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 846

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 8583	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
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
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
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

AUC

Value	Dose	Analyte	Population
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
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
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

T_1/2

Value	Dose	Analyte	Population
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
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
7.3 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

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 Health Status: healthy Age Group: 18-55 years Sex: M 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 Health Status: healthy Age Group: 18-55 years Sex: M 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 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 Health Status: unhealthy Age Group: 37.2 years Sex: M+F 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	healthy, 64.1 years Health Status: healthy Age Group: 64.1 years Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000MedR.pdf	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
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 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 1087 substrate 1946	inhibitor 2438 inducer 440 substrate 1193	inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 2153 CYP2A6 879 CYP2B6 926 CYP2C8 1057 CYP2C19 2057 CYP3A4/5 296 BCRP 910 BSEP 550 MATE1 415 MATE2 267 P-gp 1741 MRP2 499 OAT1 725 OAT3 747 OCT1 620 OCT2 779 OATP1B1 1079 OATP1B3 961	P-gp 2052 MRP1 113 MRP2 252 CYP2C19 1119 CYP2C8 810	CYP1A2 832 CYP2B6 669 CYP2C19 329

Drug as perpetrator

Target	Modality	Activity
OAT3 749	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [IC50 541 uM]
OCT2 782	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [IC50 740 uM]
OATP1B1 1095	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 200 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 650 uM]
MATE1 416	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 650 uM]
OCT1 656	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no [Inhibition 650 uM]
BCRP 985	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
BSEP 554	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP1A2 2333	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2B6 1160	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2B6 1160	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2C19 2141	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP2C9 2497	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
CYP3A4 2633	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP3A4/5 357	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
MATE2 267	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
MRP2 625	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
OAT1 730	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
OATP1B3 970	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=3 Page: 3.0	no
P-gp 1932	inhibitor 4027 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 113	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
MRP2 252	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=338 Page: 338.0	no
CYP2C19 1119	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes [Km 70 uM]
CYP2C8 810	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes
CYP2C9 1193	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2016/205836Orig1s000_205837Orig1s000_205838Orig1s000ClinPharmR.pdf#page=337 Page: 337.0	yes
CYP3A4 1946	substrate 4014 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 2263	inhibitor 2237 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
Discovery of 4-substituted pyrrolidone butanamides as new agents with significant antiepileptic activity.	2004 Jan 29	14736235
Antiepileptic drug discovery: lessons from the past and future challenges.	2005	16238713
Gateways to clinical trials.	2005 Jan-Feb	15834459
Brivaracetam UCB.	2005 Jul	16044671
New antiepileptic drugs that are second generation to existing antiepileptic drugs.	2006 Jun	16732716
Diverse mechanisms of antiepileptic drugs in the development pipeline.	2006 Jun	16621450
Brivaracetam is superior to levetiracetam in a rat model of post-hypoxic myoclonus.	2007	17690949
Gateways to clinical trials.	2007 Dec	18200333
Progress report on new antiepileptic drugs: a summary of the Eigth Eilat Conference (EILAT VIII).	2007 Jan	17158031
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
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
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
Pharmacokinetics and metabolism of 14C-brivaracetam, a novel SV2A ligand, in healthy subjects.	2008 Jan	17908923
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
Brivaracetam inhibits spreading depression in rat neocortical slices in vitro.	2009 Jul	19211275
Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs.	2010 Apr	20502724
Physiologically based pharmacokinetic/pharmacodynamic animal-to-man prediction of therapeutic dose in a model of epilepsy.	2010 Mar	20102365

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

BRIVIACT

Preferred Name

English

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

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