Page last updated: 2024-12-11
eslicarbazepine
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Market Indicators
Cross-References
ID Source | ID |
---|---|
PubMed CID | 9881504 |
CHEMBL ID | 315985 |
CHEBI ID | 174358 |
SCHEMBL ID | 418933 |
MeSH ID | M0572254 |
Synonyms (62)
Synonym |
---|
cgp-13751 |
bia-2-194 |
bia 2-194 |
eslicarbazepine |
(s)-licarbazepine |
CHEMBL315985 |
licarbazepine, (s)- |
(5s)-5-hydroxy-5,6-dihydrobenzo[b][1]benzazepine-11-carboxamide |
(s)-mhd |
CHEBI:174358 |
104746-04-5 |
eslicarbazepine (usan/inn) |
D09215 |
s-(+)-10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide |
(10s)-10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide |
(10s)-10-hydroxy-10,11-dihydro-5h-dibenzo[b,f]azepine-5 carboxamide |
(s)-(+)-10-hydroxy-10,11-dihydro-5h-dibenz[b,f]azepine-5-carboxamide |
BMPDWHIDQYTSHX-AWEZNQCLSA-N |
(s)-(+)-10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide |
(10s)-10-hydroxy-10,11-dihydro-5h-dibenzo[b,f]azepine-5-carboxamide |
(10s)-10,11-dihydro-10-hydroxy-5h-dibenz(b,f)azepine-5-carboxamide |
(10s)-10-hydroxy-10,11-dihydro-5h-dibenzo(b,f)azepin-5-carboxamide |
s(+)-liscarbazepine |
ec 810-248-9 |
eslicarbazepine [usan:inn:ban] |
unii-s5vxa428r4 |
s5vxa428r4 , |
(10s)-10-hydroxy-10,11-dihydro-5h-dibenzo[b,f]azepin-5-carboxamide |
(s)-(+)-10,11-dihydro-10-hydroxy-5h-dibenz(b,f)azepine-5-carboxamide |
5h-dibenz(b,f)azepine-5-carboxamide, 10,11-dihydro-10-hydroxy-, (10s)- |
eslicarbazepine [who-dd] |
eslicarbazepine [mi] |
eslicarbazepine [usan] |
eslicarbazepine [mart.] |
eslicarbazepine [vandf] |
eslicarbazepine [inn] |
bia-2194 |
s-10-monohydroxy-dihydro-carbamazepin |
gtpl7350 |
s-licarbazepine |
SCHEMBL418933 |
AKOS016844866 |
(s)-10-hydroxy-10,11-dihydro-5h-dibenzo[b,f]azepine-5-carboxamide |
5h-dibenz[b,f]azepine-5-carboxamide,10,11-dihydro-10-hydroxy-,(10s)- |
J-001242 |
HY-114703 |
CS-0064132 |
DB14575 |
Q27077226 |
monohydroxy carbamazepine |
(s)-licarbazepine; (10s)-10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide; s-(+)-10,11-dihydro-10-hydroxy-5h-dibenz[b,f]azepine-5-carboxamide |
eslicarbazepine (bia 2-194) |
MS-23581 |
(eslicarbazepine) |
(s)-10-monohydroxy-10,11-dihydro carbamazepine |
DTXSID901316900 |
EN300-18686811 |
(9s)-9-hydroxy-2-azatricyclo[9.4.0.0,3,8]pentadeca-1(15),3,5,7,11,13-hexaene-2-carboxamide |
eslicarbazepinum |
eslicarbazepina |
eslicarbazepine (mart.) |
n03af04 |
Research Excerpts
Overview
Eslicarbazepine is a novel anti-epileptic agent indicated for the treatment of partial-onset seizures. It is chemically related to carbamazepine but with a more favorable safety profile.
Treatment
Excerpt | Reference | Relevance |
---|---|---|
"Eslicarbazepine- and LCM-treated fast-inactivated channels recovered similarly to control conditions, whereas CBZ- and OXC-treated channels required longer pulses to recover." | ( Eslicarbazepine and the enhancement of slow inactivation of voltage-gated sodium channels: a comparison with carbamazepine, oxcarbazepine and lacosamide. Bonifácio, MJ; Hebeisen, S; Loureiro, AI; Palma, N; Pires, N; Soares-da-Silva, P; Spanswick, D; Whyment, A, 2015) | 2.58 |
Pharmacokinetics
Excerpt | Reference | Relevance |
---|---|---|
" This study evaluated the effect of multiple-dose ESL on the pharmacokinetic (PK) parameters of a single dose of rosuvastatin in healthy subjects." | ( Evidence for a pharmacokinetic interaction between eslicarbazepine and rosuvastatin: Potential effects on xenobiotic transporters. Blum, D; Gidal, BE; Grinnell, T; Kharidia, J; Mintzer, S; Schutz, R; Schwab, M; Sunkaraneni, S, 2017) | 0.71 |
Bioavailability
Excerpt | Reference | Relevance |
---|---|---|
" This study was performed to characterize the disposition of the two enantiomers of MHD after oral and intravenous administration and to estimate the bioavailability of MHD after a single oral dose administration of OXC compared to a single intravenous administration of MHD." | ( Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. Czendlik, C; Flesch, G; Lloyd, P; Renard, D, 2011) | 0.37 |
"Rosuvastatin exposure was 36-39% lower with steady-state administration of ESL, potentially due to reduced oral bioavailability of rosuvastatin." | ( Evidence for a pharmacokinetic interaction between eslicarbazepine and rosuvastatin: Potential effects on xenobiotic transporters. Blum, D; Gidal, BE; Grinnell, T; Kharidia, J; Mintzer, S; Schutz, R; Schwab, M; Sunkaraneni, S, 2017) | 0.71 |
Dosage Studied
Excerpt | Relevance | Reference |
---|---|---|
"Five groups of each of 12 female rats were orally dosed daily for 8 weeks with either carbamazepine (CBZ) (60 mg/kg), eslicarbazepine (ESL) (80 mg/kg), valproic acid (VPA) (300 mg/kg), levetiracetam (LEV) (50 mg/kg) or saline (control (CTL))." | ( Effects of carbamazepine, eslicarbazepine, valproic acid and levetiracetam on bone microarchitecture in rats. Andersen, NB; Diemar, SS; Ding, M; Eiken, P; Ellegaard, M; Jørgensen, NR; Sejling, AS, 2020) | 1.07 |
" Furthermore, most preclinical antiepileptogenic studies lack information needed for translation, such as dose-blood level relationship, brain target engagement, and dose-response, and many use treatment parameters that cannot be applied clinically, for example, treatment initiation before or at the time of injury and dosing higher than tolerated human equivalent dosing." | ( Repurposed molecules for antiepileptogenesis: Missing an opportunity to prevent epilepsy? Bar-Klein, G; Friedman, A; Hameed, MQ; Jozwiak, S; Kaminski, RM; Klein, P; Klitgaard, H; Koepp, M; Löscher, W; Prince, DA; Rotenberg, A; Twyman, R; Vezzani, A; Wong, M, 2020) | 0.56 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (1)
Class | Description |
---|---|
dibenzooxazepine | An organic heterotricyclic compound consisting of two benzene rings fused to a seven-membered ring containing one oxygen and one nitrogen atom. |
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] |
Bioassays (27)
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID1220847 | Cmax in human treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220850 | AUC (0 to 32/48 hrs) in human treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220837 | Drug excretion in human urine assessed as total amount of drug eliminated treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220829 | Total plasma clearance in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as single dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220817 | AUC (0 to 72 hrs) in human treated with monohydroxy derivative of OXC at 200 mg, iv administered as single dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID195317 | Compound was tested for anticonvulsant activity against MES-induced seizures in rat | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1220825 | Total plasma clearance in human treated with monohydroxy derivative of OXC at 150 mg, iv administered as single dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220854 | Terminal half life in human urine treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220846 | Tmax in human treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220851 | Drug excretion in human urine assessed as total amount of drug eliminated treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID190110 | Compound was tested intraperitoneally for anticonvulsant activity by rotarod test | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1220836 | AUC in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220815 | AUC (0 to 72 hrs) in human treated with monohydroxy derivative of OXC at 150 mg, iv administered as single dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220852 | Renal clearance in human treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220835 | AUC (0 to 48 hrs) in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220838 | Total plasma clearance in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220842 | Terminal half life in human urine treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220827 | Total plasma clearance in human treated with monohydroxy derivative of OXC at 200 mg, iv administered as single dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220840 | Apparent terminal half life in human plasma treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220821 | Drug excretion in human urine assessed as total amount of drug eliminated treated with monohydroxy derivative of OXC at 150 mg, iv administered as single dose measured for 72 hrs post-dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID226935 | Protective index value of the compound, given by intraperitoneally (TD50/ED50) | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID176347 | Compound was tested intraperitoneally for anticonvulsant activity against MES-induced seizures in rat by MES test | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1220839 | Renal clearance in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220853 | Apparent terminal half life in human plasma treated with oxcarbazepine at 300 mg, po administered as one-film coated tablet by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID1220841 | Volume of distribution at steady state in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as infusion over 30 mins by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
AID196513 | t max for anticonvulsant activity was tested in rats intraperitoneally | 1999 | Journal of medicinal chemistry, Jul-15, Volume: 42, Issue:14 | Anticonvulsant and sodium channel-blocking properties of novel 10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide derivatives. |
AID1220819 | AUC (0 to 72 hrs) in human treated with monohydroxy derivative of OXC at 250 mg, iv administered as single dose by high-performance liquid chromatography | 2011 | Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 39, Issue:6 | Pharmacokinetics of the monohydroxy derivative of oxcarbazepine and its enantiomers after a single intravenous dose given as racemate compared with a single oral dose of oxcarbazepine. |
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Research
Studies (41)
Timeframe | Studies, This Drug (%) | All Drugs % |
---|---|---|
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (2.44) | 18.2507 |
2000's | 0 (0.00) | 29.6817 |
2010's | 28 (68.29) | 24.3611 |
2020's | 12 (29.27) | 2.80 |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |
Market Indicators
Research Demand Index: 68.78
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.
| This Compound (68.78) All Compounds (24.57) |
Study Types
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 3 (7.14%) | 5.53% |
Reviews | 9 (21.43%) | 6.00% |
Case Studies | 10 (23.81%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 20 (47.62%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |