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], [2]
Pediatric lennox-gastaut syndrome 8A62.1 Approved [3]
Seizure disorder 8A6Z Approved [1], [4], [5]
Drug Type
Small molecular drug
Structure
3D MOL 2D MOL
#Ro5 Violations (Lipinski): 0 Molecular Weight (mw) 238.19
Topological Polar Surface Area (xlogp) 0.7
Rotatable Bond Count (rotbonds) 3
Hydrogen Bond Donor Count (hbonddonor) 1
Hydrogen Bond Acceptor Count (hbondacc) 5
ADMET Property
BDDCS Class
Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [6]
Bioavailability
85% of drug becomes completely available to its intended biological destination(s) [7]
Elimination
1% of drug is excreted from urine in the unchanged form [6]
Half-life
The concentration or amount of drug in body reduced by one-half in 6 - 10 hours [8]
Metabolism
The drug is metabolized via the carboxyesterases into inactive metabolite CGP 47292 [9]
MRTD
The Maximum Recommended Therapeutic Dose (MRTD) of drug that ensured maximising efficacy and moderate side effect is 191.9156 micromolar/kg/day [10]
Vd
The volume of distribution (Vd) of drug is 50 L [11]
Water Solubility
The ability of drug to dissolve in water is measured as 0.059 mg/mL [6]
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

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 [12]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Carboxylesterase 1 (CES1) DEB30C5 EST1_HUMAN Substrate [13]
Carboxylesterase 2 (CES2) DETHCPD EST2_HUMAN Substrate [13]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

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] [36]
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] [37]
Gilteritinib DMWQ4MZ Moderate Increased metabolism of Rufinamide caused by Gilteritinib mediated induction of CYP450 enzyme. Acute myeloid leukaemia [2A60] [38]
Oliceridine DM6MDCF Moderate Increased metabolism of Rufinamide caused by Oliceridine mediated induction of CYP450 enzyme. Acute pain [MG31] [39]
Ivabradine DM0L594 Moderate Increased metabolism of Rufinamide caused by Ivabradine mediated induction of CYP450 enzyme. Angina pectoris [BA40] [36]
Bedaquiline DM3906J Moderate Increased metabolism of Rufinamide caused by Bedaquiline mediated induction of CYP450 enzyme. Antimicrobial drug resistance [MG50-MG52] [40]
LY2835219 DM93VBZ Moderate Increased metabolism of Rufinamide caused by LY2835219 mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [41]
Tucatinib DMBESUA Moderate Increased metabolism of Rufinamide caused by Tucatinib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [42]
Palbociclib DMD7L94 Moderate Increased metabolism of Rufinamide caused by Palbociclib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [43]
Alpelisib DMEXMYK Moderate Increased metabolism of Rufinamide caused by Alpelisib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [44]
Bosutinib DMTI8YE Moderate Increased metabolism of Rufinamide caused by Bosutinib mediated induction of CYP450 enzyme. Breast cancer [2C60-2C6Y] [45]
Macitentan DMP79A1 Moderate Increased metabolism of Rufinamide caused by Macitentan mediated induction of CYP450 enzyme. Cardiovascular disease [BA00-BE2Z] [46]
Doxercalciferol DM6FG1P Moderate Increased metabolism of Rufinamide caused by Doxercalciferol mediated induction of CYP450 enzyme. Chronic kidney disease [GB61] [47]
PF-04449913 DMSB068 Moderate Increased metabolism of Rufinamide caused by PF-04449913 mediated induction of CYP450 enzyme. Chronic myelomonocytic leukaemia [2A40] [48]
Levomilnacipran DMV26S8 Moderate Antagonize the effect of Rufinamide when combined with Levomilnacipran. Chronic pain [MG30] [49]
Levonorgestrel DM1DP7T Moderate Increased metabolism of Rufinamide caused by Levonorgestrel mediated induction of CYP450 enzyme. Contraceptive management [QA21] [43]
Ulipristal DMBNI20 Moderate Increased metabolism of Rufinamide caused by Ulipristal mediated induction of CYP450 enzyme. Contraceptive management [QA21] [36]
Osilodrostat DMIJC9X Moderate Increased metabolism of Rufinamide caused by Osilodrostat mediated induction of CYP450 enzyme. Cushing syndrome [5A70] [50]
Ivacaftor DMZC1HS Moderate Increased metabolism of Rufinamide caused by Ivacaftor mediated induction of CYP450 enzyme. Cystic fibrosis [CA25] [51]
Vilazodone DM4LECQ Moderate Antagonize the effect of Rufinamide when combined with Vilazodone. Depression [6A70-6A7Z] [49]
Vortioxetine DM6F1PU Moderate Antagonize the effect of Rufinamide when combined with Vortioxetine. Depression [6A70-6A7Z] [49]
Desvenlafaxine DMHD4PE Moderate Antagonize the effect of Rufinamide when combined with Desvenlafaxine. Depression [6A70-6A7Z] [49]
Esketamine DMVU687 Moderate Additive CNS depression effects by the combination of Rufinamide and Esketamine. Depression [6A70-6A7Z] [43]
Bay 80-6946 DMLOS5R Moderate Increased metabolism of Rufinamide caused by Bay 80-6946 mediated induction of CYP450 enzyme. Follicular lymphoma [2A80] [52]
Mirabegron DMS1GYT Minor Increased metabolism of Rufinamide caused by Mirabegron mediated induction of CYP450 enzyme. Functional bladder disorder [GC50] [53]
Ripretinib DM958QB Moderate Increased metabolism of Rufinamide caused by Ripretinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [43]
Avapritinib DMK2GZX Moderate Increased metabolism of Rufinamide caused by Avapritinib mediated induction of CYP450 enzyme. Gastrointestinal stromal tumour [2B5B] [36]
Boceprevir DMBSHMF Moderate Increased metabolism of Rufinamide caused by Boceprevir mediated induction of CYP450 enzyme. Hepatitis virus infection [1E50-1E51] [54]
MK-1439 DM215WE Moderate Increased metabolism of Rufinamide caused by MK-1439 mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [55]
Cobicistat DM6L4H2 Moderate Increased metabolism of Rufinamide caused by Cobicistat mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [56]
Dolutegravir DMCZGRE Minor Increased metabolism of Rufinamide caused by Dolutegravir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [57]
Elvitegravir DMG9B1U Moderate Increased metabolism of Rufinamide caused by Elvitegravir mediated induction of CYP450 enzyme. Human immunodeficiency virus disease [1C60-1C62] [43]
Levamlodipine DM92S6N Moderate Increased metabolism of Rufinamide caused by Levamlodipine mediated induction of CYP450 enzyme. Hypertension [BA00-BA04] [36]
Tasimelteon DMLOQ1V Moderate Increased metabolism of Rufinamide caused by Tasimelteon mediated induction of CYP450 enzyme. Insomnia [7A00-7A0Z] [58]
Naloxegol DML0B41 Moderate Increased metabolism of Rufinamide caused by Naloxegol mediated induction of CYP450 enzyme. Large intestine motility disorder [DB32] [59]
Pemigatinib DM819JF Moderate Increased metabolism of Rufinamide caused by Pemigatinib mediated induction of CYP450 enzyme. Liver cancer [2C12] [36]
Crizotinib DM4F29C Moderate Increased metabolism of Rufinamide caused by Crizotinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [60]
Brigatinib DM7W94S Moderate Increased metabolism of Rufinamide caused by Brigatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [43]
Ceritinib DMB920Z Moderate Increased metabolism of Rufinamide caused by Ceritinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [61]
Lurbinectedin DMEFRTZ Moderate Increased metabolism of Rufinamide caused by Lurbinectedin mediated induction of CYP450 enzyme. Lung cancer [2C25] [62]
Osimertinib DMRJLAT Moderate Increased metabolism of Rufinamide caused by Osimertinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [63]
Capmatinib DMYCXKL Moderate Increased metabolism of Rufinamide caused by Capmatinib mediated induction of CYP450 enzyme. Lung cancer [2C25] [64]
Artemether DM48QOT Moderate Increased metabolism of Rufinamide caused by Artemether mediated induction of CYP450 enzyme. Malaria [1F40-1F45] [43]
Idelalisib DM602WT Moderate Increased metabolism of Rufinamide caused by Idelalisib mediated induction of CYP450 enzyme. Mature B-cell leukaemia [2A82] [65]
IPI-145 DMWA24P Moderate Increased metabolism of Rufinamide caused by IPI-145 mediated induction of CYP450 enzyme. Mature B-cell leukaemia [2A82] [66]
Acalabrutinib DM7GCVW Moderate Increased metabolism of Rufinamide caused by Acalabrutinib mediated induction of CYP450 enzyme. Mature B-cell lymphoma [2A85] [67]
Ibrutinib DMHZCPO Moderate Increased metabolism of Rufinamide caused by Ibrutinib mediated induction of CYP450 enzyme. Mature B-cell lymphoma [2A85] [68]
Ponatinib DMYGJQO Moderate Increased metabolism of Rufinamide caused by Ponatinib mediated induction of CYP450 enzyme. Mature B-cell lymphoma [2A85] [43]
Vemurafenib DM62UG5 Moderate Increased metabolism of Rufinamide caused by Vemurafenib mediated induction of CYP450 enzyme. Melanoma [2C30] [69]
LGX818 DMNQXV8 Moderate Increased metabolism of Rufinamide caused by LGX818 mediated induction of CYP450 enzyme. Melanoma [2C30] [70]
Allopregnanolone DMNLHAC Moderate Additive CNS depression effects by the combination of Rufinamide and Allopregnanolone. Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z] [71]
Ubrogepant DM749I3 Moderate Increased metabolism of Rufinamide caused by Ubrogepant mediated induction of CYP450 enzyme. Migraine [8A80] [72]
Lasmiditan DMXLVDT Moderate Additive CNS depression effects by the combination of Rufinamide and Lasmiditan. Migraine [8A80] [73]
Panobinostat DM58WKG Moderate Increased metabolism of Rufinamide caused by Panobinostat mediated induction of CYP450 enzyme. Multiple myeloma [2A83] [74]
Ruxolitinib DM7Q98D Moderate Increased metabolism of Rufinamide caused by Ruxolitinib mediated induction of CYP450 enzyme. Myeloproliferative neoplasm [2A20] [75]
Rolapitant DM8XP26 Moderate Increased metabolism of Rufinamide caused by Rolapitant mediated induction of CYP450 enzyme. Nausea/vomiting [MD90] [76]
Entrectinib DMMPTLH Moderate Increased metabolism of Rufinamide caused by Entrectinib mediated induction of CYP450 enzyme. Non-small cell lung cancer [2C25] [77]
Olaparib DM8QB1D Moderate Increased metabolism of Rufinamide caused by Olaparib mediated induction of CYP450 enzyme. Ovarian cancer [2C73] [43]
Macimorelin DMQYJIR Moderate Increased metabolism of Rufinamide caused by Macimorelin mediated induction of CYP450 enzyme. Pituitary gland disorder [5A60-5A61] [78]
Lefamulin DME6G97 Moderate Increased metabolism of Rufinamide caused by Lefamulin mediated induction of CYP450 enzyme. Pneumonia [CA40] [79]
Lonafarnib DMGM2Z6 Moderate Increased metabolism of Rufinamide caused by Lonafarnib mediated induction of CYP450 enzyme. Premature ageing appearance [LD2B] [80]
Enzalutamide DMGL19D Moderate Increased metabolism of Rufinamide caused by Enzalutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [81]
Darolutamide DMV7YFT Moderate Increased metabolism of Rufinamide caused by Darolutamide mediated induction of CYP450 enzyme. Prostate cancer [2C82] [82]
Silodosin DMJSBT6 Moderate Increased metabolism of Rufinamide caused by Silodosin mediated induction of CYP450 enzyme. Prostate hyperplasia [GA90] [43]
Riociguat DMXBLMP Moderate Increased metabolism of Rufinamide caused by Riociguat mediated induction of CYP450 enzyme. Pulmonary hypertension [BB01] [83]
Temsirolimus DMS104F Moderate Increased metabolism of Rufinamide caused by Temsirolimus mediated induction of CYP450 enzyme. Renal cell carcinoma [2C90] [43]
Tofacitinib DMBS370 Moderate Increased metabolism of Rufinamide caused by Tofacitinib mediated induction of CYP450 enzyme. Rheumatoid arthritis [FA20] [43]
Avanafil DM75CXN Moderate Increased metabolism of Rufinamide caused by Avanafil mediated induction of CYP450 enzyme. Sexual dysfunction [HA00-HA01] [84]
LDE225 DMM9F25 Moderate Increased metabolism of Rufinamide caused by LDE225 mediated induction of CYP450 enzyme. Skin cancer [2C30-2C37] [85]
Larotrectinib DM26CQR Moderate Increased metabolism of Rufinamide caused by Larotrectinib mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [43]
Armodafinil DMGB035 Moderate Increased metabolism of Rufinamide caused by Armodafinil mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [86]
LEE011 DMMX75K Moderate Increased metabolism of Rufinamide caused by LEE011 mediated induction of CYP450 enzyme. Solid tumour/cancer [2A00-2F9Z] [43]
Fostamatinib DM6AUHV Moderate Increased metabolism of Rufinamide caused by Fostamatinib mediated induction of CYP450 enzyme. Thrombocytopenia [3B64] [87]
Apixaban DM89JLN Moderate Increased metabolism of Rufinamide caused by Apixaban mediated induction of CYP450 enzyme. Thrombosis [DB61-GB90] [88]
Brilinta DMBR01X Moderate Increased metabolism of Rufinamide caused by Brilinta mediated induction of CYP450 enzyme. Thrombosis [DB61-GB90] [56]
Cabozantinib DMIYDT4 Moderate Increased metabolism of Rufinamide caused by Cabozantinib mediated induction of CYP450 enzyme. Thyroid cancer [2D10] [89]
Elagolix DMB2C0E Moderate Increased metabolism of Rufinamide caused by Elagolix mediated induction of CYP450 enzyme. Uterine fibroid [2E86] [90]
⏷ Show the Full List of 76 DDI Information of This Drug

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
⏷ 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

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63 Product Information. Tagrisso (osimertinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
64 Product Information. Tabrecta (capmatinib). Novartis Pharmaceuticals, East Hanover, NJ.
65 Product Information. Zydelig (idelalisib). Gilead Sciences, Foster City, CA.
66 Product Information. Copiktra (duvelisib). Verastem, Inc., Needham, MA.
67 Product Information. Calquence (acalabrutinib). Astra-Zeneca Pharmaceuticals, Wilmington, DE.
68 Product Information. Imbruvica (ibrutinib). Pharmacyclics Inc, Sunnyvale, CA.
69 Product Information. Zelboraf (vemurafenib). Genentech, South San Francisco, CA.
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72 Product Information. Ubrelvy (ubrogepant). Allergan Inc, Irvine, CA.
73 Product Information. Reyvow (lasmiditan). Lilly, Eli and Company, Indianapolis, IN.
74 Product Information. Farydak (panobinostat). Novartis Pharmaceuticals, East Hanover, NJ.
75 Product Information. Jakafi (ruxolitinib). Incyte Corporation, Wilmington, DE.
76 Product Information. Varubi (rolapitant). Tesaro Inc., Waltham, MA.
77 Product Information. Rozlytrek (entrectinib). Genentech, South San Francisco, CA.
78 Product Information. Macrilen (macimorelin). Aeterna Zentaris, Charleston, SC.
79 Product Information. Xenleta (lefamulin). Nabriva Therapeutics US, Inc., King of Prussia, PA.
80 Product Information. Zokinvy (lonafarnib). Eiger BioPharmaceuticals, Palo Alto, CA.
81 Product Information. Xtandi (enzalutamide). Astellas Pharma US, Inc, Deerfield, IL.
82 Product Information. Nubeqa (darolutamide). Bayer HealthCare Pharmaceuticals Inc., Whippany, NJ.
83 Product Information. Adempas (riociguat). Bayer Pharmaceutical Inc, West Haven, CT.
84 Product Information. Stendra (avanafil). Vivus Inc, Mountain View, CA.
85 Product Information. Odomzo (sonidegib). Novartis Pharmaceuticals, East Hanover, NJ.
86 Product Information. Nuvigil (armodafinil). Cephalon Inc, West Chester, PA.
87 Product Information. Tavalisse (fostamatinib). Rigel Pharmaceuticals, South San Francisco, CA.
88 Product Information. Eliquis (apixaban). Bristol-Myers Squibb Canada Inc, Montreal, IN.
89 Product Information. Cabometyx (cabozantinib). Exelixis Inc, S San Francisco, CA.
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