Vorinostat
Histone deacetylase (HDAC) inhibitors
Histone deacetylase (HDAC) inhibitorsHigh alert
An 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.
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.
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.
- Vorinostat enters the HDAC active site
- Its hydroxamic acid chelates the zinc ion
- Acetylated histones accumulate and chromatin opens
- Silenced genes return: arrest or apoptosis
Indications
- Cutaneous T-cell lymphoma with progressive, persistent or recurrent skin disease during or after two systemic therapies. Mycosis fungoides and Sézary syndrome (cutaneous T-cell lymphoma) →
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).
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.
