rufinamide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	3534	106308-44-5

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: rufinamide inovelon banzel CGP-33101 CGP 33101	The precise mechanism(s) by which rufinamide exerts its antiepileptic effect is unknown. The results of in vitro studies suggest that 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. Molecular weight: 238.20 Formula: C10H8F2N4O CLOGP: 0.51 LIPINSKI: 0 HAC: 5 HDO: 1 TPSA: 73.80 ALOGS: -2.57 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

rufinamide
inovelon
banzel
CGP-33101
CGP 33101

The precise mechanism(s) by which rufinamide exerts its antiepileptic effect is unknown. The results of in vitro studies suggest that 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.

Molecular weight: 238.20
Formula: C10H8F2N4O
CLOGP: 0.51
LIPINSKI: 0
HAC: 5
HDO: 1
TPSA: 73.80
ALOGS: -2.57
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
1.40	g	O

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	85 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	191.92 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.75 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
S (Water solubility)	0.03 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Jan. 16, 2007	EMA	Eisai Ltd
Nov. 14, 2008	FDA	EISAI INC

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Seizure	291.38	48.94	99	887	132535	63355501
Drug resistance	183.96	48.94	47	939	22886	63465150
Multiple-drug resistance	96.20	48.94	21	965	5149	63482887
Status epilepticus	92.06	48.94	25	961	15208	63472828
Stillbirth	74.89	48.94	18	968	6732	63481304
Drug ineffective	69.36	48.94	82	904	1044683	62443353
Atonic seizures	52.34	48.94	9	977	630	63487406

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Seizure	211.65	48.85	87	924	104770	34851150
Status epilepticus	163.37	48.85	43	968	12571	34943349
Multiple-drug resistance	123.94	48.85	29	982	5210	34950710
Tonic convulsion	88.46	48.85	17	994	1184	34954736
Petit mal epilepsy	77.82	48.85	18	993	3060	34952860
Epilepsy	68.27	48.85	25	986	21470	34934450
Aggression	66.70	48.85	29	982	38935	34916985
Drug ineffective	56.48	48.85	67	944	456684	34499236

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Seizure	254.93	42.26	106	1484	188728	79554070
Status epilepticus	243.52	42.26	63	1527	24978	79717820
Drug resistance	172.45	42.26	54	1536	42159	79700639
Multiple-drug resistance	156.21	42.26	36	1554	8772	79734026
Tonic convulsion	102.44	42.26	20	1570	2200	79740598
Epilepsy	86.58	42.26	32	1558	40828	79701970
Petit mal epilepsy	78.40	42.26	19	1571	5708	79737090
Drug ineffective	63.19	42.26	91	1499	1080822	78661976
Aggression	56.27	42.26	25	1565	50933	79691865
Stillbirth	53.50	42.26	13	1577	3942	79738856

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N03AF03	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Carboxamide derivatives
MeSH PA	D000927	Anticonvulsants
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D026941	Sodium Channel Blockers
MeSH PA	D061567	Voltage-Gated Sodium Channel Blockers

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Lennox-Gastaut syndrome	indication	230418006
Atypical absence seizure	off-label use	23374007
Atonic seizure	off-label use	42365007
Absence seizure	off-label use	79631006
Suicidal thoughts	contraindication	6471006
Depressive disorder	contraindication	35489007
Hepatic failure	contraindication	59927004
Shortened QT interval	contraindication	77867006
Leukopenia	contraindication	84828003	DOID:615
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.56	acidic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Sodium channel alpha subunit	Ion channel	P35498 P35499 Q01118 Q14524 Q15858 Q99250 Q9NY46 Q9UI33 Q9UQD0 Q9Y5Y9	SCN1A_HUMAN SCN4A_HUMAN SCN7A_HUMAN SCN5A_HUMAN SCN9A_HUMAN SCN2A_HUMAN SCN3A_HUMAN SCNBA_HUMAN SCN8A_HUMAN SCNAA_HUMAN	BLOCKER				CHEMBL	CHEMBL
Carbonic anhydrase 5A, mitochondrial	Enzyme	P35218	CAH5A_HUMAN		Ki	6.46		CHEMBL

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External reference:

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ID	Source
012301	NDDF
129228	PUBCHEM_CID
158992	MMSL
24915	MMSL
340515	MMSL
4025270	VUID
4025270	VANDF
429802008	SNOMEDCT_US
429835003	SNOMEDCT_US
69036	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	62856-582	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	62856-582	TABLET, FILM COATED	200 mg	ORAL	NDA	33 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	62856-583	TABLET, FILM COATED	400 mg	ORAL	NDA	33 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	62856-583	TABLET, FILM COATED	400 mg	ORAL	NDA	33 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	62856-584	SUSPENSION	40 mg	ORAL	NDA	33 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	62856-584	SUSPENSION	40 mg	ORAL	NDA	33 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	68180-797	SUSPENSION	40 mg	ORAL	ANDA	26 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	68180-797	SUSPENSION	40 mg	ORAL	ANDA	26 sections
Banzel	HUMAN PRESCRIPTION DRUG LABEL	1	68180-797	SUSPENSION	40 mg	ORAL	ANDA	26 sections
Rufinamide	HUMAN PRESCRIPTION DRUG LABEL	1	0054-0425	TABLET, FILM COATED	200 mg	ORAL	ANDA	26 sections

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