U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C16H18FN3O2
Molecular Weight 303.3314
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of EZOGABINE

SMILES

CCOC(=O)NC1=CC=C(NCC2=CC=C(F)C=C2)C=C1N

InChI

InChIKey=PCOBBVZJEWWZFR-UHFFFAOYSA-N
InChI=1S/C16H18FN3O2/c1-2-22-16(21)20-15-8-7-13(9-14(15)18)19-10-11-3-5-12(17)6-4-11/h3-9,19H,2,10,18H2,1H3,(H,20,21)

HIDE SMILES / InChI
Molecular Formula C16H18FN3O2
Molecular Weight 303.3314
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/21686305; https://www.ncbi.nlm.nih.gov/pubmed/?term=22221318

Ezogabine (U.S. adopted name) or retigabine (international nonproprietary name) is one of a family of aminopyrroles with anticonvulsant activity. It is used as an adjunctive treatment for partial epilepsies in treatment-experienced adult patients. The drug was approved by the European Medicines Agency under the trade name Trobalt and by the United States Food and Drug Administration (FDA), under the trade name Potiga. The mechanism by which ezogabine exerts its therapeutic effects has not been fully elucidated. In vitro studies indicate that ezogabine enhances transmembrane potassium currents mediated by the KCNQ (Kv7.2 to 7.5) family of ion channels. By activating KCNQ channels, ezogabine is thought to stabilize the resting membrane potential and reduce brain excitability. This mechanism of action is unique among antiepileptic drugs, and may hold promise for the treatment of other neurologic conditions, including migraine, tinnitus and neuropathic pain. In vitro studies suggest that ezogabine may also exert therapeutic effects through augmentation of GABA-mediated currents.

CNS Activity

CNS Penetrant
2523
Curator's Comment: Ezogabine can cross the blood–brain barrier and is not subject to P-glycoprotein active transport across this barrier, free brain concentrations will closely follow free plasma concentrations.

Originator

Valeant|GlaxoSmithKline
3
Curator's Comment: # Valeant Pharmaceuticals International and GlaxoSmithKline

Approval Year

2011
562
Targets

Targets

Primary TargetPharmacologyConditionPotency
Activator
1410
 1.6 µM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Secondary
Approved
8360
POTIGA

Approved Use

Indicated as adjunctive treatment of partial-onset seizures in patients aged 18 years and older who have responded inadequately to several alternative treatments and for whom the benefits outweigh the risk of retinal abnormalities and potential decline in visual acuity

Launch Date

1.30766406E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
414 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
498 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
551.9 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
561 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
819 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
842 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
993 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
978 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
728.8 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
938.7 ng/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
1831 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
1914 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
3972.5 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: HIGH-FAT
4393.8 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
5134 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5136 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5184 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
5279 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7355.9 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
7895.9 ng × h/mL
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
8.4 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.2 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
100 mg 2 times / day multiple, oral
dose: 100 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.4 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.9 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
250 mg single, oral
dose: 250 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
6.8 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
250 mg 2 times / day multiple, oral
dose: 250 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
200 mg 2 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.57 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
6.28 h
OTHER GOV
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2011/022345Orig1s000ClinPharmR.pdf
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
EZOGABINE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: HIGH-FAT
Doses

Doses

DosePopulationAdverse events​
350 mg 3 times / day multiple, oral
Recommended
Dose: 350 mg, 3 times / day
Route: oral
Route: multiple
Dose: 350 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25006968
unhealthy, 30 years
n = 2
Health Status: unhealthy
Condition: epilepsy
Age Group: 30 years
Sex: F
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/25006968
Disc. AE: Mucocutaneous disorder...
AEs leading to
discontinuation/dose reduction:
Mucocutaneous disorder (2 patients)
Sources:
https://pubmed.ncbi.nlm.nih.gov/25006968
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Disc. AE: Dizziness, Confusional state...
Other AEs: Urinary tract infection, Influenza...
AEs leading to
discontinuation/dose reduction:
Dizziness (9.2%)
Confusional state (6.5%)
Ataxia (2.6%)
Somnolence (3.9%)
Dysarthria (2.6%)
Headache (1.3%)
Fatigue (3.3%)
Vision blurred (1.3%)
Tremor (2.6%)
Nausea (2.6%)
Speech disorder (0.7%)
Memory impairment (0.7%)
Diplopia (2%)
Gait disturbance (1.3%)
Balance disorder (0.7%)
Vomiting (1.3%)
Anxiety (1.3%)
Disturbance in attention (2%)
Other AEs:
Urinary tract infection (11.8%)
Influenza (7.8%)
Constipation (5.9%)
Urinary hesitation (5.9%)
Dysuria (5.2%)
Disorientation (5.2%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
50 mg 3 times / day multiple, oral (starting)
Recommended
Dose: 50 mg, 3 times / day
Route: oral
Route: multiple
Dose: 50 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26909536
unhealthy, 48 years
n = 1
Health Status: unhealthy
Condition: epilepsy
Age Group: 48 years
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/26909536
Disc. AE: Maculopathy...
AEs leading to
discontinuation/dose reduction:
Maculopathy (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/26909536
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy, adult
n = 813
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 813
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Disc. AE: Dizziness, Confusional state...
AEs leading to
discontinuation/dose reduction:
Dizziness (6%)
Confusional state (4%)
Fatigue (3%)
Somnolence (3%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
2500 mg 1 times / day multiple, oral
Overdose
Dose: 2500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy
Health Status: unhealthy
Condition: epilepsy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Other AEs: Agitation, Aggressive behavior...
Other AEs:
Agitation
Aggressive behavior
Irritability
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
AEs

AEs

AESignificanceDosePopulation
Mucocutaneous disorder 2 patients
Disc. AE
350 mg 3 times / day multiple, oral
Recommended
Dose: 350 mg, 3 times / day
Route: oral
Route: multiple
Dose: 350 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/25006968
unhealthy, 30 years
n = 2
Health Status: unhealthy
Condition: epilepsy
Age Group: 30 years
Sex: F
Population Size: 2
Sources:
https://pubmed.ncbi.nlm.nih.gov/25006968
Balance disorder 0.7%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Memory impairment 0.7%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Speech disorder 0.7%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Anxiety 1.3%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Gait disturbance 1.3%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Headache 1.3%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Vision blurred 1.3%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Vomiting 1.3%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Urinary tract infection 11.8%
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Diplopia 2%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Disturbance in attention 2%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Ataxia 2.6%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Dysarthria 2.6%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Nausea 2.6%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Tremor 2.6%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Fatigue 3.3%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Somnolence 3.9%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Disorientation 5.2%
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Dysuria 5.2%
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Constipation 5.9%
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Urinary hesitation 5.9%
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Confusional state 6.5%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Influenza 7.8%
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Dizziness 9.2%
Disc. AE
1200 mg 1 times / day multiple, oral
Highest studied dose
Dose: 1200 mg, 1 times / day
Route: oral
Route: multiple
Dose: 1200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
unhealthy, 37.7 years (range: 18 –71 years)
n = 153
Health Status: unhealthy
Condition: drug-resistant partial epilepsy
Age Group: 37.7 years (range: 18 –71 years)
Sex: M+F
Population Size: 153
Sources:
https://pubmed.ncbi.nlm.nih.gov/21451152
Maculopathy 1 patient
Disc. AE
50 mg 3 times / day multiple, oral (starting)
Recommended
Dose: 50 mg, 3 times / day
Route: oral
Route: multiple
Dose: 50 mg, 3 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/26909536
unhealthy, 48 years
n = 1
Health Status: unhealthy
Condition: epilepsy
Age Group: 48 years
Sex: F
Population Size: 1
Sources:
https://pubmed.ncbi.nlm.nih.gov/26909536
Fatigue 3%
Disc. AE
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy, adult
n = 813
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 813
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Somnolence 3%
Disc. AE
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy, adult
n = 813
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 813
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Confusional state 4%
Disc. AE
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy, adult
n = 813
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 813
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Dizziness 6%
Disc. AE
600 mg 1 times / day multiple, oral
Recommended
Dose: 600 mg, 1 times / day
Route: oral
Route: multiple
Dose: 600 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy, adult
n = 813
Health Status: unhealthy
Age Group: adult
Sex: M+F
Population Size: 813
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Aggressive behavior
2500 mg 1 times / day multiple, oral
Overdose
Dose: 2500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy
Health Status: unhealthy
Condition: epilepsy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Agitation
2500 mg 1 times / day multiple, oral
Overdose
Dose: 2500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy
Health Status: unhealthy
Condition: epilepsy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Irritability
2500 mg 1 times / day multiple, oral
Overdose
Dose: 2500 mg, 1 times / day
Route: oral
Route: multiple
Dose: 2500 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
unhealthy
Health Status: unhealthy
Condition: epilepsy
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/022345s000lbl.pdf
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inhibitor
1752
inhibitor
1837
inhibitor
1599

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1509

CYP2A6
704

CYP2C8
901

CYP2C19
1463

CYP2E1
876

CYP3A4/5
273

P-gp
1437
UGT1A1
418

UGT1A3
422

UGT1A9
380

UGT1A4
347

UGT1A6
307

UGT1A7
236

UGT1A10
290

UGT2B4
249

UGT2B7
389

UGT2B15
203

CYP 450
31

P-gp
1527
CYP1A2
689

CYP3A4/5
120

CYP2C
15

P-gp
257
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
P-gp
1626
 likely
N-AMR
3
CYP1A2
1673
 no
CYP1A2
1673
 no
CYP2A6
736
 no
CYP2C
34
 no
CYP2C19
1537
 no
CYP2C8
955
 no
CYP2C9
1803
 no
CYP2D6
1875
 no
CYP2E1
964
 no
CYP3A4/5
330
 no
CYP3A4/5
330
 no
P-gp
1626
 no
P-gp
1626
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP 450
31
 no evidence
P-gp
1527
 no
UGT1A10
290
 no
UGT1A6
307
 no
UGT1A7
236
 no
UGT2B15
203
 no
UGT2B4
249
 no
UGT2B7
389
 no
UGT1A3
422
 yes
UGT1A4
347
 yes
UGT1A9
380
 yes
UGT1A1
418
 yes
no (pharmacogenomic study)
Comment: AUC of the acetylated metabolite was higher in subjects with UGT1A1*28 mutation versus subjects with UGT1A1 wildtype. The differences in PK parameters do not warrant dose change recommendations.
Page: 14.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1632
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:68584
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:68584
ChemicalBook
CB7506804
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB7506804
MolPort
MolPort-003-850-148
https://www.molport.com/shop/molecule-link/MolPort-003-850-148
ZINC
ZINC000000016154
http://zinc15.docking.org/substances/ZINC000000016154
eMolecules
2729733
https://www.emolecules.com/cgi-bin/more?vid=2729733
PubMed

PubMed

TitleDatePubMed
Future prospects for the drug treatment of epilepsy.
2001
The new generation of GABA enhancers. Potential in the treatment of epilepsy.
2001
Characterization of KCNQ5/Q3 potassium channels expressed in mammalian cells.
2001 Jan
Progress report on new antiepileptic drugs: a summary of the Fifth Eilat Conference (EILAT V).
2001 Jan
KCNQ4 channel activation by BMS-204352 and retigabine.
2001 Jun
Influence of retigabine on the anticonvulsant activity of some antiepileptic drugs against audiogenic seizures in DBA/2 mice.
2001 Mar
Effects of retigabine on rhythmic synchronous activity of human neocortical slices.
2001 May
Multiple-dose, linear, dose-proportional pharmacokinetics of retigabine in healthy volunteers.
2002 Feb
Activation of KCNQ5 channels stably expressed in HEK293 cells by BMS-204352.
2002 Feb 22
Pharmacokinetic interaction between retigabine and lamotrigine in healthy subjects.
2003 Apr
Voltage-independent KCNQ4 currents induced by (+/-)BMS-204352.
2003 Aug
Activation of M1 muscarinic receptors triggers transmitter release from rat sympathetic neurons through an inhibition of M-type K+ channels.
2003 Dec 15
Protein 4.1N is required for translocation of inositol 1,4,5-trisphosphate receptor type 1 to the basolateral membrane domain in polarized Madin-Darby canine kidney cells.
2003 Feb 7
Effects of age and sex on the disposition of retigabine.
2003 Jan
Neuroprotective effects of anticonvulsants in rat hippocampal slice cultures exposed to oxygen/glucose deprivation.
2003 Jan 2
Lack of pharmacokinetic interaction between retigabine and phenobarbitone at steady-state in healthy subjects.
2003 Jul
Effect of the KCNQ potassium channel opener retigabine on single KCNQ2/3 channels expressed in CHO cells.
2003 May 15
A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells.
2004 Dec
KCNQ/M channels control spike afterdepolarization and burst generation in hippocampal neurons.
2004 May 12
Progress report on new antiepileptic drugs: a summary of the Seventh Eilat Conference (EILAT VII).
2004 Sep-Oct
Ion channel defects in idiopathic epilepsies.
2005
Ion channels and epilepsy.
2005
Voltage gated ion channels: targets for anticonvulsant drugs.
2005
The new anticonvulsant retigabine favors voltage-dependent opening of the Kv7.2 (KCNQ2) channel by binding to its activation gate.
2005 Apr
Kv7/KCNQ/M and HCN/h, but not KCa2/SK channels, contribute to the somatic medium after-hyperpolarization and excitability control in CA1 hippocampal pyramidal cells.
2005 Aug 1
Effects of M-current modulators on the excitability of immature rat spinal sensory and motor neurones.
2005 Dec
Gateways to clinical trials.
2005 Jan-Feb
Anxiolytic effects of Maxipost (BMS-204352) and retigabine via activation of neuronal Kv7 channels.
2005 Jul
Presynaptic inhibition of transmitter release from rat sympathetic neurons by bradykinin.
2005 Jun
The KCNQ5 potassium channel from mouse: a broadly expressed M-current like potassium channel modulated by zinc, pH, and volume changes.
2005 Sep 13
[Voltage-activated potassium channels of the inhibitory interneurons of the hippocampus in culture].
2006
Pulmonary vasoconstrictor action of KCNQ potassium channel blockers.
2006 Feb 20
New antiepileptic drugs that are second generation to existing antiepileptic drugs.
2006 Jun
Diverse mechanisms of antiepileptic drugs in the development pipeline.
2006 Jun
KCNQ/Kv7 channel regulation of hippocampal gamma-frequency firing in the absence of synaptic transmission.
2006 May
KCNQ channels mediate IKs, a slow K+ current regulating excitability in the rat node of Ranvier.
2006 May 15
Recruitment of apical dendritic T-type Ca2+ channels by backpropagating spikes underlies de novo intrinsic bursting in hippocampal epileptogenesis.
2007 Apr 15
Phenytoin- and carbamazepine-resistant spontaneous bursting in rat entorhinal cortex is blocked by retigabine in vitro.
2007 May
Pharmacological comparison of anticonvulsant drugs in animal models of persistent pain and anxiety.
2007 Oct
The effectiveness of anticonvulsants in psychiatric disorders.
2008
Expression profile and characterisation of a truncated KCNQ5 splice variant.
2008 Jul 11
Retigabine reduces the excitability of unmyelinated peripheral human axons.
2008 Jun
Gateways to clinical trials.
2008 Mar
Antiepileptogenic and antiictogenic effects of retigabine under conditions of rapid kindling: an ontogenic study.
2008 Oct
Bimodal effects of the Kv7 channel activator retigabine on vascular K+ currents.
2008 Sep
Expression and function of K(v)7 channels in murine myometrium throughout oestrous cycle.
2009 Mar
Patents

Patents

US2006258712
3
US2007225274
3
US2010015228
3
US2010160411
3
US7365095
3
US7368477
3
US7501414
3
US7906537
3
US8017772
3

Sample Use Guides

In Vivo Use Guide
Potiga should be given orally in 3 equally divided doses daily, with or without food. The initial dosage should be 100 mg 3 times daily (300 mg per day) and should be increased gradually at weekly intervals by no more than 50 mg 3 times daily (increase in the daily dose of no more than 150 mg per day) up to a maintenance dosage of 200 mg to 400 mg 3 times daily (600 mg to 1,200 mg per day), based on individual patient response and tolerability.
Route of Administration: Oral
In Vitro Use Guide
KCNQ4 channels, stably expressed in HEK293 cells, were activated by retigabine (ezogabine) in a reversible and concentration-dependent manner in the concentration range 0.1-10 uM. Retigabine shifted the KCNQ4 channel activation curves towards more negative potentials by about 10 mV.
Substance Class Chemical
Created
by admin
on Thu Jul 06 22:20:24 UTC 2023
Edited
by admin
on Thu Jul 06 22:20:24 UTC 2023
Record UNII
12G01I6BBU
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
EZOGABINE
DASH   MI   ORANGE BOOK   USAN   VANDF  
USAN  
Official Name English
RETIGABINE
EMA EPAR   INN   MART.   WHO-DD  
INN  
Official Name English
Retigabine [WHO-DD]
Common Name English
POTIGA
Brand Name English
AWD-21360
Code English
GW582892X
Code English
EZOGABINE [MI]
Common Name English
TROBALT
Brand Name English
GKE-841
Code English
EZOGABINE [VANDF]
Common Name English
GW-582892X
Code English
RETIGABINE [MART.]
Common Name English
retigabine [INN]
Common Name English
AWD21-360
Code English
CARBAMIC ACID, (2-AMINO-4-(((4-FLUORO-PHENYL)METHYL)AMINO)PHENYL)-ETHYL ESTER
Systematic Name English
RETIGABINE [EMA EPAR]
Common Name English
D-23129
Code English
WAY-143841
Code English
EZOGABINE [ORANGE BOOK]
Common Name English
N-[2-Amino-4-(4-fluorobenzylamino)-phenyl]carbamic acid ethyl ester
Systematic Name English
EZOGABINE [USAN]
Common Name English
Classification Tree Code System Code
NDF-RT N0000182729
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
DEA NO. 2779
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
EMA ASSESSMENT REPORTS TROBALT (AUTHORIZED: EPILEPSY)
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
FDA ORPHAN DRUG 639118
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
WHO-VATC QN03AX21
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
NCI_THESAURUS C264
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
WHO-ATC N03AX21
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
LIVERTOX NBK548304
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
Code System Code Type Description
PUBCHEM
121892
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
MERCK INDEX
M5229
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY Merck Index
HSDB
8171
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
WIKIPEDIA
Retigabine
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
IUPHAR
2601
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
LACTMED
Ezogabine
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
INN
7545
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
CHEBI
68584
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
SMS_ID
100000080573
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
CAS
150812-12-7
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
USAN
SS-10
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
DRUG CENTRAL
4181
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
NCI_THESAURUS
C72839
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
EVMPD
SUB10291MIG
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
RXCUI
1112990
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY RxNorm
NDF-RT
N0000182728
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY Potassium Channel Openers [MoA]
EPA CompTox
DTXSID40164615
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
DRUG BANK
DB04953
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
ChEMBL
CHEMBL41355
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
FDA UNII
12G01I6BBU
Created by admin on Thu Jul 06 22:20:25 UTC 2023 , Edited by admin on Thu Jul 06 22:20:25 UTC 2023
PRIMARY
Related Record Type Details
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A4
METABOLIC ENZYME -> SUBSTRATE
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A1
METABOLIC ENZYME -> SUBSTRATE
Structure of EZOGABINE
EXCRETED UNCHANGED
URINE
Structure of EZOGABINE HYDROCHLORIDE
SALT/SOLVATE -> PARENT
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
URIDINE DIPHOSPHATE GLUCURONOSYLTRANSFERASE 1A3
METABOLIC ENZYME -> SUBSTRATE
ARYLAMINE N-ACETYLTRANSFERASE 2
METABOLIC ENZYME -> SUBSTRATE
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Structure of (2S,3S,4S,5R)-6-(2-(ETHOXYCARBONYLAMINO)-5-((4-FLUOROPHENYL)METHYLAMINO)ANILINO)-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
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Structure of (2S,3S,4S,5R)-6-(2-ACETAMIDO-5-((4-FLUOROPHENYL)METHYLAMINO)ANILINO)-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
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METABOLITE -> PARENT
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Structure of (2S,3S,4S,5R)-6-(4-ACETAMIDO-3-AMINO-N-((4-FLUOROPHENYL)METHYL)ANILINO)-3,4,5-TRIHYDROXY-TETRAHYDROPYRAN-2-CARBOXYLIC ACID
METABOLITE -> PARENT
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Structure of EZOGABINE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
ORAL BIOAVAILABILITY PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC INTRAVENOUS ADMINISTRATION

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