Valproic Acid
Small molecule targets GSK3B, UGT2B7 via inhibition
Regulatory milestones approvals, filings & regulatory actions · 1 recorded
| Milestone | Jurisdiction | Brand | Indication | Date | Sentence it was read from |
|---|---|---|---|---|---|
| Approved | US (FDA) | DEPAKENE | — | 1978-02-28 | fda.gov ↗ |
Trials 110 · started per year
Also used as a comparator or background therapy in 23 trials
| Phase | Registry id | Dates | Indication | Sponsor | Status | Outcome |
|---|---|---|---|---|---|---|
| Phase 13 trials | ||||||
| Phase 1 | NCT03885947 Background | Feb 2019 → Mar 2021 | Hodgkins lymphoma, acute lymphoblastic leukemia, myelodysplastic syndrome | Alla Keyzner | Completed | No outcome recorded |
| Phase 1 | NCT02761291 Background | May 2016 → Jun 2017 | nasopharyngeal carcinoma | Chang Gung Memorial Hospital | Unknown | No outcome recorded |
| Phase 1 | NCT00530907 Background | Jun 2007 → Nov 2013 | — | M.D. Anderson Cancer Center | Completed | No outcome recorded |
| Phase 1/23 trials | ||||||
| Phase 1/2 | NCT06199557 Comparator | May 2024 → Nov 2025 overdue | acute myeloid leukemia, myelodysplastic syndrome | Haukeland University Hospital | Recruiting | No outcome recorded |
| Phase 1/2 | NCT04729543 Background | Oct 2020 → Dec 2024 overdue | uveal melanoma | Erasmus Medical Center | Recruiting | No outcome recorded |
| Phase 1/2 | NCT01898104 Comparator | May 2012 → Nov 2023 | colorectal cancer | National Cancer Institute, Naples | Unknown | No outcome recorded |
| Phase 26 trials | ||||||
| Phase 2 | NCT03885154 Comparator | Oct 2017 → Mar 2019 | migraine disorder | Kimberly S Jones | Terminated | No outcome recorded |
| Phase 2 | NCT01674010 Background | Aug 2012 → Jun 2014 | bipolar I disorder | OPKO Health, Inc. | Terminated | No outcome recorded |
| Phase 2 | NCT01399515 Comparator | Mar 2011 → Aug 2013 | retinitis pigmentosa | Seoul National University Hospital | Completed | No outcome recorded |
| Phase 2 | NCT01233609 Comparator | Nov 2010 → Dec 2015 | retinitis pigmentosa | Foundation Fighting Blindness | Completed | No outcome recorded |
| Phase 2 | NCT00481013 Comparator | Jul 2007 → Dec 2009 | spinal muscular atrophy | University of Utah | Completed | No outcome recorded |
| Phase 2 | NCT00382590 Comparator | Aug 2005 → Feb 2008 | acute myeloid leukemia, myelodysplastic syndrome | M.D. Anderson Cancer Center | Completed | No outcome recorded |
| Phase 34 trials | ||||||
| Phase 3 | NCT06248931 Comparator | May 2022 → Jun 2024 | migraine disorder | Kafrelsheikh University | Completed | No outcome recorded |
| Phase 3 | NCT01960075 Comparator | Oct 2015 → Feb 2019 | — | University of Virginia | Completed | No outcome recorded |
| Phase 3 | NCT01586208 Comparator | Jan 2010 → May 2012 | epilepsy with generalized tonic-clonic seizures | Hospital Universitari de Bellvitge | Completed | No outcome recorded |
| Phase 3 | NCT00088452 Comparator | Jul 2004 → Jan 2013 | childhood absence epilepsy | Children's Hospital Medical Center, Cincinnati | Completed | No outcome recorded |
| Phase 47 trials | ||||||
| Phase 4 | NCT07047651 Background | Jun 2025 → Dec 2027 expected | treatment-refractory schizophrenia | Dr. Stavroula Rakitzi | Active not recruiting | No outcome recorded |
| Phase 4 | NCT06485726 Comparator | Jan 2023 → Jul 2024 overdue | migraine disorder | Kafrelsheikh University | Recruiting | No outcome recorded |
| Phase 4 | NCT03048084 Comparator | Feb 2018 → Jul 2026 overdue | glioma | Leiden University Medical Center | Recruiting | No outcome recorded |
| Phase 4 | NCT02670161 Comparator | May 2016 → Dec 2026 expected | Parkinson disease, brain neoplasm, cognitive impairment with or without cerebellar ataxia, epilepsy +6 | Endeavor Health | Enrolling by invitation | No outcome recorded |
| Phase 4 | NCT02870283 Comparator | May 2010 → Nov 2014 | bipolar disorder | Federal University of Rio Grande do Sul | Completed | No outcome recorded |
| Phase 4 | NCT00976794 Comparator | Jan 2009 → Jun 2012 | bipolar I disorder | University of Sao Paulo | Completed | No outcome recorded |
| Phase 4 | NCT01115959 Comparator | Feb 2003 → Oct 2008 | intracerebral hemorrhage | Wolfson Medical Center | Completed | No outcome recorded |
Evidence & citations 23 cited values
Every value below carries the sentence it was read from. 146 sources stand behind the page.
| Field | Value | Cited text |
|---|---|---|
| Known as | VALPROIC acid | “In recent years, a number of preclinical studies have found that valproic acid has a potential neuroprotective effect in acute ischemic brain injury, which can decrease infarct...” NCT06020898 ↗131“Valproic acid: Starting at 500mg daily, dose weekly adjusted according to blood serum level (50 and 125µg/ml), efficacy and tolerability.” NCT00976794 ↗ “Combination of Valproic Acid and Lenalidomide in the Treatment of Patients With Myelodysplastic Syndrome With Favorable Risk Profile” NCT00977132 ↗ “Drugs: carbamazepine, lamotrigine, levetiracetam, oxcarbazepine, phenobarbital, phenytoin, topiramate, valproic acid, zonisamide” NCT05236166 ↗ “Valproic acid with 1000mg loading dose with 500mg q12 4 hours later to maintain a trough level above 75ug/ml” NCT02848105 ↗ “5-azacytidine (Vidaza®) + Valproic Acid (Depakine ®) Before Administration of Retinoic Acid (Vesanoid®)” NCT00339196 ↗ “Option 2: valproic acid bolus 10-20 mg/kg in 30 min, followed by15 mg/kg/day in 2 dosages intravenously” NCT02056236 ↗ “carbamazepine, valproic acid, topiramate, oxcarbazepine, levetiracetam or lamotrigine” NCT02429596 ↗ “as well as the plasma levels of hydralazine and valproic acid.” NCT00395655 ↗ “brain tumors (lamotrigine, levetiracetam, valproic acid)” NCT02670161 ↗ “Valproic Acid (VPA) expanded cord blood stem cells” NCT03885947 ↗ “valproic acid (VAL, a UGT2B7 inhibiting drug)” NCT03512860 ↗ “another drug called Valproic Acid (VPA)” NCT01010854 ↗ “Valproic acid (VP)” NCT04729543 ↗ “valproic acid” NCT01356875 ↗ |
| Known as | 2-propylpentanoic acid | “Valproic acid (VPA, 2-propylpentanoic acid) is an established drug in the long-term therapy of epilepsy.” NCT00439673 ↗ |
| Known as | Depakine | “The combination of pharmacotherapy (anxiolytics (Tavor, clonotril, lexotanil) antidepressants (SSRI, SNRI), mood stabilizers (lithium, depakine), antipsychotics (clozapine and...” NCT06993662 ↗2“5-azacytidine (Vidaza®) + Valproic Acid (Depakine ®) Before Administration of Retinoic Acid (Vesanoid®)” NCT00339196 ↗ |
| Known as | Depakine-Chrono | “Valproic Acid (Depakine-Chrono®) (VPA) will be administered concomitantly for a minimum of 6 cycles.” NCT01342692 ↗ |
| Known as | Depakote | “The purpose of this research study is to test the safety, tolerability, and effectiveness of the combination of three drugs, sorafenib (Nexavar®), valproic acid (Depakote®),...” NCT01817751 ↗1“Valproic Acid (Depakote[Registered Trademark]) to Treat Autoimmune Lymphoproliferative Syndrome (ALPS)” NCT00605657 ↗ |
| Known as | Depakote (Valproic Acid) | “Depakote (Valproic Acid)” NCT00996060 ↗ |
| Known as | Depakote ER | “Patients with plasma HIV RNA<50 c/mL added sustained-release VPA (Depakote ER) twice daily, RAL 400 mg twice daily, or ENF 90 mcg twice daily.” PMID 20186346 ↗ Feb 20101“Valproic Acid (Depakote ER) in Patients With Advanced Thyroid Cancer” NCT00525135 ↗ |
| Known as | Epival | “The purpose of this study is to examine whether the co-administration of valproic acid (Epival®), with highly active antiretroviral therapy (HAART) can reduce the size of HIV...” NCT00289952 ↗ |
| Known as | Ergenyl | “E.g. Valproat-neuraxpharm®, Valproat-neuraxpharm® Lösung, Ergenyl®, Ergenyl®-Lösung oder Orfiril® Saft (Valproic acid);” NCT03243461 ↗ |
| Known as | Ergenyl-Lösung | “E.g. Valproat-neuraxpharm®, Valproat-neuraxpharm® Lösung, Ergenyl®, Ergenyl®-Lösung oder Orfiril® Saft (Valproic acid);” NCT03243461 ↗ |
| Known as | Orfiril Saft | “E.g. Valproat-neuraxpharm®, Valproat-neuraxpharm® Lösung, Ergenyl®, Ergenyl®-Lösung oder Orfiril® Saft (Valproic acid);” NCT03243461 ↗ |
| Known as | Sodium valproate or valproic acid (Depakote) | “Sodium valproate or valproic acid (Depakote)” NCT00563992 ↗ |
| Known as | VAL | “valproic acid (VAL, a UGT2B7 inhibiting drug)” NCT03512860 ↗ |
| Known as | Valproat-neuraxpharm | “E.g. Valproat-neuraxpharm®, Valproat-neuraxpharm® Lösung, Ergenyl®, Ergenyl®-Lösung oder Orfiril® Saft (Valproic acid);” NCT03243461 ↗ |
| Known as | Valproat-neuraxpharm Lösung | “E.g. Valproat-neuraxpharm®, Valproat-neuraxpharm® Lösung, Ergenyl®, Ergenyl®-Lösung oder Orfiril® Saft (Valproic acid);” NCT03243461 ↗ |
| Known as | valproate | “We used valproate (VPA), a histone deacetylase inhibitor that has been used for decades as a chronic, safe treatment for epileptic disorders.” PMID 17717136 ↗ Aug 2007 |
| Known as | Valproic acid (VP) | “Valproic acid (VP)” NCT04729543 ↗ |
| Known as | Valproic acid (VPA) (depakote) | “Valproic acid (VPA) (depakote)” NCT00614458 ↗ |
| Known as | VPA | “The objectives of this study are to evaluate the efficacy of Valproic Acid (VPA) to both slow the progression of visual function loss and/or to restore visual function in...” NCT01233609 ↗36“Owing to its HDACi activity and its safe use for epileptic disorders, valproic acid (VPA) is a good candidate for anticancer therapy that we have largely explored preclinically...” PMID 32849914 ↗ Aug 2020 “Valproic acid (VPA), a branched short-chain fatty acid, is widely used in clinical as an antiepileptic drug and a mood stabilizer, primarily in the treatment of epilepsy,...” NCT02761291 ↗ “PURPOSE: To study the efficacy and tolerability of valproic acid (VPA) and radiation, followed by VPA and bevacizumab in children with newly diagnosed diffuse intrinsic pontine...” PMID 32285998 ↗ Apr 2020 “We conducted a phase 1/2 study of the combination of 5-aza-2'-deoxycytidine (decitabine) and the histone deacetylase inhibitor valproic acid (VPA) in patients with advanced...” PMID 16882711 ↗ Aug 2006 “histone deacetylase (HDAC) inhibitor valproic acid (VPA; Barker et al. 2013; Wolff et al. 2008, 2011; Felix et al. 2011; Su et al. 2011; Rokes et al. 2010; Masoudi et al. 2008;...” NCT03243461 ↗ “Due to its histone deacetylase (HDAC) inhibiting activity and its safe use as a chronic therapy for epileptic disorders, valproic acid (VPA) has been considered a good...” PMID 27884140 ↗ Nov 2016 “Conflicting results have been reported regarding the ability of valproic acid (VPA) to reduce the size of HIV reservoirs in patients receiving suppressive highly active...” PMID 22276680 ↗ Jan 2012 “The trial investigates the use of VPA (Valproic Acid) for the treatment of adult patients with biopsy proven idiopathic focal segmentel glomerulosclerosis (FSGS) or minimal...” NCT02896270 ↗ “Valproic acid (VPA) is a generic low-cost anticonvulsant and mood stabilizer with HDAC inhibitory activity, and anticancer properties also demonstrated in PDAC models.” PMID 39300376 ↗ Sep 2024 “Fosphenytoin (FOS) and its active form, phenytoin (PHT), levetiracetam (LEV), and valproic acid (VPA) are commonly used second-line treatments of status epilepticus.” PMID 33336359 ↗ Jan 2021 “The purpose of this study is to investigate the efficacy of valproic acid (VPA), an HDAC inhibitor, in treating HIV infected adults using anti-HIV drugs.” NCT00312546 ↗ “Valproic Acid (VPA) has long been used to treat neurological disorders; however, recent work has demonstrated its potential as a neuroprotective agent.” PMID 41420823 ↗ Dec 2025 “We used valproate (VPA), a histone deacetylase inhibitor that has been used for decades as a chronic, safe treatment for epileptic disorders.” PMID 17717136 ↗ Aug 2007 “Valproic acid (VPA) is an inhibitor of histone deacetylase (HDAC) used as an anticonvulsant and mood-stabilizing drug for decades.” NCT01295593 ↗ “An initial dose of Valproic Acid (VPA) will be given IV at 20mg/kg, followed by continuous infusion of 1mg/kg/hour for 24 hours.” NCT03885154 ↗ “AML cells from patients before and after treatment with valproic acid (VPA), all-trans retinoic acid (ATRA) and theophylline.” PMID 33917201 ↗ Apr 2021 “valproic acid (VPA) as histone deacetylase inhibitor can inhibit CD4+ Th1 and Th17 cells and control the aGVDH in mice model” NCT02848105 ↗ “To evaluate the ability to induce serum folate receptor (FR) with dexamethasone (Dex) and valproic acid (VPA) treatment” NCT02520115 ↗ “All participants will be treated with valproic acid (VPA) at a starting dose of 15 mg/kg/day orally in divided doses.” NCT00524667 ↗ “oral valproic acid (VPA) twice daily until a target serum trough VPA concentration range is maintained for 28 days.” NCT00107458 ↗ “Study of Safety and Dosing Effect on SMN Levels of Valproic Acid (VPA) in Patients With Spinal Muscular Atrophy” NCT00374075 ↗ “Valproic acid (VPA, 2-propylpentanoic acid) is an established drug in the long-term therapy of epilepsy.” NCT00439673 ↗ “Valproic Acid (VPA, 12.5 mg/kg) once per day and Avelumab (10 mg/kg IV) every 2 weeks for up to 2 years.” NCT03357757 ↗ “Valproic acid (VPA) is a medicine that has been used for many years to treat patients with epilepsy.” NCT00661453 ↗ “Valproic Acid (Depakine-Chrono®) (VPA) will be administered concomitantly for a minimum of 6 cycles.” NCT01342692 ↗ “We evaluated the effectiveness of valproic acid (VPA) to treat CBHS and predictors of improvement.” PMID 32969724 ↗ Nov 2020 “The purpose of this study is to find out if a drug called valproic acid (VPA) will protect organs” NCT04531579 ↗ “Valproic acid (VPA) has been used clinically as an anticonvulsant and mood-stabilizing drug.” NCT06199557 ↗ “Valproic acid (VPA) is an anti-epileptic drug with HDACi and anticancer activity.” PMID 25421252 ↗ Nov 2014 “a drug called valproic acid (VPA) will protect organs” NCT04531592 ↗ “another drug called Valproic Acid (VPA)” NCT01010854 ↗ “Valproic Acid (VPA)” NCT01900730 ↗ “Valproic Acid (VPA)” NCT00481013 ↗ “Valproic acid (VPA)” NCT00326170 ↗ “Valproic Acid (VPA)” NCT06714357 ↗ “valproic acid (VPA)” NCT01586208 ↗ |
| Action | Inhibit | “the histone deacetylase inhibitor valproic acid (VPA)” PMID 16882711 ↗ Aug 2006 |
| Modality | Small molecule | “Valproic acid is a short chained fatty acid” NCT00339196 ↗ |
| Route | Oral | “valproic acid (lowest dose in the first 5 patients and a higher dose in patients 6 and 7) orally every 8 hours” NCT00000629 ↗ |
| Target | GSK3B | “valproic acid was able to inhibit the activity of GSK3b” NCT00385710 ↗ |