Details of the Drug

General Information of Drug (ID: DMWE60C)

Drug Name

Rufinamide

Synonyms

106308-44-5; Inovelon; Banzel; 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide; CGP-33101; Cgp 33101; Xilep; 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-Triazole-4-carboxamide; RUF-331; UNII-WFW942PR79; RUF 331; 1-[(2,6-difluorophenyl)methyl]triazole-4-carboxamide; WFW942PR79; C10H8F2N4O; E 2080; POGQSBRIGCQNEG-UHFFFAOYSA-N; 1H-1,2,3-Triazole-4-carboxamide, 1-[(2,6-difluorophenyl)methyl]-; NCGC00165883-02; E2080; DSSTox_CID_26506; DSSTox_RID_81675; DSSTox_GSID_46506; Banzel; Banzel, Rufinamide; E-2080; SYN-111; Rufinamide (USAN/INN); Inovelon/Banzel

Indication

Disease Entry	ICD 11	Status	REF
Epilepsy	8A60-8A68	Approved (orphan drug)	[1]
Pediatric lennox-gastaut syndrome	8A62.1	Approved	[2]
Seizure disorder	8A6Z	Approved	[1]
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Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

238.19

Logarithm of the Partition Coefficient (xlogp)

0.7

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [3]
Bioavailability: 85% of drug becomes completely available to its intended biological destination(s) [4]
Elimination: 1% of drug is excreted from urine in the unchanged form [3]
Half-life: The concentration or amount of drug in body reduced by one-half in 6 - 10 hours [5]
Metabolism: The drug is metabolized via the carboxyesterases into inactive metabolite CGP 47292 []
MRTD: The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 191.9156 micromolar/kg/day [6]
Vd: The volume of distribution (Vd) of drug is 50 L []
Water Solubility: The ability of drug to dissolve in water is measured as 0.059 mg/mL [3]

Chemical Identifiers

Formula: C10H8F2N4O
IUPAC Name: 1-[(2,6-difluorophenyl)methyl]triazole-4-carboxamide
Canonical SMILES: C1=CC(=C(C(=C1)F)CN2C=C(N=N2)C(=O)N)F
InChI: 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)
InChIKey: POGQSBRIGCQNEG-UHFFFAOYSA-N

Cross-matching ID

PubChem CID: 129228
ChEBI ID: CHEBI:134966
CAS Number: 106308-44-5
DrugBank ID: DB06201
TTD ID: D0MD2L
INTEDE ID: DR1450
ACDINA ID: D00610

Combinatorial Drugs (CBD)

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Repurposed Drugs (RPD)

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Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Sodium channel unspecific (NaC)	TTRK8B9	NOUNIPROTAC	Blocker	[7]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Carboxylesterase 1 (CES1)	DEB30C5	EST1_HUMAN	Substrate	[8]
Carboxylesterase 2 (CES2)	DETHCPD	EST2_HUMAN	Substrate	[8]

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Molecular Interaction Atlas (MIA)

MIA Detail

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Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Same Disease as Rufinamide

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Disease	REF
Stiripentol	DMMSDOY	Moderate	Increased metabolism of Rufinamide caused by Stiripentol mediated induction of CYP450 enzyme.	Epilepsy/seizure [8A61-8A6Z]	[9]
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Coadministration of a Drug Treating the Disease Different from Rufinamide (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Midostaurin	DMI6E0R	Moderate	Increased metabolism of Rufinamide caused by Midostaurin mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[10]
Gilteritinib	DMTI0ZO	Moderate	Increased metabolism of Rufinamide caused by Gilteritinib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[11]
Oliceridine	DM6MDCF	Moderate	Increased metabolism of Rufinamide caused by Oliceridine mediated induction of CYP450 enzyme.	Acute pain [MG31]	[12]
Ivabradine	DM0L594	Moderate	Increased metabolism of Rufinamide caused by Ivabradine mediated induction of CYP450 enzyme.	Angina pectoris [BA40]	[9]
Bedaquiline	DM3906J	Moderate	Increased metabolism of Rufinamide caused by Bedaquiline mediated induction of CYP450 enzyme.	Antimicrobial drug resistance [MG50-MG52]	[13]
LY2835219	DM93VBZ	Moderate	Increased metabolism of Rufinamide caused by LY2835219 mediated induction of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[14]
Tucatinib	DMBESUA	Moderate	Increased metabolism of Rufinamide caused by Tucatinib mediated induction of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[15]
Palbociclib	DMD7L94	Moderate	Increased metabolism of Rufinamide caused by Palbociclib mediated induction of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[16]
Alpelisib	DMEXMYK	Moderate	Increased metabolism of Rufinamide caused by Alpelisib mediated induction of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[17]
Bosutinib	DMTI8YE	Moderate	Increased metabolism of Rufinamide caused by Bosutinib mediated induction of CYP450 enzyme.	Breast cancer [2C60-2C6Y]	[18]
Macitentan	DMP79A1	Moderate	Increased metabolism of Rufinamide caused by Macitentan mediated induction of CYP450 enzyme.	Cardiovascular disease [BA00-BE2Z]	[19]
Doxercalciferol	DM6FG1P	Moderate	Increased metabolism of Rufinamide caused by Doxercalciferol mediated induction of CYP450 enzyme.	Chronic kidney disease [GB61]	[20]
PF-04449913	DMSB068	Moderate	Increased metabolism of Rufinamide caused by PF-04449913 mediated induction of CYP450 enzyme.	Chronic myelomonocytic leukaemia [2A40]	[21]
Levomilnacipran	DMV26S8	Moderate	Antagonize the effect of Rufinamide when combined with Levomilnacipran.	Chronic pain [MG30]	[22]
Levonorgestrel	DM1DP7T	Moderate	Increased metabolism of Rufinamide caused by Levonorgestrel mediated induction of CYP450 enzyme.	Contraceptive management [QA21]	[16]
Ulipristal	DMBNI20	Moderate	Increased metabolism of Rufinamide caused by Ulipristal mediated induction of CYP450 enzyme.	Contraceptive management [QA21]	[9]
Osilodrostat	DMIJC9X	Moderate	Increased metabolism of Rufinamide caused by Osilodrostat mediated induction of CYP450 enzyme.	Cushing syndrome [5A70]	[23]
Ivacaftor	DMZC1HS	Moderate	Increased metabolism of Rufinamide caused by Ivacaftor mediated induction of CYP450 enzyme.	Cystic fibrosis [CA25]	[24]
Vilazodone	DM4LECQ	Moderate	Antagonize the effect of Rufinamide when combined with Vilazodone.	Depression [6A70-6A7Z]	[22]
Vortioxetine	DM6F1PU	Moderate	Antagonize the effect of Rufinamide when combined with Vortioxetine.	Depression [6A70-6A7Z]	[22]
Desvenlafaxine	DMHD4PE	Moderate	Antagonize the effect of Rufinamide when combined with Desvenlafaxine.	Depression [6A70-6A7Z]	[22]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of Rufinamide and Esketamine.	Depression [6A70-6A7Z]	[16]
Bay 80-6946	DMLOS5R	Moderate	Increased metabolism of Rufinamide caused by Bay 80-6946 mediated induction of CYP450 enzyme.	Follicular lymphoma [2A80]	[25]
Mirabegron	DMS1GYT	Minor	Increased metabolism of Rufinamide caused by Mirabegron mediated induction of CYP450 enzyme.	Functional bladder disorder [GC50]	[26]
Ripretinib	DM958QB	Moderate	Increased metabolism of Rufinamide caused by Ripretinib mediated induction of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[16]
Avapritinib	DMK2GZX	Moderate	Increased metabolism of Rufinamide caused by Avapritinib mediated induction of CYP450 enzyme.	Gastrointestinal stromal tumour [2B5B]	[9]
Boceprevir	DMBSHMF	Moderate	Increased metabolism of Rufinamide caused by Boceprevir mediated induction of CYP450 enzyme.	Hepatitis virus infection [1E50-1E51]	[27]
MK-1439	DM215WE	Moderate	Increased metabolism of Rufinamide caused by MK-1439 mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[28]
Cobicistat	DM6L4H2	Moderate	Increased metabolism of Rufinamide caused by Cobicistat mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[29]
Dolutegravir	DMCZGRE	Minor	Increased metabolism of Rufinamide caused by Dolutegravir mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[30]
Elvitegravir	DMG9B1U	Moderate	Increased metabolism of Rufinamide caused by Elvitegravir mediated induction of CYP450 enzyme.	Human immunodeficiency virus disease [1C60-1C62]	[16]
Levamlodipine	DM92S6N	Moderate	Increased metabolism of Rufinamide caused by Levamlodipine mediated induction of CYP450 enzyme.	Hypertension [BA00-BA04]	[9]
Tasimelteon	DMLOQ1V	Moderate	Increased metabolism of Rufinamide caused by Tasimelteon mediated induction of CYP450 enzyme.	Insomnia [7A00-7A0Z]	[31]
Naloxegol	DML0B41	Moderate	Increased metabolism of Rufinamide caused by Naloxegol mediated induction of CYP450 enzyme.	Large intestine motility disorder [DB32]	[32]
Pemigatinib	DM819JF	Moderate	Increased metabolism of Rufinamide caused by Pemigatinib mediated induction of CYP450 enzyme.	Liver cancer [2C12]	[9]
Crizotinib	DM4F29C	Moderate	Increased metabolism of Rufinamide caused by Crizotinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[33]
Brigatinib	DM7W94S	Moderate	Increased metabolism of Rufinamide caused by Brigatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[16]
Ceritinib	DMB920Z	Moderate	Increased metabolism of Rufinamide caused by Ceritinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[34]
Lurbinectedin	DMEFRTZ	Moderate	Increased metabolism of Rufinamide caused by Lurbinectedin mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[35]
Osimertinib	DMRJLAT	Moderate	Increased metabolism of Rufinamide caused by Osimertinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[36]
Capmatinib	DMYCXKL	Moderate	Increased metabolism of Rufinamide caused by Capmatinib mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[37]
Artemether	DM48QOT	Moderate	Increased metabolism of Rufinamide caused by Artemether mediated induction of CYP450 enzyme.	Malaria [1F40-1F45]	[16]
Idelalisib	DM602WT	Moderate	Increased metabolism of Rufinamide caused by Idelalisib mediated induction of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[38]
IPI-145	DMWA24P	Moderate	Increased metabolism of Rufinamide caused by IPI-145 mediated induction of CYP450 enzyme.	Mature B-cell leukaemia [2A82]	[39]
Acalabrutinib	DM7GCVW	Moderate	Increased metabolism of Rufinamide caused by Acalabrutinib mediated induction of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[40]
Ibrutinib	DMHZCPO	Moderate	Increased metabolism of Rufinamide caused by Ibrutinib mediated induction of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[41]
Ponatinib	DMYGJQO	Moderate	Increased metabolism of Rufinamide caused by Ponatinib mediated induction of CYP450 enzyme.	Mature B-cell lymphoma [2A85]	[16]
Vemurafenib	DM62UG5	Moderate	Increased metabolism of Rufinamide caused by Vemurafenib mediated induction of CYP450 enzyme.	Melanoma [2C30]	[42]
LGX818	DMNQXV8	Moderate	Increased metabolism of Rufinamide caused by LGX818 mediated induction of CYP450 enzyme.	Melanoma [2C30]	[43]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of Rufinamide and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[44]
Ubrogepant	DM749I3	Moderate	Increased metabolism of Rufinamide caused by Ubrogepant mediated induction of CYP450 enzyme.	Migraine [8A80]	[45]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of Rufinamide and Lasmiditan.	Migraine [8A80]	[46]
Panobinostat	DM58WKG	Moderate	Increased metabolism of Rufinamide caused by Panobinostat mediated induction of CYP450 enzyme.	Multiple myeloma [2A83]	[47]
Ruxolitinib	DM7Q98D	Moderate	Increased metabolism of Rufinamide caused by Ruxolitinib mediated induction of CYP450 enzyme.	Myeloproliferative neoplasm [2A20]	[48]
Rolapitant	DM8XP26	Moderate	Increased metabolism of Rufinamide caused by Rolapitant mediated induction of CYP450 enzyme.	Nausea/vomiting [MD90]	[49]
Entrectinib	DMMPTLH	Moderate	Increased metabolism of Rufinamide caused by Entrectinib mediated induction of CYP450 enzyme.	Non-small cell lung cancer [2C25]	[50]
Olaparib	DM8QB1D	Moderate	Increased metabolism of Rufinamide caused by Olaparib mediated induction of CYP450 enzyme.	Ovarian cancer [2C73]	[16]
Macimorelin	DMQYJIR	Moderate	Increased metabolism of Rufinamide caused by Macimorelin mediated induction of CYP450 enzyme.	Pituitary gland disorder [5A60-5A61]	[51]
Lefamulin	DME6G97	Moderate	Increased metabolism of Rufinamide caused by Lefamulin mediated induction of CYP450 enzyme.	Pneumonia [CA40]	[52]
Lonafarnib	DMGM2Z6	Moderate	Increased metabolism of Rufinamide caused by Lonafarnib mediated induction of CYP450 enzyme.	Premature ageing appearance [LD2B]	[53]
Enzalutamide	DMGL19D	Moderate	Increased metabolism of Rufinamide caused by Enzalutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[54]
Darolutamide	DMV7YFT	Moderate	Increased metabolism of Rufinamide caused by Darolutamide mediated induction of CYP450 enzyme.	Prostate cancer [2C82]	[55]
Silodosin	DMJSBT6	Moderate	Increased metabolism of Rufinamide caused by Silodosin mediated induction of CYP450 enzyme.	Prostate hyperplasia [GA90]	[16]
Riociguat	DMXBLMP	Moderate	Increased metabolism of Rufinamide caused by Riociguat mediated induction of CYP450 enzyme.	Pulmonary hypertension [BB01]	[56]
Temsirolimus	DMS104F	Moderate	Increased metabolism of Rufinamide caused by Temsirolimus mediated induction of CYP450 enzyme.	Renal cell carcinoma [2C90]	[16]
Tofacitinib	DMBS370	Moderate	Increased metabolism of Rufinamide caused by Tofacitinib mediated induction of CYP450 enzyme.	Rheumatoid arthritis [FA20]	[16]
Avanafil	DM75CXN	Moderate	Increased metabolism of Rufinamide caused by Avanafil mediated induction of CYP450 enzyme.	Sexual dysfunction [HA00-HA01]	[57]
LDE225	DMM9F25	Moderate	Increased metabolism of Rufinamide caused by LDE225 mediated induction of CYP450 enzyme.	Skin cancer [2C30-2C37]	[58]
Larotrectinib	DM26CQR	Moderate	Increased metabolism of Rufinamide caused by Larotrectinib mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[16]
Armodafinil	DMGB035	Moderate	Increased metabolism of Rufinamide caused by Armodafinil mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[59]
LEE011	DMMX75K	Moderate	Increased metabolism of Rufinamide caused by LEE011 mediated induction of CYP450 enzyme.	Solid tumour/cancer [2A00-2F9Z]	[16]
Fostamatinib	DM6AUHV	Moderate	Increased metabolism of Rufinamide caused by Fostamatinib mediated induction of CYP450 enzyme.	Thrombocytopenia [3B64]	[60]
Apixaban	DM89JLN	Moderate	Increased metabolism of Rufinamide caused by Apixaban mediated induction of CYP450 enzyme.	Thrombosis [DB61-GB90]	[61]
Brilinta	DMBR01X	Moderate	Increased metabolism of Rufinamide caused by Brilinta mediated induction of CYP450 enzyme.	Thrombosis [DB61-GB90]	[29]
Cabozantinib	DMIYDT4	Moderate	Increased metabolism of Rufinamide caused by Cabozantinib mediated induction of CYP450 enzyme.	Thyroid cancer [2D10]	[62]
Elagolix	DMB2C0E	Moderate	Increased metabolism of Rufinamide caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[63]
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Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
Sodium lauryl sulfate	E00464	3423265	Emulsifying agent; Modified-release agent; Penetration agent; Solubilizing agent; Surfactant; lubricant
Carboxymethylcellulose sodium	E00621	Not Available	Adsorbent; Binding agent; Disintegrant; Emulsifying agent; Suspending agent; Viscosity-controlling agent
Eisenoxyd	E00585	56841934	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Silicon dioxide	E00670	Not Available	Anticaking agent; Opacifying agent; Viscosity-controlling agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
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⏷ Show the Full List of 8 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Rufinamide 200 mg tablet	200 mg	Oral Tablet	Oral
Rufinamide 400 mg tablet	400 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

References

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50	Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
51	Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
52	Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
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60	Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
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62	Product Information. Cabometyx (cabozantinib). Exelixis Inc, S San Francisco, CA.
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