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

Details

Stereochemistry ABSOLUTE
Molecular Formula C11H20N2O2
Molecular Weight 212.2891
Optical Activity UNSPECIFIED
Defined Stereocenters 2 / 2
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of BRIVARACETAM

SMILES

CCC[C@]1([H])CC(=O)N(C1)[C@@]([H])(CC)C(=N)O

InChI

InChIKey=MSYKRHVOOPPJKU-BDAKNGLRSA-N
InChI=1S/C11H20N2O2/c1-3-5-8-6-10(14)13(7-8)9(4-2)11(12)15/h8-9H,3-7H2,1-2H3,(H2,12,15)/t8-,9+/m1/s1

HIDE SMILES / InChI
Molecular Formula C11H20N2O2
Molecular Weight 212.2891
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 2 / 2
E/Z Centers 0
Optical Activity UNSPECIFIED

Description

Brivaracetam (UCB 34714, trade name Briviact), the 4-n-propyl analog of levetiracetam, is a racetam derivative with anticonvulsant properties. Briviact is indicated as adjunctive therapy in the treatment of partial-onset seizures in patients 16 years of age and older with epilepsy. Brivaracetam is believed to act by binding to the ubiquitous synaptic vesicle glycoprotein 2A (SV2A), like levetiracetam, but with 20-fold greater affinity. There is some evidence that racetams including levetiracetam and brivaracetam access the luminal side of recycling synaptic vesicles during vesicular endocytosis. They may reduce excitatory neurotransmitter release and enhance synaptic depression during trains of high-frequency activity, such as is believed to occur during epileptic activity.

CNS Activity

Originator

Approval Year

2016
481
Targets

Targets

Primary TargetPharmacologyConditionPotency
Modulator
780
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Approved
8043
BRIVIACT

Approved Use

BRIVIACT is indicated as adjunctive therapy in the treatment of partial-onset seizures in patients 16 years of age and older with epilepsy

Launch Date

1.46301125E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
3.5 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
200 mg 1 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.7 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
13.3 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
800 mg 1 times / day multiple, oral
dose: 800 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
9 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
2.2 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
4.7 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
28 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
200 mg 1 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
55.4 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
90.8 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
800 mg 1 times / day multiple, oral
dose: 800 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
104.1 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
27.5 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
56 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
200 mg 1 times / day multiple, oral
dose: 200 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
6.8 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
400 mg 1 times / day multiple, oral
dose: 400 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
6.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
800 mg 1 times / day multiple, oral
dose: 800 mg
route of administration: Oral
experiment type: MULTIPLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.8 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.7 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
200 mg single, oral
dose: 200 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
7.3 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18341673
400 mg single, oral
dose: 400 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
BRIVARACETAM plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
80%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2018/205836s005,205837s004,205838s003lbl.pdf
unknown, unknown
 BRIVARACETAM plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Other AEs: Somnolence, Blurred vision...
Other AEs:
Somnolence (severe, 2 patients)
Blurred vision (1 patient)
Dizziness (2 patients)
Agitation (1 patient)
Bradyphrenia (1 patient)
Disorientation (1 patient)
Euphoric mood (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Other AEs: Somnolence, Blurred vision...
Other AEs:
Somnolence (2 patients)
Blurred vision (1 patient)
Dizziness (3 patients)
Agitation (1 patient)
Bradyphrenia (1 patient)
Disorientation (1 patient)
Euphoric mood (1 patient)
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Disc. AE: Convulsion, Somnolence...
AEs leading to
discontinuation/dose reduction:
Convulsion (1.4%)
Somnolence (0.7%)
Depression (0.6%)
Dizziness (0.6%)
Fatigue (0.5%)
Suicidal ideation (0.5%)
Suicide attempt (0.5%)
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
healthy, 64.1 years
n = 7
Health Status: healthy
Age Group: 64.1 years
Population Size: 7
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
Other AEs: Somnolence, Dizziness...
Other AEs:
Somnolence (57.1%)
Dizziness (42.9%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
2 mg/kg 2 times / day steady, oral
Highest studied dose
Dose: 2 mg/kg, 2 times / day
Route: oral
Route: steady
Dose: 2 mg/kg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/31250322
unhealthy, <8 years
Health Status: unhealthy
Condition: generalized epilepsy
Age Group: <8 years
Sex: M+F
Sources:
https://pubmed.ncbi.nlm.nih.gov/31250322
Sources:
https://pubmed.ncbi.nlm.nih.gov/31250322
AEs

AEs

AESignificanceDosePopulation
Agitation 1 patient
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Blurred vision 1 patient
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Bradyphrenia 1 patient
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Disorientation 1 patient
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Euphoric mood 1 patient
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Dizziness 2 patients
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Somnolence severe, 2 patients
1400 mg single, oral
Highest studied dose|MID
Dose: 1400 mg
Route: oral
Route: single
Dose: 1400 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Agitation 1 patient
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Blurred vision 1 patient
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Bradyphrenia 1 patient
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Disorientation 1 patient
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Euphoric mood 1 patient
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Somnolence 2 patients
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Dizziness 3 patients
1000 mg single, oral
MTD
Dose: 1000 mg
Route: oral
Route: single
Dose: 1000 mg
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
healthy, 18-55 years
n = 6
Health Status: healthy
Age Group: 18-55 years
Sex: M
Population Size: 6
Sources:
https://pubmed.ncbi.nlm.nih.gov/17223857
Fatigue 0.5%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Suicidal ideation 0.5%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Suicide attempt 0.5%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Depression 0.6%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Dizziness 0.6%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Somnolence 0.7%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Convulsion 1.4%
Disc. AE
200 mg 1 times / day steady, oral (max)
Recommended
Dose: 200 mg, 1 times / day
Route: oral
Route: steady
Dose: 200 mg, 1 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
unhealthy, 37.2 years
n = 2186
Health Status: unhealthy
Age Group: 37.2 years
Sex: M+F
Population Size: 2186
Sources:
https://pubmed.ncbi.nlm.nih.gov/27265725
Dizziness 42.9%
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
healthy, 64.1 years
n = 7
Health Status: healthy
Age Group: 64.1 years
Population Size: 7
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
Somnolence 57.1%
800 mg 1 times / day steady, oral
Highest studied dose
Dose: 800 mg, 1 times / day
Route: oral
Route: steady
Dose: 800 mg, 1 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
healthy, 64.1 years
n = 7
Health Status: healthy
Age Group: 64.1 years
Population Size: 7
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf
Page: p. 28
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
707

substrate
1601
inhibitor
1604

inducer
355

substrate
936
inhibitor
1702
inhibitor
1475

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP1A2
1383

CYP2A6
627

CYP2B6
717

CYP2C8
818

CYP2C19
1325

CYP3A4/5
241

BCRP
643

BSEP
376

MATE1
290

MATE2
251

P-gp
1330

MRP2
346

OAT1
554

OAT3
588

OCT1
480

OCT2
594

OATP1B1
733

OATP1B3
657
P-gp
1400

MRP1
97

MRP2
182

CYP2C19
910

CYP2C8
634
CYP1A2
637

CYP2B6
501

CYP2C19
269
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
OAT3
590
 no [IC50 541 uM]
OCT2
595
 no [IC50 740 uM]
OATP1B1
748
 no [Inhibition 200 uM]
CYP2C9
1648
 no [Inhibition 650 uM]
MATE1
292
 no [Inhibition 650 uM]
OCT1
495
 no [Inhibition 650 uM]
BCRP
713
 no
BSEP
377
 no
CYP1A2
1532
 no
CYP1A2
1532
 no
CYP2A6
659
 no
CYP2B6
884
 no
CYP2B6
884
 no
CYP2C19
1392
 no
CYP2C19
1392
 no
CYP2C8
865
 no
CYP2C9
1648
 no
CYP2D6
1738
 no
CYP3A4
1772
 no
CYP3A4/5
293
 no
MATE2
251
 no
MRP2
434
 no
OAT1
558
 no
OATP1B3
666
 no
P-gp
1514
 no
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
MRP1
97
 no
MRP2
182
 no
P-gp
1400
 no
CYP2C19
910
 yes [Km 70 uM]
CYP2C8
634
 yes
CYP2C9
936
 yes
CYP3A4
1601
 yes
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1507
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:133013
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:133013
ZINC
ZINC000003979899
http://zinc15.docking.org/substances/ZINC000003979899
PubMed

PubMed

TitleDatePubMed
Antiepileptic drug discovery: lessons from the past and future challenges.
2005
Gateways to clinical trials.
2005 Jan-Feb
Brivaracetam UCB.
2005 Jul
New antiepileptic drugs that are second generation to existing antiepileptic drugs.
2006 Jun
Diverse mechanisms of antiepileptic drugs in the development pipeline.
2006 Jun
Gateways to clinical trials.
2007 Dec
Pharmacological management of epilepsy: recent advances and future prospects.
2008
Gateways to clinical trials.
2008 Apr
Treatment of Lennox-Gastaut syndrome: overview and recent findings.
2008 Dec
New molecular targets for antiepileptic drugs: alpha(2)delta, SV2A, and K(v)7/KCNQ/M potassium channels.
2008 Jul
Gateways to clinical trials.
2008 Mar
SVOP is a nucleotide binding protein.
2009
Brivaracetam inhibits spreading depression in rat neocortical slices in vitro.
2009 Jul
Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions.
2009 Mar-Apr
Adjunctive brivaracetam for refractory partial-onset seizures: a randomized, controlled trial.
2010 Aug 10
New drugs for pediatric epilepsy.
2010 Dec
Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders.
2010 Feb 12
Physiologically based pharmacokinetic/pharmacodynamic animal-to-man prediction of therapeutic dose in a model of epilepsy.
2010 Mar
Patents

Patents

07629474
1
20030040631
3
JP2007515387A
1
JP2010024156A
2
JP2011507800A
42
JP2011513246A
21
JP4658937B2
1

Sample Use Guides

In Vivo Use Guide
The recommended starting dosage is 50 mg twice daily (100 mg per day). Based on individual patient tolerability and therapeutic response, the dosage may be adjusted down to 25 mg twice daily (50 mg per day) or up to 100 mg twice daily (200 mg per day). BRIVIACT (brivaracetam) injection may be used when oral administration is temporarily not feasible. BRIVIACT injection should be administered at the same dosage and same frequency as BRIVIACT tablets and oral solution.
Route of Administration: Other
In Vitro Use Guide
Brivaracetam (BRV) is able to modulate the voltage-activated Na(+) inflow in cortical neurons. Voltage-activated Na(+) currents were recorded by whole-cell patch-clamp on neuronal somas of rat neocortical neurons, grown in dissociated cell culture for up to 12 days. BRV, dissolved at the desired final concentration (between 0.2 microM and 1 mM) was applied by a multi-barrel pipette system near the soma of the recorded neuron. BRV produced a concentration-dependent inhibition of voltage-dependent Na(+) currents with IC(50) values of 41 microM at the holding potential of -100 mV, and of 6.5 microM at the holding potential of -60 mV. The voltage-dependence of activation and the kinetics of fast inactivation were not modified in the presence of BRV (30 microM).
Substance Class Chemical
Created
by admin
on Fri Jun 25 21:35:16 UTC 2021
Edited
by admin
on Fri Jun 25 21:35:16 UTC 2021
Record UNII
U863JGG2IA
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
BRIVARACETAM
DASH   INN   MART.   MI   USAN   WHO-DD  
USAN   INN  
Official Name English
BRIVARACETAM [MART.]
Common Name English
BRIVARACETAM [INN]
Common Name English
BRIVARACETAM [USAN]
Common Name English
BRIVARACETAM [WHO-DD]
Common Name English
BRIVARACETAM [MI]
Common Name English
UCB 34714
Code English
BRIVIACT
Brand Name English
UCB-34714
Code English
(2S)-2-((4R)-2-OXO-4-PROPYLPYRROLIDIN-1-YL)BUTANAMIDE
Systematic Name English
(2S)-2-((4R)-2-OXO-4-PROPYLTETRAHYDRO-1H-PYRROL-1-YL) BUTANAMIDE
Systematic Name English
1-PYRROLIDINEACETAMIDE, .ALPHA.-ETHYL-2-OXO-4-PROPYL (.ALPHA.S,4R)-
Common Name English
BRIVARACETAM [ORANGE BOOK]
Common Name English
Classification Tree Code System Code
EU-Orphan Drug EU/3/05/315
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
WHO-ATC N03AX23
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
FDA ORPHAN DRUG 207305
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
FDA ORPHAN DRUG 724019
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
FDA ORPHAN DRUG 711119
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
Code System Code Type Description
WIKIPEDIA
BRIVARACETAM
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
DRUG CENTRAL
5068
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
PUBCHEM
9837243
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
ChEMBL
CHEMBL607400
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
INN
8642
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
NDF-RT
N0000192345
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY Epoxide Hydrolase Inhibitors [MoA]
NCI_THESAURUS
C65270
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
EVMPD
SUB25397
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
DRUG BANK
DB05541
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
LACTMED
Brivaracetam
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
RXCUI
1739745
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
FDA UNII
U863JGG2IA
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
CAS
357336-20-0
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY
MERCK INDEX
M2654
Created by admin on Fri Jun 25 21:35:16 UTC 2021 , Edited by admin on Fri Jun 25 21:35:16 UTC 2021
PRIMARY Merck Index
Related Record Type Details
CYTOCHROME P450 2C19
METABOLIC ENZYME -> SUBSTRATE
MAJOR
CYTOCHROME P450 2C9
METABOLIC ENZYME -> SUBSTRATE
Structure of BRIVARACETAM
EXCRETED UNCHANGED
AMOUNT EXCRETED
URINE
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
SYNAPTIC VESICLE GLYCOPROTEIN 2A
TARGET->LIGAND
Related Record Type Details
Structure of UCB-100406-1
METABOLITE INACTIVE -> PARENT
AMOUNT EXCRETED
URINE
Structure of UCB-100406-1
METABOLITE INACTIVE -> PARENT
MAJOR
PLASMA
Structure of BRIVARACETAM ACID
METABOLITE INACTIVE -> PARENT
AMOUNT EXCRETED
URINE
Related Record Type Details
Structure of BRIVARACETAM
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
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