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Synonyms: A-44090 | Depakote® | Epilim® | valproate sodium
valproic acid is an approved drug (FDA (1978))
Compound class: Synthetic organic
Comment: Valproic acid is a fatty acid with anticonvulsant properties. It is commonly administered in a salt preparation, valproate sodium.
Ligand Activity Visualisation Charts
These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.✖
View more information in the IUPHAR Pharmacology Education Project: valproic acid
|No information available.
|Summary of Clinical Use
|Valproic acid is currently approved for the treatment of various seizure disorders, manic episodes of bipolar disorder and migraine headache. Valproic acid is, in addition, a histone deacetylase (HDAC) inhibitor and is being investigated as a treatment for HIV infection and various cancers.
|Mechanism Of Action and Pharmacodynamic Effects
|Inhibition of succinic semi-aldehyde dehydrogenase (ALDH5A1) may contribute to the elevated levels of cerebral and cerebellar GABA observed as a result of valproic acid administration (in animal models). ALDH5A1 is a GABA degradative enzyme. Increased levels of GABA cause neuro-inhibition and may be mechanistically linked to the drug's anticonvulsant and mood-stabilising effects. However, we have been unable to find affinity data for this drug to substantiate this proposed MMOA.
Valproic acid is also an inhibitor of Class I and II HDACs. In relation to HIV infection and the potential antiviral effects of valproic acid, HDAC1 is required for persistence of HIV in infected cells.
For extended ADME data see the following:
Electronic Medicines Compendium (eMC)