Vorinostat
FDA-approved HDAC-inhibitor cancer drug; its neuroprotective effect is preclinical only.
Pharmacology
Contents
WHAT IS VORINOSTAT?
Detailed overview
Vorinostat (SAHA, suberoylanilide hydroxamic acid) is a hydroxamic-acid histone deacetylase (HDAC) pan-inhibitor approved by the FDA in 2006 as Zolinza for cutaneous T-cell lymphoma. The molecule chelates the zinc ion in the catalytic pocket of HDAC enzymes, blocking their activity, so acetyl groups accumulate on histones, loosening DNA packaging and shifting gene expression. In neuroscience research this epigenetic reprogramming is of interest for memory consolidation, synaptic plasticity and neuroprotection: in rodent models vorinostat reversed learning and memory deficits and enhanced long-term potentiation. In humans, however, a neuroprotective benefit has never been demonstrated; brain penetration is poor, and as a prescription oncology drug it carries a serious side-effect profile.
Mechanism
HDAC pan-inhibitor (zinc chelation)
Half-life
Approximately 2 hours
Legal status
FDA-approved prescription cancer drug
Receptor profile
- Histone deacetylase (HDAC) enzymesStrong
- Gene transcription / chromatin remodelingStrong
- Memory and neuroprotection (research)Weak
Safety
Side effects, stop signs, contraindications
Side effects · 6
- Fatigue, nausea, diarrhea (common at clinical oncology doses)
- Reduced platelet and blood cell counts (thrombocytopenia, anemia)
- Increased tendency to blood clots (risk of pulmonary embolism and deep vein thrombosis)
- Fluctuating blood glucose (hyperglycemia)
- Prolongation of cardiac electrical conduction (QT prolongation)
- Dehydration, loss of appetite, taste disturbance
Contraindications · 5
- Pregnancy and breastfeeding: teratogenic and fetotoxic, strictly avoid
- History of thromboembolism (deep vein thrombosis, pulmonary embolism): increased clot risk
- QT prolongation or concurrent QT-prolonging drugs: arrhythmia risk
- Bone marrow suppression or low platelet count: requires regular blood-count monitoring
- Prescription oncology drug, only under medical supervision; not for self-medication
Related Nootropics
Same therapeutic category
Studies
Related research and clinical findings
Suberoylanilide Hydroxamic Acid (SAHA) Is a Driver Molecule of Neuroplasticity: Implication for Neurological Diseases
Epigenetic modifications by inhibiting histone deacetylases reverse memory impairment in insulin resistance induced cognitive deficit in mice
Suberoylanilide hydroxamic acid reversed cognitive and synaptic plasticity impairments induced by sevoflurane exposure in adult mice
Cognitive Improvement by Vorinostat through Modulation of Endoplasmic Reticulum Stress in a Corticosterone-Induced Chronic Stress Model in Mice
Repurposing Vorinostat for the Treatment of Disorders Affecting Brain
SAHA enhances synaptic function and plasticity in vitro but has limited brain availability in vivo and does not impact cognition
FAQ
FAQ
FDA-approved HDAC-inhibitor cancer drug; its neuroprotective effect is preclinical only.
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Structure & chemistry
The information here is strictly for educational and scientific purposes. It does not replace medical advice or clinical consultation, and it does not encourage illegal substance or pharmaceutical use. Data is sourced. When in doubt, consult your doctor.