Eslicarbazepine acetate

Identification

Summary

Eslicarbazepine acetate is an anticonvulsant agent used as an adjunct to treat partial-onset seizures in patients with inadequate clinical response to conventional antiepileptic therapy.

Brand Names
Aptiom, Zebinix
Generic Name
Eslicarbazepine acetate
DrugBank Accession Number
DB09119
Background

Eslicarbazepine acetate (ESL) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy. Eslicarbazepine acetate is a prodrug that is rapidly converted to eslicarbazepine, the primary active metabolite in the body. Eslicarbazepine's mechanism of action is not well understood, but it is known that it does exert anticonvulsant activity by inhibiting repeated neuronal firing and stabilizing the inactivated state of voltage-gated sodium channels, thus preventing their return to the activated state during which seizure activity can occur.

Eslicarbazepine acetate is marketed as Aptiom in North America and Zebinix or Exalief in Europe. It is available in 200, 400, 600, or 800mg tablets that are taken once daily, with or without food. Eslicarbazepine acetate is associated with numerous side effects including dizziness, drowsiness, nausea, vomiting, diarrhea, headache, aphasia, lack of concentration, psychomotor retardation, speech disturbances, ataxia, depression and hyponatremia. It is recommended that patients taking eslicarbazepine acetate be monitored for suicidality.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 296.326
Monoisotopic: 296.116092383
Chemical Formula
C17H16N2O3
Synonyms
  • (10S)-10-acetoxy-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide
  • (10S)-5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl acetate
  • ESL
  • Eslicarbazepine acetate
External IDs
  • BIA 2-093
  • BIA-2-093
  • BIA2-093
  • SEP 0002093
  • SEP-0002093
  • SEP0002093

Pharmacology

Indication

Eslicarbazepine acetate is indicated for the treatment of partial-onset seizures in patients 4 years of age and older.13

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofPartial-onset seizures••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Eslicarbazepine acetate is associated with a dose- and concentration-dependant increase in heart rate and prolongation of PR interval.

Mechanism of action

Eslicarbazepine acetate is converted to the active metabolite eslicarbazepine which carries out its anticonvulsant activity. The exact mechanism of action is unknown, but it is thought to involve the inhibition of voltage-gated sodium channels. In in vitro electrophysiological studies, eslicarbazepine was shown to inhibit repeated neuronal firing by stabilizing the inactivated state of voltage-gated sodium channels and preventing their return to the activated state. In vitro studies also showed eslicarbazepine inhibiting T-type calcium channels, which likely also has a role in anticonvulsant activity.

TargetActionsOrganism
AP2X purinoceptor 4
antagonist
Humans
Absorption

Eslicarbazepine active metabolite has a high bioavailability and reaches peak serum concentration 1-4 hours after a given dose. Eslicarbazepine acetate absorption is not affected by food.

Volume of distribution

The apparent volume of distribution of eslicarbazepine is 61.3 L for a body weight of 70 kg based on population PK analysis.

Protein binding

Eslicarbazepine is bound to plasma proteins at a relatively low rate of <40%, independent of concentration. In vitro studies have shown that plasma protein binding is not relevantly affected by the presence of other medications such as warfarin, diazepam, digoxin, phenytoin or tolbutamide. Similarly, the binding of these medications was not significantly affected by the presence of eslicarbazepine.

Metabolism

Eslicarbazepine acetate is rapidly and extensively metabolized to its major active metabolite, eslicarbazepine, via hydrolytic first-pass metabolism. Eslicarbazepine corresponds to about 92% of systemic exposure. Minor active metabolites (R)-licarbazepine and oxcarbazepine consist of <5% of systemic exposure. Active metabolites are then metabolized to inactive glucuronides that correspond to about 3% of systemic exposure.

Eslicarbazepine had a moderate inhibitory effect on CYP2C19 and a mild activation of UGT1A1-mediated glucuronidation when studied in human hepatic microsomes. It has been shown to induce CYP3A4 enzymes in vivo.

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Route of elimination

Eslicarbazepine acetate and its metabolites are eliminated primarily via renal excretion. Eslicarbazepine active metabolite is excreted two-thirds in the unchanged form and one-third as a glucuronide conjugate. This accounts for around 90% of total metabolites excreted, with the remaining 10% being minor metabolites. Renal tubular reabsorption is expected to occur with eslicarbazepine.

Half-life

The apparent plasma half-life of eslicarbazepine is 10-20 hours in healthy subjects and 13-20 hours in epilepsy patients. Steady-state plasma concentrations are attained after 4 to 5 days of once daily dosing.

Clearance

Renal clearance of eslicarbazepine was found to be approximately 20 mL/min in healthy subjects with normal renal function.

Adverse Effects
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Toxicity

There are no adequate and well-controlled studies of the use of eslicarbazepine acetate in pregnant women. In studies conducted in pregnant mice, rats, and rabbits, eslicarbazepine acetate did show developmental toxicities, including teratogenicity, embryolethality, and fetal growth retardation, at clinically relevant doses. Drug-induced liver injury ranging from mild to moderate elevations in transaminases (>3 times the upper limit of normal) to rare cases with concomitant elevations of total bilirubin (>2 times the upper limit of normal) have been reported with the use of eslicarbazepine. Overdose with eslicarbazepine acetate appears similar to its known adverse reactions and includes symptoms of hyponatremia, dizziness, nausea, vomiting, somnolence, euphoria, oral paraesthesias, ataxia, and diplopia. There is no specific antidote for eslicarbazepine acetate overdose and it should be treated primarily with supportive measures. If required, the drug may be removed by gastric lavage, partially by hemodialysis or inactivated with activated charcoal.

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
1,2-BenzodiazepineThe risk or severity of CNS depression can be increased when Eslicarbazepine acetate is combined with 1,2-Benzodiazepine.
AbemaciclibThe metabolism of Abemaciclib can be increased when combined with Eslicarbazepine acetate.
AbrocitinibThe metabolism of Abrocitinib can be decreased when combined with Eslicarbazepine acetate.
AcalabrutinibThe metabolism of Acalabrutinib can be increased when combined with Eslicarbazepine acetate.
AcenocoumarolThe metabolism of Acenocoumarol can be increased when combined with Eslicarbazepine acetate.
Food Interactions
  • Take with or without food.

Products

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Active Moieties
NameKindUNIICASInChI Key
EslicarbazepineprodrugS5VXA428R4104746-04-5BMPDWHIDQYTSHX-AWEZNQCLSA-N
International/Other Brands
Eksaliyef (Bial-Portela & Ca. S.A.) / Erelib (Bial-Portela & Ca. S.A.) / Eslicar (Emcure Pharmaceuticals Ltd) / Eslify (Torrent Pharmaceuticals Ltd) / Eslistar (Lupin Ltd) / Eslizen (Intas Pharmaceuticals Ltd) / Exalief (Bial-Portela & Ca. S.A.) / Normictal (Abbott India Ltd) / Stedesa / Zefretol (Sun Pharma Laboratories Ltd)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AptiomTablet400 mg/1OralSumitomo Pharma America, Inc.2014-04-07Not applicableUS flag
AptiomTablet600 mgOralSunovion2014-08-07Not applicableCanada flag
AptiomTablet800 mg/1OralSumitomo Pharma America, Inc.2014-04-07Not applicableUS flag
AptiomTablet200 mg/1OralSumitomo Pharma America, Inc.2014-04-07Not applicableUS flag
AptiomTablet400 mgOralSunovion2014-08-07Not applicableCanada flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Eslicarbazepine acetateTablet400 mg/1OralCamber Pharmaceuticals, Inc.2023-08-03Not applicableUS flag
Eslicarbazepine acetateTablet800 mg/1OralCamber Pharmaceuticals, Inc.2023-08-03Not applicableUS flag
Eslicarbazepine acetateTablet200 mg/1OralCamber Pharmaceuticals, Inc.2023-08-03Not applicableUS flag
Eslicarbazepine acetateTablet600 mg/1OralCamber Pharmaceuticals, Inc.2023-08-03Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
AptiomEslicarbazepine acetate (400 mg/1) + Eslicarbazepine acetate (800 mg/1)KitOralSumitomo Pharma America, Inc.2014-04-07Not applicableUS flag
AptiomEslicarbazepine acetate (400 mg/1) + Eslicarbazepine acetate (800 mg/1)KitOralSumitomo Pharma America, Inc.2014-04-07Not applicableUS flag

Categories

Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as dibenzazepines. These are compounds with two benzene rings connected by an azepine ring. Azepine is an unsaturated seven-member heterocycle with one nitrogen atom replacing a carbon atom.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Benzazepines
Sub Class
Dibenzazepines
Direct Parent
Dibenzazepines
Alternative Parents
Azepines / Benzenoids / Ureas / Carboxylic acid esters / Monocarboxylic acids and derivatives / Azacyclic compounds / Organopnictogen compounds / Organonitrogen compounds / Organic oxides / Hydrocarbon derivatives
show 1 more
Substituents
Aromatic heteropolycyclic compound / Azacycle / Azepine / Benzenoid / Carbonic acid derivative / Carbonyl group / Carboxylic acid derivative / Carboxylic acid ester / Dibenzazepine / Hydrocarbon derivative
show 8 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
acetate ester, carboxamide, dibenzoazepine (CHEBI:87016)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
BEA68ZVB2K
CAS number
236395-14-5
InChI Key
QIALRBLEEWJACW-INIZCTEOSA-N
InChI
InChI=1S/C17H16N2O3/c1-11(20)22-16-10-12-6-2-4-8-14(12)19(17(18)21)15-9-5-3-7-13(15)16/h2-9,16H,10H2,1H3,(H2,18,21)/t16-/m0/s1
IUPAC Name
(9S)-2-carbamoyl-2-azatricyclo[9.4.0.0³,⁸]pentadeca-1(15),3,5,7,11,13-hexaen-9-yl acetate
SMILES
CC(=O)O[C@H]1CC2=CC=CC=C2N(C(N)=O)C2=CC=CC=C12

References

Synthesis Reference
  • Ravinder B, Reddy SR, Sridhar M, Mohan MM, Srinivas K, Reddy AP, Bandichhor R. An efficient synthesis for eslicarbazepine acetate, oxcarbazepine, and carbamazepine. Tetrahedron Letters. 2013 May 29;54(22):2841-4.
  • Desai S, Poddar A, Sawant K: Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability. Mater Sci Eng C Mater Biol Appl. 2016 Jan 1;58:826-34. doi: 10.1016/j.msec.2015.09.019. Epub 2015 Sep 8. Pubmed.
General References
  1. Banach M, Borowicz KK, Czuczwar SJ: Pharmacokinetic/pharmacodynamic evaluation of eslicarbazepine for the treatment of epilepsy. Expert Opin Drug Metab Toxicol. 2015 Apr;11(4):639-48. doi: 10.1517/17425255.2015.1021686. Epub 2015 Mar 5. [Article]
  2. Bialer M, White HS: Key factors in the discovery and development of new antiepileptic drugs. Nat Rev Drug Discov. 2010 Jan;9(1):68-82. doi: 10.1038/nrd2997. [Article]
  3. Bialer M, Soares-da-Silva P: Pharmacokinetics and drug interactions of eslicarbazepine acetate. Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x. Epub 2012 May 21. [Article]
  4. Villanueva V, Serratosa JM, Guillamon E, Garces M, Giraldez BG, Toledo M, Salas-Puig J, Lopez Gonzalez FJ, Flores J, Rodriguez-Uranga J, Castillo A, Mauri JA, Camacho JL, Lopez-Gomariz E, Giner P, Torres N, Palau J, Molins A: Long-term safety and efficacy of eslicarbazepine acetate in patients with focal seizures: results of the 1-year ESLIBASE retrospective study. Epilepsy Res. 2014 Sep;108(7):1243-52. doi: 10.1016/j.eplepsyres.2014.04.014. Epub 2014 May 14. [Article]
  5. Soares-da-Silva P, Pires N, Bonifacio MJ, Loureiro AI, Palma N, Wright LC: Eslicarbazepine acetate for the treatment of focal epilepsy: an update on its proposed mechanisms of action. Pharmacol Res Perspect. 2015 Mar;3(2):e00124. doi: 10.1002/prp2.124. Epub 2015 Mar 30. [Article]
  6. Rocamora R: A review of the efficacy and safety of eslicarbazepine acetate in the management of partial-onset seizures. Ther Adv Neurol Disord. 2015 Jul;8(4):178-86. doi: 10.1177/1756285615589711. [Article]
  7. Tomic MA, Pecikoza UB, Micov AM, Stepanovic-Petrovic RM: The Efficacy of Eslicarbazepine Acetate in Models of Trigeminal, Neuropathic, and Visceral Pain: The Involvement of 5-HT1B/1D Serotonergic and CB1/CB2 Cannabinoid Receptors. Anesth Analg. 2015 Dec;121(6):1632-9. doi: 10.1213/ANE.0000000000000953. [Article]
  8. Jacobson MP, Pazdera L, Bhatia P, Grinnell T, Cheng H, Blum D: Efficacy and safety of conversion to monotherapy with eslicarbazepine acetate in adults with uncontrolled partial-onset seizures: a historical-control phase III study. BMC Neurol. 2015 Mar 28;15:46. doi: 10.1186/s12883-015-0305-5. [Article]
  9. Zaccara G, Giovannelli F, Cincotta M, Carelli A, Verrotti A: Clinical utility of eslicarbazepine: current evidence. Drug Des Devel Ther. 2015 Feb 10;9:781-9. doi: 10.2147/DDDT.S57409. eCollection 2015. [Article]
  10. Sperling MR, Abou-Khalil B, Harvey J, Rogin JB, Biraben A, Galimberti CA, Kowacs PA, Hong SB, Cheng H, Blum D, Nunes T, Soares-da-Silva P: Eslicarbazepine acetate as adjunctive therapy in patients with uncontrolled partial-onset seizures: Results of a phase III, double-blind, randomized, placebo-controlled trial. Epilepsia. 2015 Feb;56(2):244-53. doi: 10.1111/epi.12894. Epub 2014 Dec 22. [Article]
  11. Shaikh S, Rizvi SM, Hameed N, Biswas D, Khan M, Shakil S, Kamal MA: Aptiom (eslicarbazepine acetate) as a dual inhibitor of beta-secretase and voltage-gated sodium channel: advancement in Alzheimer's disease-epilepsy linkage via an enzoinformatics study. CNS Neurol Disord Drug Targets. 2014;13(7):1258-62. [Article]
  12. Doeser A, Soares-da-Silva P, Beck H, Uebachs M: The effects of eslicarbazepine on persistent Na(+) current and the role of the Na(+) channel beta subunits. Epilepsy Res. 2014 Feb;108(2):202-11. doi: 10.1016/j.eplepsyres.2013.11.022. Epub 2013 Dec 8. [Article]
  13. FDA Approved Drug Products: Aptiom (eslicarbazepine acetate) tablets for oral use [Link]
KEGG Drug
D09612
PubChem Compound
179344
PubChem Substance
310265036
ChemSpider
156110
BindingDB
50240669
RxNav
1482501
ChEBI
87016
ChEMBL
CHEMBL87992
ZINC
ZINC000000007295
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
PDRhealth
PDRhealth Drug Page
Wikipedia
Eslicarbazepine_acetate
FDA label
Download (820 KB)
MSDS
Download (44.8 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentEpilepsy1
4CompletedTreatmentPartial-Onset Seizures1
3CompletedTreatmentEpilepsy5
3CompletedTreatmentEpilepsy With Simple or Complex Partial Onset Seizures1
3CompletedTreatmentPartial Epilepsy3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
KitOral
TabletOral200 mg/1
TabletOral200 mg
TabletOral400 mg/1
TabletOral400 mg
TabletOral600 mg
TabletOral600 mg/1
TabletOral800 mg/1
TabletOral800 MG
SuspensionOral50 MG/ML
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5753646No1998-05-192016-06-27US flag
US8372431No2013-02-122030-04-17US flag
US9206135No2015-12-082026-04-21US flag
US9643929No2017-05-092026-04-21US flag
US9566244No2017-02-142028-10-23US flag
US9763954No2017-09-192028-09-13US flag
US9750747No2017-09-052032-08-24US flag
US10695354No2020-06-302025-05-06US flag
US10675287No2020-06-092025-05-06US flag
US10702536No2020-07-072025-05-06US flag
US10912781No2021-02-092028-10-23US flag
US11364247No2005-05-062025-05-06US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityWater solubility of eslicarbazepine acetate is low at less than 1 mg/mL including at different pH values. Its main metabolite eslicarbazepine has a greater water solubility of 4.2 mg/mL.# Banach M, Borowicz KK, Czuczwar SJ: Pharmacokinetic/pharmacodynamic evaluation of eslicarbazepine for the treatment of epilepsy. Expert Opin Drug Metab Toxicol. 2015 Apr;11(4):639-48. doi: 10.1517/17425255.2015.1021686. Epub 2015 Mar 5. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/25740561
logP8.8# Bialer M, Soares-da-Silva P: Pharmacokinetics and drug interactions of eslicarbazepine acetate. Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x. Epub 2012 May 21. "Pubmed":http://www.ncbi.nlm.nih.gov/pubmed/22612290
Predicted Properties
PropertyValueSource
Water Solubility0.11 mg/mLALOGPS
logP1.99ALOGPS
logP2.17Chemaxon
logS-3.4ALOGPS
pKa (Strongest Acidic)15.96Chemaxon
pKa (Strongest Basic)-3.8Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count2Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area72.63 Å2Chemaxon
Rotatable Bond Count2Chemaxon
Refractivity81.44 m3·mol-1Chemaxon
Polarizability30.19 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-000l-4290000000-ce88828aa8458d5001cf
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-000b-0190000000-7af1e0dfe0325ae3ab4a
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-9100000000-aa98df9e1fa47b1e2c74
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-01p6-0490000000-4ede23df8099b65574d0
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a4i-9000000000-06464f476e9b46a53d83
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-0490000000-5d275ffc6cc7e404595d
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-052f-9000000000-dc41dbb452f3d9a806b4
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-179.0404472
predicted
DarkChem Lite v0.1.0
[M-H]-161.73204
predicted
DeepCCS 1.0 (2019)
[M+H]+179.9304472
predicted
DarkChem Lite v0.1.0
[M+H]+164.09009
predicted
DeepCCS 1.0 (2019)
[M+Na]+179.4916472
predicted
DarkChem Lite v0.1.0
[M+Na]+170.35072
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
Receptor for ATP that acts as a ligand-gated ion channel. This receptor is insensitive to the antagonists PPADS and suramin.
Gene Name
P2RX4
Uniprot ID
Q99571
Uniprot Name
P2X purinoceptor 4
Molecular Weight
43368.725 Da
References
  1. Tian M, Abdelrahman A, Weinhausen S, Hinz S, Weyer S, Dosa S, El-Tayeb A, Muller CE: Carbamazepine derivatives with P2X4 receptor-blocking activity. Bioorg Med Chem. 2014 Feb 1;22(3):1077-88. doi: 10.1016/j.bmc.2013.12.035. Epub 2013 Dec 25. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
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
  1. Bialer M, Soares-da-Silva P: Pharmacokinetics and drug interactions of eslicarbazepine acetate. Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x. Epub 2012 May 21. [Article]
  2. Bialer M, White HS: Key factors in the discovery and development of new antiepileptic drugs. Nat Rev Drug Discov. 2010 Jan;9(1):68-82. doi: 10.1038/nrd2997. [Article]
  3. Galiana GL, Gauthier AC, Mattson RH: Eslicarbazepine Acetate: A New Improvement on a Classic Drug Family for the Treatment of Partial-Onset Seizures. Drugs R D. 2017 Sep;17(3):329-339. doi: 10.1007/s40268-017-0197-5. [Article]
  4. Eslicarbazepine, PDR [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
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
  1. Bialer M, Soares-da-Silva P: Pharmacokinetics and drug interactions of eslicarbazepine acetate. Epilepsia. 2012 Jun;53(6):935-46. doi: 10.1111/j.1528-1167.2012.03519.x. Epub 2012 May 21. [Article]
  2. Bialer M, White HS: Key factors in the discovery and development of new antiepileptic drugs. Nat Rev Drug Discov. 2010 Jan;9(1):68-82. doi: 10.1038/nrd2997. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Curator comments
The FDA label reports a mild activation of UGT1A1- mediated glucuronidation was observed in human hepatic microsomes, in relation to eslicarbazepine metabolism.
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. FDA Approved Drug Products: Aptiom (eslicarbazepine acetate) tablets for oral use [Link]

Drug created at September 22, 2015 20:02 / Updated at March 19, 2024 11:06