BRIVARACETAM

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C11H20N2O2
Molecular Weight	212.2887
Optical Activity	UNSPECIFIED
Defined Stereocenters	2 / 2
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

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

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/205836Orig1s000,205837Orig1s000,205838Orig1s000lbl.pdf | https://www.ncbi.nlm.nih.gov/pubmed/17199019

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

Targets

Primary Target	Pharmacology	Condition	Potency
Synaptic vesicle glycoprotein 2A 2 Target ID: CHEMBL1998 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19914041	Modulator 828

Conditions

Condition	Modality	Targets	Highest Phase	Product
Epilepsy 121 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/205836Orig1s000,205837Orig1s000,205838Orig1s000lbl.pdf	Primary		Approved 8429	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 2016

C_max

Value	Dose	Analyte	Population
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

Value	Dose	Analyte	Population
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

T_1/2

Value	Dose	Analyte	Population
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

F_unbound

Value	Dose	Co-administered	Analyte	Population
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

Dose	Population	Adverse 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

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
inducer 781 substrate 1737	inhibitor 1767 inducer 389 substrate 1037	inhibitor 1852	inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1524 CYP2A6 707 CYP2B6 810 CYP2C8 911 CYP2C19 1478 CYP3A4/5 278 BCRP 699 BSEP 402 MATE1 306 MATE2 263 P-gp 1461 MRP2 383 OAT1 599 OAT3 642 OCT1 512 OCT2 647 OATP1B1 788 OATP1B3 706	P-gp 1537 MRP1 107 MRP2 205 CYP2C19 991 CYP2C8 693	CYP1A2 701 CYP2B6 547 CYP2C19 293

Drug as perpetrator

Target	Modality	Activity
OAT3 644	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [IC50 541 uM]
OCT2 648	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [IC50 740 uM]
OATP1B1 803	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 200 uM]
CYP2C9 1819	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 650 uM]
MATE1 308	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 650 uM]
OCT1 543	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 650 uM]
BCRP 773	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
BSEP 403	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP1A2 1692	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP1A2 1692	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2A6 739	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2B6 1001	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2B6 1001	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2C19 1553	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2C19 1553	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2C8 965	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2C9 1819	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2D6 1891	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP3A4 1925	inducer 1573 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP3A4/5 335	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
MATE2 263	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
MRP2 475	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
OAT1 603	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
OATP1B3 715	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
P-gp 1650	inhibitor 3277 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no

Drug as victim

Target	Modality	Activity
MRP1 107	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
MRP2 205	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
P-gp 1537	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2C19 991	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes [Km 70 uM]
CYP2C8 693	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes
CYP2C9 1037	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes
CYP3A4 1737	substrate 3367 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1647	inhibitor 1626 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000PharmR.pdf#page=6 Page: 6.0

Sourcing

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

PubMed

Title	Date	PubMed
Brivaracetam is superior to levetiracetam in a rat model of post-hypoxic myoclonus.	2007	17690949
Gateways to clinical trials.	2007 Dec	18200333
The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after single increasing oral doses in healthy males.	2007 Jun	17223857
Evaluation of brivaracetam, a novel SV2A ligand, in the photosensitivity model.	2007 Sep 4	17785672
Pharmacological management of epilepsy: recent advances and future prospects.	2008	18778117
The effectiveness of anticonvulsants in psychiatric disorders.	2008	18472486
Gateways to clinical trials.	2008 Apr	18597009
Effect of brivaracetam on cardiac repolarisation--a thorough QT study.	2008 Aug	18601811
Brivaracetam: a rational drug discovery success story.	2008 Aug	18552880
Anti-convulsive and anti-epileptic properties of brivaracetam (ucb 34714), a high-affinity ligand for the synaptic vesicle protein, SV2A.	2008 Aug	18500360
Treatment of Lennox-Gastaut syndrome: overview and recent findings.	2008 Dec	19337447
Debate: Does genetic information in humans help us treat patients? PRO--genetic information in humans helps us treat patients. CON--genetic information does not help at all.	2008 Dec	19087113
Brivaracetam and seletracetam, two new SV2A ligands, improve paroxysmal dystonia in the dt sz mutant hamster.	2008 Dec 28	19014930
Modifications of antiepileptic drugs for improved tolerability and efficacy.	2008 Feb 14	19787095
Pharmacokinetics and metabolism of 14C-brivaracetam, a novel SV2A ligand, in healthy subjects.	2008 Jan	17908923
New molecular targets for antiepileptic drugs: alpha(2)delta, SV2A, and K(v)7/KCNQ/M potassium channels.	2008 Jul	18590620
The pharmacokinetics, CNS pharmacodynamics and adverse event profile of brivaracetam after multiple increasing oral doses in healthy men.	2008 Jul	18341673
Gateways to clinical trials.	2008 Mar	18560631
Brivaracetam: a new drug in development for epilepsy and neuropathic pain.	2008 Mar	18321235
SVOP is a nucleotide binding protein.	2009	19390693
What is the promise of new antiepileptic drugs in status epilepticus? Focus on brivaracetam, carisbamate, lacosamide, NS-1209, and topiramate.	2009 Dec	19941524
Progress report on new antiepileptic drugs: a summary of the Ninth Eilat Conference (EILAT IX).	2009 Jan	19008076
Brivaracetam inhibits spreading depression in rat neocortical slices in vitro.	2009 Jul	19211275
Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions.	2009 Mar-Apr	19443931
Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs.	2010 Apr	20502724
Gateways to clinical trials.	2010 Apr	20448862
Adjunctive brivaracetam for refractory partial-onset seizures: a randomized, controlled trial.	2010 Aug 10	20592253
New drugs for pediatric epilepsy.	2010 Dec	21183127
Progress report on new antiepileptic drugs: a summary of the Tenth Eilat Conference (EILAT X).	2010 Dec	20970964
Piracetam and piracetam-like drugs: from basic science to novel clinical applications to CNS disorders.	2010 Feb 12	20166767
Brivaracetam (ucb 34714) inhibits Na(+) current in rat cortical neurons in culture.	2010 Jan	19914041
Gateways to clinical trials.	2010 Mar	20401351
Physiologically based pharmacokinetic/pharmacodynamic animal-to-man prediction of therapeutic dose in a model of epilepsy.	2010 Mar	20102365
Antiepileptic drug interactions - principles and clinical implications.	2010 Sep	21358975
Brivaracetam does not alter spatial learning and memory in both normal and amygdala-kindled rats.	2010 Sep	20678901
Emerging drugs for partial onset seizures.	2010 Sep	20476851

Patents

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).

Name

Type

Language

BRIVARACETAM

Official Name

English

BRIVARACETAM [MART.]

Common Name

English

brivaracetam [INN]

Common Name

English

Brivaracetam [WHO-DD]

Common Name

English

BRIVARACETAM [USAN]

Common Name

English

BRIVARACETAM [MI]

Common Name

English

UCB 34714

Code

English

BRIVARACETAM [JAN]

Common Name

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