effects

Common

  • Diarrhoea, nausea, vomiting, decreased appetite, weight loss
  • Fatigue, dizziness, drowsiness
  • Taste changes, dry mouth
  • Thrombocytopenia, anaemia
  • Hair loss, itching, muscle aches

Contraindications

  • Severe liver impairment (excluded from treatment)
  • Caution with prior blood clots, diabetes, rhythm problems and low potassium or magnesium

Key interactions

Drugs that prolong the QT interval or lower potassium or magnesium
Add to the risk of rhythm problems; electrolytes are corrected.
Anticoagulants and antiplatelet drugs
Bleeding risk is higher when platelets fall; coagulation tests and counts are watched.

What is monitored

  • Complete blood count, especially platelets
  • Electrolytes (potassium, magnesium), creatinine and glucose
  • ECG when there is a risk of QT prolongation
  • Signs of clots: painful leg swelling, chest pain, breathlessness
  • Hydration

Administration and safety

  • Oral, once a day with food at about the same time.
  • Capsules are swallowed whole and not opened or crushed.
  • Plenty of fluids are taken every day to prevent dehydration.
  • Hazardous oral chemotherapy: handled with gloves and kept away from children; caregivers who are pregnant avoid handling it.

Pregnancy and breastfeeding

May harm the fetus; a pregnancy test is done before starting and effective contraception is used; breastfeeding is avoided during treatment and shortly after.

Nursing care

  • Ask about diarrhoea and vomiting and check for dehydration.
  • Check glucose, especially in people with diabetes.
  • Ask about leg swelling, chest pain or sudden breathlessness (clots).
  • Teaching: drink plenty of fluids, report bleeding or bruising, be careful driving if drowsy, tell lab staff about the treatment.

Pharmacokinetics

Absorption
Oral; absorption is slightly better with a meal.
Metabolism
Mostly glucuronidation and hydrolysis.
Half-life
Short, about 2 hours.

Test yourself

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

What enzyme family does vorinostat inhibit?

Histone deacetylases (HDACs).

How does vorinostat bind its target?

It binds the HDAC active site and chelates the catalytic zinc ion.

Which lymphoma is vorinostat used for?

Cutaneous T-cell lymphoma.

Which two metabolic or vascular problems are watched with vorinostat?

Any two of: hyperglycaemia, dehydration, blood clots (pulmonary embolism, deep vein thrombosis).

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Connections

← Back to the class: Histone deacetylase (HDAC) inhibitors

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); Vorinostat - NCI (National Cancer Institute, 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026).

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Representative model, for educational purposes only.