Identification
- Summary
Stiripentol is an antiepileptic agent used in combination with other anticonvulsants to treat seizures associated with Dravet syndrome.
- Brand Names
- Diacomit
- Generic Name
- Stiripentol
- DrugBank Accession Number
- DB09118
- Background
Stiripentol is an antiepileptic agent that is an aromatic allylic alcohol drug, which makes it structurally unique from other antiepileptic drugs.2,6 The clinical development and marketing of stiripentol were first delayed due to the drug's potent inhibitory effects on hepatic cytochrome P450 (CYP) enzymes.6 However, its clinical efficacy as adjunctive therapy for epilepsies stems from its inhibitory action on CYP enzymes, as stiripentol reduces the degradation of CYP-sensitive antiepileptic drugs, hence boosting their therapeutic efficacy. Stiripentol may also exhibit direct anticonvulsant properties, although the exact mechanism of action is fully understood.1
Approved in the US, Canada, and Europe, stiripentol is used to treat seizures associated with Dravet syndrome.7,8,10 It is marketed under the brand name Diacomit.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Stiripentol (DB09118)
- Weight
- Average: 234.295
Monoisotopic: 234.12559444 - Chemical Formula
- C14H18O3
- Synonyms
- 1-(1,3-Benzodioxol-5-yl)-4,4-dimethyl-1-penten-3-ol
- 4,4-Dimethyl-1-((3,4-methylenedioxy)phenyl)-1-penten-3-ol
- Estiripentol
- Stiripentol
- Stiripentolum
- External IDs
- BCX 2600
- BCX-2600
- BRN 1313047
Pharmacology
- Indication
In the US, stiripentol is indicated for the treatment of seizures associated with Dravet syndrome in patients taking clobazam who are 6 months of age and older and weighing 7 kg or more. There are no clinical data to support the use of stiripentol as monotherapy in Dravet syndrome.8
In Europe and Canada, stiripentol is indicated for use as adjunctive therapy with clobazam and valproate to refractory generalized tonic-clonic seizures in patients with Dravet syndrome in infancy whose seizures are not adequately controlled with clobazam and valproate alone.7,10
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Used in combination to manage Seizures Regimen in combination with: Clobazam (DB00349) •••••••••••• •••• •••••• •• •• ••••• • •• Used as adjunct in combination to manage Refractory grand mal generalized tonic-clonic seizure Regimen in combination with: Clobazam (DB00349), Valproic acid (DB00313) •••••••••••• •••••••••• ••••••• •••• ••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Stiripentol is an antiepileptic agent that works to reduce seizure frequency. It demonstrates anticonvulsant properties when administered alone and may potentiate GABAergic inhibition via several proposed mechanisms.4 It provides a therapeutic advantage in improving the efficacy of other antiepileptic drugs by inhibiting cytochrome P450 enzymes that normally metabolize those drugs.8 The anticonvulsant activity of stiripentol is age-dependent, with increased efficacy in younger patients.4
- Mechanism of action
The mechanism by which stiripentol exerts its anticonvulsant effect in humans has not been fully elucidated. Possible mechanisms of action include direct effects mediated through the gamma-aminobutyric acid GABAA receptor and indirect effects involving inhibition of cytochrome P450 activity with a resulting increase in blood levels of clobazam and its active metabolite.8
Stiripentol is a positive allosteric modulator of GABAA receptors in the brain that enhances the opening duration of the channel by binding to a site different than the benzodiazepine binding site.1 It binds to GABAA receptors containing any of the α, β, γ, or δ-subunits but displays the most potent potency when bound to receptors containing α3 or δ subunits.4 Stiripentol also binds to GABAA receptor-dependent chloride channels via a barbiturate-like mechanism.5 Stiripentol potentiates GABA transmission by enhancing the release of GABA,1,2 reducing synaptosomal uptake of GABA,7 and inhibiting GABA transaminase-mediated breakdown of GABA.7
Stiripentol is an inhibitor of lactate dehydrogenase (LDH), which is involved in the energy metabolism of neurons and regulation of neuronal excitation. The drug binds to the site separate from the enzyme's lactate and pyruvate binding sites, thereby inhibiting both pyruvate-to-lactate conversion and lactate-to-pyruvate conversion.3 By inhibiting LDH, stiripentol may induce hyperpolarization, thereby reducing neuronal excitability.5 LDH inhibitors, including stiripentol, mimic a ketogenic diet, where the energy source in the brain is switched from glucose to mainly ketone bodies. The ketone bodies directly regulate neuronal excitation and seizures via ATP-sensitive potassium channels and vesicular glutamate transporters.3 Stiripentol is also suggested to exhibit neuroprotective properties, which may reduce injury caused by oxygen-glucose deprivation and glutamate excess.5
Target Actions Organism AGABA(A) Receptor agonistpositive allosteric modulatorHumans AL-lactate dehydrogenase A chain inhibitorHumans AL-lactate dehydrogenase B chain inhibitorHumans - Absorption
After oral administration, stiripentol is quickly and readily absorbed 2 with a median Tmax of two to three hours.8 The systemic exposure increases dose-proportionally.7 Stiripentol has a low bioavailability due to water insolubility and extensive metabolism.2
- Volume of distribution
The average volume of distribution is 1.03 L/kg but does not display a dose-dependent relationship. Following administration, stiripentol enters the brain and accumulates in the cerebellum and medulla.2
- Protein binding
Protein binding of stiripentol is 99%.8
- Metabolism
Stiripentol is extensively metabolized. About 13 different metabolites have been found in urine. The main metabolic processes are demethylenation (oxidative cleavage of the methylenedioxy ring system) and glucuronidation, although precise identification of the enzymes involved has not yet been achieved.7,10 Other metabolic pathways include O-methylation of catechol metabolites, hydroxylation of the t-butyl group, and conversion of the allylic alcohol side-chain to the isomeric 3-pentanone structure.2
In vitro studies suggested that the phase I metabolism of stiripentol is catalyzed by CYP1A2, CYP2C19 and CYP3A4 and possibly other enzymes.10
- Route of elimination
Stiripentol is mainly eliminated via metabolism.2 Its metabolites are excreted mainly via the kidney. Urinary metabolites of stiripentol accounted collectively for the majority (73%) of an oral acute dose whereas a further 13-24% was recovered in feces as unchanged drug.7
- Half-life
The elimination half life is approximately ranges from 4.5 to 13 hours, in a dose-dependent manner.8
- Clearance
Plasma clearance decreases markedly at high doses; it falls from approximately 40 L/kg/day at the dose of 600 mg/day to about 8 L/kg/day at the dose of 2,400 mg. Clearance is decreased after repeated administration of stiripentol, probably due to inhibition of the cytochrome P450 isoenzymes responsible for its metabolism.7
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
The oral LD50 in rats is >3 g/kg.9
There is limited clinical data on stiripentol overdose in humans. In mice, high doses of stiripentol (600 to 1800 mg/kg i.p.) caused decreased motor activity and respiration. Overdose should be managed with supportive and symptomatic treatment.8
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your software1,2-Benzodiazepine The metabolism of 1,2-Benzodiazepine can be decreased when combined with Stiripentol. Abacavir Abacavir may decrease the excretion rate of Stiripentol which could result in a higher serum level. Abametapir The serum concentration of Stiripentol can be increased when it is combined with Abametapir. Abatacept The metabolism of Stiripentol can be increased when combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be decreased when combined with Stiripentol. - Food Interactions
- Avoid excessive or chronic alcohol consumption. Ingesting alcohol may increase the risk of sedation and somnolence that can be caused by stiripentol.
- Avoid milk and dairy products. These products may interfere with the absorption of stiripentol.
- Limit caffeine intake. Stiripentol may attenuate CYP1A2-mediated metabolism of caffeine.
- Take with a full glass of water. Oral capsules should be swallowed whole with a glass of water during a meal and oral suspension should be mixed in a glass of water and should be taken immediately after mixing during a meal.
- Take with food. Stiripentol degrades rapidly in an acidic environment.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Diacomit Capsule 250 mg Oral Biocodex 2016-09-07 Not applicable EU 
Diacomit Powder, for suspension 500 mg / sachet Oral Biocodex Sa 2013-05-01 Not applicable Canada 
Diacomit Capsule 250 mg Oral Biocodex Sa 2013-05-01 Not applicable Canada Diacomit Capsule 500 mg/1 Oral BIOCODEX, INC. 2018-08-21 Not applicable US 
Diacomit Powder, for suspension 500 mg Oral Biocodex 2016-09-07 Not applicable EU
Categories
- ATC Codes
- N03AX17 — Stiripentol
- Drug Categories
- Anticonvulsants
- BCRP/ABCG2 Inhibitors
- Central Nervous System Agents
- Central Nervous System Depressants
- Cytochrome P-450 CYP1A2 Inducers
- Cytochrome P-450 CYP1A2 Inducers (strength unknown)
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2B6 Inhibitors
- Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C19 Inhibitors
- Cytochrome P-450 CYP2C19 Inhibitors (strong)
- Cytochrome P-450 CYP2C19 Substrates
- Cytochrome P-450 CYP2C8 Inhibitors
- Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2D6 Inhibitors
- Cytochrome P-450 CYP2D6 Inhibitors (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (strong)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Dioxoles
- Drugs causing inadvertant photosensitivity
- Drugs that are Mainly Renally Excreted
- Miscellaneous Anticonvulsants
- Nervous System
- P-glycoprotein inhibitors
- Photosensitizing Agents
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as benzodioxoles. These are organic compounds containing a benzene ring fused to either isomers of dioxole. Dioxole is a five-membered unsaturated ring of two oxygen atoms and three carbon atoms.
- Kingdom
- Organic compounds
- Super Class
- Organoheterocyclic compounds
- Class
- Benzodioxoles
- Sub Class
- Not Available
- Direct Parent
- Benzodioxoles
- Alternative Parents
- Styrenes / Secondary alcohols / Oxacyclic compounds / Acetals / Hydrocarbon derivatives
- Substituents
- Acetal / Alcohol / Aromatic heteropolycyclic compound / Benzenoid / Benzodioxole / Hydrocarbon derivative / Organic oxygen compound / Organooxygen compound / Oxacycle / Secondary alcohol
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- R02XOT8V8I
- CAS number
- 49763-96-4
- InChI Key
- IBLNKMRFIPWSOY-FNORWQNLSA-N
- InChI
- InChI=1S/C14H18O3/c1-14(2,3)13(15)7-5-10-4-6-11-12(8-10)17-9-16-11/h4-8,13,15H,9H2,1-3H3/b7-5+
- IUPAC Name
- (1E)-1-(2H-1,3-benzodioxol-5-yl)-4,4-dimethylpent-1-en-3-ol
- SMILES
- CC(C)(C)C(O)\C=C\C1=CC2=C(OCO2)C=C1
References
- General References
- Quilichini PP, Chiron C, Ben-Ari Y, Gozlan H: Stiripentol, a putative antiepileptic drug, enhances the duration of opening of GABA-A receptor channels. Epilepsia. 2006 Apr;47(4):704-16. [Article]
- Trojnar MK, Wojtal K, Trojnar MP, Czuczwar SJ: Stiripentol. A novel antiepileptic drug. Pharmacol Rep. 2005 Mar-Apr;57(2):154-60. [Article]
- Sada N, Lee S, Katsu T, Otsuki T, Inoue T: Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy. Science. 2015 Mar 20;347(6228):1362-7. doi: 10.1126/science.aaa1299. [Article]
- Grosenbaugh DK, Mott DD: Stiripentol in refractory status epilepticus. Epilepsia. 2013 Sep;54 Suppl 6:103-5. doi: 10.1111/epi.12291. [Article]
- Frampton JE: Stiripentol: A Review in Dravet Syndrome. Drugs. 2019 Nov;79(16):1785-1796. doi: 10.1007/s40265-019-01204-y. [Article]
- Chiron C: Stiripentol. Neurotherapeutics. 2007 Jan;4(1):123-5. doi: 10.1016/j.nurt.2006.10.001. [Article]
- EMA Approved Drug Products: DIACOMIT (stiripentol) Oral Capsules [Link]
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
- Cayman Chemical: Stiripentol MSDS [Link]
- Health Canada Approved Drug Products: DIACOMIT (stiripentol) Oral Capsules or Powder for suspension [Link]
- External Links
- PubChem Compound
- 5311454
- PubChem Substance
- 310265035
- ChemSpider
- 4470940
- BindingDB
- 50504273
- 2054968
- ChEMBL
- CHEMBL1983350
- Wikipedia
- Stiripentol
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Recruiting Treatment Pharmacoresistant Focal Epilepsies 1 4 Unknown Status Treatment Epilepsy 1 2 Completed Treatment Primary Hyperoxaluria 1 1 Completed Basic Science Healthy Subjects (HS) 1 1 Not Yet Recruiting Other Renal Insufficiency,Chronic 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Capsule Oral 100 MG Capsule Oral 250 mg/1 Capsule Oral 250 mg Capsule Oral 500 mg/1 Capsule Oral 500 mg Powder, for suspension Oral 250 MG Powder, for suspension Oral 250 mg/1 Powder, for suspension Oral 250 mg / sachet Powder, for suspension Oral 500 mg/1 Powder, for suspension Oral 500 mg / sachet Powder, for suspension Oral 500 MG - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 73-74 https://www.trc-canada.com/prod-img/MSDS/S686825MSDS.pdf logP 2.94 https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/206709s003;207223s003lbl.pdf pKa 14.2 https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/206709s003;207223s003lbl.pdf - Predicted Properties
Property Value Source Water Solubility 0.405 mg/mL ALOGPS logP 3.01 ALOGPS logP 3.12 Chemaxon logS -2.8 ALOGPS pKa (Strongest Acidic) 14.34 Chemaxon pKa (Strongest Basic) -3.1 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 38.69 Å2 Chemaxon Rotatable Bond Count 3 Chemaxon Refractivity 66.77 m3·mol-1 Chemaxon Polarizability 26.21 Å3 Chemaxon Number of Rings 2 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-014i-0090000000-68ca0cd1edbcd2f614bb Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-0090000000-7192276f09710813e11c Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-00m0-2290000000-13eed9f691c004e5daf0 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0910000000-c36dbaa65f726e65e6b9 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-014i-2910000000-35414f9546df540d4bd3 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0r0c-3920000000-a16fe2a7d43c397f8a6f Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 158.44931 predictedDeepCCS 1.0 (2019) [M+H]+ 160.80733 predictedDeepCCS 1.0 (2019) [M+Na]+ 166.90047 predictedDeepCCS 1.0 (2019)
Targets
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- AgonistPositive allosteric modulator
- General Function
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine...
Components:
References
- Fisher JL: The anti-convulsant stiripentol acts directly on the GABA(A) receptor as a positive allosteric modulator. Neuropharmacology. 2009 Jan;56(1):190-7. doi: 10.1016/j.neuropharm.2008.06.004. Epub 2008 Jun 10. [Article]
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Nad binding
- Specific Function
- Not Available
- Gene Name
- LDHA
- Uniprot ID
- P00338
- Uniprot Name
- L-lactate dehydrogenase A chain
- Molecular Weight
- 36688.465 Da
References
- Sada N, Lee S, Katsu T, Otsuki T, Inoue T: Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy. Science. 2015 Mar 20;347(6228):1362-7. doi: 10.1126/science.aaa1299. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Nad binding
- Specific Function
- Not Available
- Gene Name
- LDHB
- Uniprot ID
- P07195
- Uniprot Name
- L-lactate dehydrogenase B chain
- Molecular Weight
- 36638.225 Da
References
- Sada N, Lee S, Katsu T, Otsuki T, Inoue T: Epilepsy treatment. Targeting LDH enzymes with a stiripentol analog to treat epilepsy. Science. 2015 Mar 20;347(6228):1362-7. doi: 10.1126/science.aaa1299. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55930.545 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
- Gene Name
- CYP2D6
- Uniprot ID
- P10635
- Uniprot Name
- Cytochrome P450 2D6
- Molecular Weight
- 55768.94 Da
References
- EMA Approved Drug Products: DIACOMIT (stiripentol) Oral Capsules [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitorInducer
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitorInducer
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- Tran A, Rey E, Pons G, Rousseau M, d'Athis P, Olive G, Mather GG, Bishop FE, Wurden CJ, Labroo R, Trager WF, Kunze KL, Thummel KE, Vincent JC, Gillardin JM, Lepage F, Levy RH: Influence of stiripentol on cytochrome P450-mediated metabolic pathways in humans: in vitro and in vivo comparison and calculation of in vivo inhibition constants. Clin Pharmacol Ther. 1997 Nov;62(5):490-504. doi: 10.1016/S0009-9236(97)90044-8. [Article]
- Chiron C: Stiripentol. Expert Opin Investig Drugs. 2005 Jul;14(7):905-11. doi: 10.1517/13543784.14.7.905 . [Article]
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Trojnar MK, Wojtal K, Trojnar MP, Czuczwar SJ: Stiripentol. A novel antiepileptic drug. Pharmacol Rep. 2005 Mar-Apr;57(2):154-60. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- InhibitorInducer
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Steroid hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
- Gene Name
- ABCG2
- Uniprot ID
- Q9UNQ0
- Uniprot Name
- ATP-binding cassette sub-family G member 2
- Molecular Weight
- 72313.47 Da
References
- FDA Approved Drug Products: DIACOMIT (stiripentol) suspension or capsules, for oral use [Link]
Drug created at September 22, 2015 19:59 / Updated at February 20, 2024 23:55