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

Details

Stereochemistry ACHIRAL
Molecular Formula C10H8F2N4O
Molecular Weight 238.1939
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of RUFINAMIDE

SMILES

c1cc(c(Cn2cc(C(=N)O)nn2)c(c1)F)F

InChI

InChIKey=POGQSBRIGCQNEG-UHFFFAOYSA-N
InChI=1S/C10H8F2N4O/c11-7-2-1-3-8(12)6(7)4-16-5-9(10(13)17)14-15-16/h1-3,5H,4H2,(H2,13,17)

HIDE SMILES / InChI
Molecular Formula C10H8F2N4O
Molecular Weight 238.1939
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: http://www.rxlist.com/banzel-drug.htm https://www.drugs.com/mtm/rufinamide.html

Rufinamide is an anti-epileptic drug that is FDA approved for the treatment of lennox-gastaut syndrome (LGS). The principal mechanism of action of rufinamide is modulation of the activity of sodium channels and, in particular, prolongation of the inactive state of the channel. Hormonal contraceptives may be less effective with rufinamide. Patients on valproate should begin at a rufinamide dose lower than 10 mg/kg per day (pediatric patients) or 400 mg per day (adults). Common adverse reactions include headache, dizziness, fatigue, somnolence, and nausea.

CNS Activity

Originator

Approval Year

2008
56
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
7701
Modulator
777
 3.8 µM [EC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
7997
BANZEL

Approved Use

I NDICATIONS AND USAGE BANZEL is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome in pediatric patients 1 year of age and older and in adults. BANZEL is indicated for adjunctive treatment of seizures associated with Lennox-Gastaut Syndrome (LGS) in pediatric patients 1 year of age and older, and in adults (1)

Launch Date

1.2266208E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
3.8 μg/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18503564/
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RUFINAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
70.3 μg × h/mL
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18503564/
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RUFINAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
7.2 h
EXPERIMENT
https://pubmed.ncbi.nlm.nih.gov/18503564/
800 mg single, oral
dose: 800 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
RUFINAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
10 h
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204988Orig1s000lbl.pdf
200 mg 2 times / day unknown, oral
dose: 200 mg
route of administration: Oral
experiment type: UNKNOWN
co-administered:
RUFINAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
66%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/204988Orig1s000lbl.pdf
200 mg 2 times / day unknown, oral
dose: 200 mg
route of administration: Oral
experiment type: UNKNOWN
co-administered:
RUFINAMIDE plasma
Homo sapiens
population: UNHEALTHY
age: ADULT
sex: FEMALE / MALE
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
3600 mg 2 times / day multiple, oral
MTD
Dose: 3600 mg, 2 times / day
Route: oral
Route: multiple
Dose: 3600 mg, 2 times / day
Sources:
https://pubmed.ncbi.nlm.nih.gov/18503564
Page: p.1125, p.1139
healthy
n = 15
Health Status: healthy
Population Size: 15
Sources:
https://pubmed.ncbi.nlm.nih.gov/18503564
Page: p.1125, p.1139
Sources:
https://pubmed.ncbi.nlm.nih.gov/18503564
Page: p.1125, p.1139
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Other AEs: Depression worsened, Suicidal behavior...
Other AEs:
Depression worsened
Suicidal behavior (serious)
Leukopenia (serious)
Mood change
Central nervous system disorder NOS
Hypersensitivity reaction
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
Disc. AE: Fatigue...
Other AEs: QT shortened...
AEs leading to
discontinuation/dose reduction:
Fatigue (1-2)
Other AEs:
QT shortened (serious)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
Disc. AE: Convulsion, Rash...
AEs leading to
discontinuation/dose reduction:
Convulsion (2%)
Rash (2%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
Disc. AE: Vomiting, Dizziness...
AEs leading to
discontinuation/dose reduction:
Vomiting (1%)
Dizziness (3%)
Headache (2%)
Nausea (1%)
Ataxia (1%)
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
AEs

AEs

AESignificanceDosePopulation
Central nervous system disorder NOS
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Depression worsened
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Hypersensitivity reaction
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Mood change
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Leukopenia serious
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Suicidal behavior serious
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.1
Fatigue 1-2
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
QT shortened serious
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.4
Convulsion 2%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
Rash 2%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.7
Ataxia 1%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
Nausea 1%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
Vomiting 1%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
Headache 2%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
Dizziness 3%
Disc. AE
22.5 mg/kg 2 times / day multiple, oral
Studied dose
Dose: 22.5 mg/kg, 2 times / day
Route: oral
Route: multiple
Dose: 22.5 mg/kg, 2 times / day
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
unhealthy
Health Status: unhealthy
Condition: Lennox-Gastaut Syndrome
Sources:
https://www.accessdata.fda.gov/drugsatfda_docs/label/2015/021911s012lbl.pdf
Page: p.8
Overview

Overview

CYP3A4CYP2C9CYP2D6hERG
inducer
657
inhibitor
1360

OverviewOther

Other InhibitorOther SubstrateOther Inducer
CYP2E1
761

P-gp
1089
CYP
231

P-gp
1223
CYP1A
46
Drug as perpetrator​

Drug as perpetrator​

TargetModalityActivityMetaboliteClinical evidence
P-gp
1255
 inconclusive
CYP1A
105
 no
CYP3A4
1462
 weak
yes (co-administration study)
Comment: coadministration with triazolam resulted in a 37% decrease in AUC and 23% decrease in Cmax of triazolam
Page: 21.0
CYP2E1
841
 yes [Ki 450 uM]
Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
CYP
231
 no
P-gp
1223
 no
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
hERG
1392
Sourcing

Sourcing

Vendor/AggregatorIDURL
001 Chemical
DY34223
https://www.001chemical.com/chem/106308-44-5
3B Scientific (Wuhan) Corp
3B3-032294
http://www.3bsc.com/index/pro_info.php?id=53558
AA Blocks
AA0083RI
https://www.aablocks.com/goods/Goods/detail?id=AA0083RI
AHH Chemical co.,ltd
MT-27313
http://www.ahhchemical.com/product/MT-27313.html
AK Scientific, Inc. (AKSCI)
J10459
http://www.aksci.com/item_detail.php?cat=J10459
AK Scientific, Inc. (AKSCI)
Q503
http://www.aksci.com/item_detail.php?cat=Q503
Aaron Chemicals
AR0084JA
http://www.aaronchem.com/106308-44-5
AbMole Bioscience
M5943
http://www.abmole.com/search?q=M5943
Acadechem
ACDS-026251
http://www.acadechemical.com/product/100950
Achemtek
0104-006439
http://www.achemtek.com/106308-44-5
Alfa Chemistry
AP106308445
https://reagents.alfa-chemistry.com/product/rufinamide-cas-106308-44-5-1178.html
Ambeed
A193932
https://www.ambeed.com/products/106308-44-5.html
Angel Pharmatech
AG100069
http://www.angelpharmatech.com/106308-44-5.html
Angene
AGN-PC-04XLIP
http://www.angenechemical.com/productshow/AGN-PC-04XLIP.html
ApexBio Technology
B2280
http://www.apexbt.com/rufinamide.html
Ark Pharm
AK00592772
http://www.arkpharminc.com/products/106308-44-5.html
Aromsyn
AS07135
http://www.aromsyn.com/product/AS07135.html
Aurora Fine Chemicals LLC
A13.142.788
http://online.aurorafinechemicals.com/info?ID=A13.142.788
Aurum Pharmatech LLC
W-5135
http://www.Aurumpharmatech.com/Product/ProductDetails/W_5135
AvaChem Scientific
6755
https://www.avachem.com/productSearch.asp?6755
BLD Pharm
BD150601
http://www.bldpharm.com/products/106308-44-5.html
BioChemPartner
BCP21828
http://www.biochempartner.com/106308-44-5-BCP21828
BioCrick
BCC5078
http://www.biocrick.com/Rufinamide-BCC5078.html
BioSynth
J-001568
https://www.biosynth.com/en/products/all-products/products/J-001568.html
Boerchem
BC224496
http://www.boerchem.com/?product_37826.html
CSNpharm
CSN11872
https://www.csnpharm.com/products/rufinamide.html
Capot Chemical
14896
http://www.capotchem.com/en/14896.htm
Capot Chemical
PubChem14896
http://www.capotchem.com/en/14896.htm
Chem Scene
CS-1455
http://www.chemscene.com/106308-44-5.html
ChemMol
30108593
http://www.chemmol.com/chemmol/30108593.html
ChemMol
44007210
http://www.chemmol.com/chemmol/44007210.html
ChemMol
49400040
http://www.chemmol.com/chemmol/49400040.html
ChemMol
51502959
http://www.chemmol.com/chemmol/51502959.html
ChemMol
97900688
http://www.chemmol.com/chemmol/97900688.html
Chemenu
CM110361
http://www.chemenu.com/products/CM110361
Chemspace
CSSB00000694639
https://chem-space.com/CSSB00000694639
Clearsynth
CS-O-02240
https://www.clearsynth.com/en/CSO02240.html
Clearsynth
CS-T-42005
https://www.clearsynth.com/en/CST42005.html
DC Chemicals
DC7272
http://www.dcchemicals.com/product_show-Rufinamide.html
Enamine
Z1541638521
https://www.enaminestore.com/catalog/Z1541638521
Finetech
FT-0656828
http://www.finetechnology-ind.com/prod/detail/pub/106308-44-5.html
Finetech
FT-0674479
http://www.finetechnology-ind.com/prod/detail/pub/170939-95-4.html
Glentham Life Sciences
GP1695
http://www.glentham.com/products/product/GP1695/
Hairui
HR111623
http://www.hairuichem.com/en/product/106308-44-5.html
Hello Bio
HB1039
https://www.hellobio.com/rufinamide.html
Lab Network
LN00236052
https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00236052
MedChem Express
HY-A0042
https://www.medchemexpress.com/rufinamide.html
Molcore
MC34223
https://www.molcore.com/product/106308-44-5
MuseChem
I000319
https://www.musechem.com/product/I000319.html
OChem
9340
http://www.ocheminc.com/index.php?act=psearch&pid=308R445
Selleck Chemicals
S1256
http://www.selleckchem.com/products/Rufinamide.html
Sigma-Aldrich
PHR1625_SIAL
https://www.sigmaaldrich.com/catalog/product/sial/phr1625?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
R8404_SIGMA
https://www.sigmaaldrich.com/catalog/product/sigma/r8404?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich
1606401_USP
https://www.sigmaaldrich.com/catalog/product/usp/1606401?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sinfoo Biotech
S010594
http://www.sinfoobiotech.com/product/1013992
Smolecule
S542061
http://www.smolecule.com/products/s542061
Smolecule
S774580
https://www.smolecule.com/products/s774580
Synblock Inc
SB18904
http://www.synblock.com/product/106308-44-5.html
Synchem UG and Co KG
68220
http://www.synchem.de/chemical_Rufinamide.html
TCI (Tokyo Chemical Industry)
R0143
http://www.tcichemicals.com/eshop/en/us/commodity/R0143/index.html
THE BioTek
bt-280582
https://www.thebiotek.com/product/inhibitors/bt-280582
Tocris
3828
https://www.tocris.com/products/rufinamide_3828
VladaChem
VL278792-100MG
https://www.vladachem.com/product.php?products=106308-44-5
Yuhao Chemical
RT2381
http://www.chemyuhao.com/106308-44-5.html
abcr GmbH
AB505794
http://www.abcr.com/shop/en/AB505794
eNovation Chemicals
D546945
https://www.enovationchem.com/ProductDetails.asp?ProductID=D546945
iChemical
EBD35607
http://www.ichemical.com/chemicals/cas-106308-44-5
mcule
MCULE-6872329028
https://mcule.com/MCULE-6872329028/
PubMed

PubMed

TitleDatePubMed
Rufinamide: Further evaluation is needed in Lennox-Gastaut syndrome.
2008 Aug
Update on the management of Lennox-Gastaut syndrome with a focus on rufinamide.
2009
Onset of action and seizure control in Lennox-Gaustaut syndrome: focus on rufinamide.
2009 Apr
Rufinamide for the adjunctive treatment of partial seizures in adults and adolescents: a randomized placebo-controlled trial.
2009 Aug
Safety and tolerability of rufinamide in children with epilepsy: a pooled analysis of 7 clinical studies.
2009 Dec
Treatment of Lennox-Gastaut syndrome.
2009 Jul 8
Minimizing AED adverse effects: improving quality of life in the interictal state in epilepsy care.
2009 Jun
Truly "rational" polytherapy: maximizing efficacy and minimizing drug interactions, drug load, and adverse effects.
2009 Jun
Transitional polytherapy: tricks of the trade for monotherapy to monotherapy AED conversions.
2009 Jun
Antiepileptic drug monotherapy: the initial approach in epilepsy management.
2009 Jun
Third-generation antiepileptic drugs: mechanisms of action, pharmacokinetics and interactions.
2009 Mar-Apr
Adopting an orphan drug: rufinamide for Lennox-Gastaut syndrome.
2009 May-Jun
New drugs: Febuxostat, lacosamide, and rufinamide.
2009 May-Jun
Gateways to clinical trials.
2009 Nov
The possible antianxiety and mood-stabilizing effects of rufinamide.
2010
The cost effectiveness of rufinamide in the treatment of Lennox-Gastaut syndrome in the UK.
2010
Recent advances in adjunctive therapy for epilepsy: focus on sodium channel blockers as third-generation antiepileptic drugs.
2010 Apr
Gateways to clinical trials.
2010 Apr
Rufinamide: a new antiepileptic medication for the treatment of seizures associated with lennox-gastaut syndrome.
2010 Apr
First European long-term experience with the orphan drug rufinamide in childhood-onset refractory epilepsy.
2010 Apr
"Epileptic encephalopathy" of infancy and childhood: electro-clinical pictures and recent understandings.
2010 Dec
New drugs for pediatric epilepsy.
2010 Dec
Post-treatment with voltage-gated Na(+) channel blocker attenuates kainic acid-induced apoptosis in rat primary hippocampal neurons.
2010 Dec
Ethyl 1-(2,6-difluoro-benz-yl)-1H-1,2,3-triazole-4-carboxyl-ate.
2010 Dec 15
Selected pharmacokinetic issues of the use of antiepileptic drugs and parenteral nutrition in critically ill patients.
2010 Dec 31
Supporting the recommended paediatric dosing regimen for rufinamide in Lennox-Gastaut syndrome using clinical trial simulation.
2010 Feb
New Drugs2010, PART 1.
2010 Feb
A 24-week multicenter, randomized, double-blind, parallel-group, dose-ranging study of rufinamide in adults and adolescents with inadequately controlled partial seizures.
2010 Feb
Simultaneous HPLC-UV analysis of rufinamide, zonisamide, lamotrigine, oxcarbazepine monohydroxy derivative and felbamate in deproteinized plasma of patients with epilepsy.
2010 Feb 1
Lennox-Gastaut syndrome: An overview.
2010 Jan
Rufinamide: a novel broad-spectrum antiepileptic drug.
2010 Jan
Drug interactions involving the new second- and third-generation antiepileptic drugs.
2010 Jan
Cost-utility analysis of rufinamide versus topiramate and lamotrigine for the treatment of children with Lennox-Gastaut Syndrome in the United Kingdom.
2010 Jan
Drug-induced QT interval shortening: potential harbinger of proarrhythmia and regulatory perspectives.
2010 Jan
New antiepileptic drugs: lacosamide, rufinamide, and vigabatrin.
2010 Jul
Update on anticonvulsant drugs.
2010 Jul
Rufinamide: a new antiepileptic drug treatment for Lennox-Gastaut syndrome.
2010 Jun
Gateways to clinical trials.
2010 Mar
Stability of extemporaneously prepared rufinamide oral suspensions.
2010 Mar
Severe constipation associated with the use of rufinamide (Banzel) in an adolescent.
2010 May
[Antiepileptic drugs in North America].
2010 May
Medical management of Lennox-Gastaut syndrome.
2010 May
Rufinamide in children and adults with Lennox-Gastaut syndrome: first Italian multicenter experience.
2010 Nov
Expression, regulation and function of phosphofructo-kinase/fructose-biphosphatases (PFKFBs) in glucocorticoid-induced apoptosis of acute lymphoblastic leukemia cells.
2010 Nov 23
Treating Lennox-Gastaut syndrome in epileptic pediatric patients with third-generation rufinamide.
2010 Oct 5
Antiepileptic drug interactions - principles and clinical implications.
2010 Sep
Experience with rufinamide in a pediatric population: a single center's experience.
2010 Sep
Emerging drugs for partial onset seizures.
2010 Sep
Adjunctive rufinamide in Lennox-Gastaut syndrome: a long-term, open-label extension study.
2010 Sep
Rufinamide for pediatric patients with Lennox-Gastaut syndrome: a comprehensive overview.
2011 Apr 1
Patents

Patents

08183269
2
EP 199262
1
US 4789680
1

Sample Use Guides

In Vivo Use Guide
Starting daily dose: 400-800 mg per day in two equally divided doses. Increase by 400-800 mg every other day until a maximum dose of 3200 mg per day, in two divided doses, is reached.
Route of Administration: Oral
In Vitro Use Guide
In vitro studies with human liver microsomes using con-centrations of rufinamide in the range of 10–300 µmol/L(2.4–72 µg/ml) found no significant inhibition of any ofeight major human CYP isozymes—CYP1A2, CYP2A6,CYP2C9, CYP2C19, CYP2D6, CYP2E1, CYP3A4/5, andCYP4A9/11.
Substance Class Chemical
Created
by admin
on Sat Jun 26 05:39:43 UTC 2021
Edited
by admin
on Sat Jun 26 05:39:43 UTC 2021
Record UNII
WFW942PR79
Record Status Validated (UNII)
Record Version
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Name Type Language
RUFINAMIDE
DASH   EMA EPAR   INN   MART.   MI   ORANGE BOOK   USAN   USP-RS   VANDF   WHO-DD  
INN   USAN  
Official Name English
1-(2,6-DIFLUOROBENZYL)-1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE
Systematic Name English
1H-1,2,3-TRIAZOLE-4-CARBOXAMIDE, 1-((2,6-DIFLUOROPHENYL)METHYL)-
Systematic Name English
RUFINAMIDE [ORANGE BOOK]
Common Name English
RUFINAMIDE [WHO-DD]
Common Name English
RUFINAMIDE [JAN]
Common Name English
INOVELON
Brand Name English
RUFINAMIDE [MART.]
Common Name English
RUF 331
Code English
RUFINAMIDE [EMA EPAR]
Common Name English
CGP 33101
Code English
E-2080
Code English
CGP-33101
Code English
RUFINAMIDE [VANDF]
Common Name English
RUFINAMIDE [USP MONOGRAPH]
Common Name English
RUF-331
Code English
60231/4
Code English
RUFINAMIDE [MI]
Common Name English
E2080
Code English
RUFINAMIDE [USP-RS]
Common Name English
RUFINAMIDE [USAN]
Common Name English
RUFINAMIDE [INN]
Common Name English
BANZEL
Brand Name English
Classification Tree Code System Code
WHO-ATC N03AF03
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
NCI_THESAURUS C264
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
WHO-VATC QN03AF03
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
LIVERTOX 865
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
EU-Orphan Drug EU/3/04/240
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
EMA ASSESSMENT REPORTS INOVELON (AUTHORIZED: EPILEPSY)
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
FDA ORPHAN DRUG 193504
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
Code System Code Type Description
MESH
C079703
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
INN
7387
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
WIKIPEDIA
RUFINAMIDE
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
CAS
106308-44-5
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
FDA UNII
WFW942PR79
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
USP_CATALOG
1606401
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY USP-RS
PUBCHEM
129228
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
IUPHAR
7470
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
EVMPD
SUB10403MIG
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
ChEMBL
CHEMBL1201754
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
RXCUI
69036
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY RxNorm
LACTMED
Rufinamide
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
MERCK INDEX
M9696
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY Merck Index
NCI_THESAURUS
C75167
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
DRUG BANK
DB06201
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
EPA CompTox
106308-44-5
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
DRUG CENTRAL
3534
Created by admin on Sat Jun 26 05:39:44 UTC 2021 , Edited by admin on Sat Jun 26 05:39:44 UTC 2021
PRIMARY
Related Record Type Details
CYTOCHROME P450 2E1
METABOLIC ENZYME -> INHIBITOR
Ki
Structure of RUFINAMIDE
BASIS OF STRENGTH->SUBSTANCE
ASSAY (HPLC)
USP
Structure of RUFINAMIDE
EXCRETED UNCHANGED
FECAL; URINE
CYTOCHROME P450 3A4
METABOLIC ENZYME -> INDUCER
WEAK
PLASMA PROTEIN FRACTION (HUMAN)
BINDER->LIGAND
BINDING
SODIUM CHANNEL PROTEIN TYPE 1 SUBUNIT ALPHA
TARGET -> INHIBITOR
Shifts hNav1.1 opening to more depolarized voltages without further alterations in the gating properties of hNav1.1, hNav1.2, hNav1.3, and hNav1.6;
Related Record Type Details
Structure of CGP-47292
METABOLITE -> PARENT
MAJOR
PLASMA
Related Record Type Details
Structure of DESFLUORORUFINAMIDE
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Structure of CGP-47292 METHYL ESTER
IMPURITY -> PARENT
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
Related Record Type Details
Structure of RUFINAMIDE
ACTIVE MOIETY
Name Property Type Amount Referenced Substance Defining Parameters References
Tmax PHARMACOKINETIC
Biological Half-life PHARMACOKINETIC
Volume of Distribution PHARMACOKINETIC
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
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