Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00610)
Name
Rufinamide
Synonyms    Click to Show/Hide the Synonyms of This API
Rufinamide; 106308-44-5; Inovelon; Banzel; 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazole-4-carboxamide; Cgp 33101; CGP-33101; 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-Triazole-4-carboxamide; RUF 331; RUF-331; UNII-WFW942PR79; C10H8F2N4O; 1-[(2,6-difluorophenyl)methyl]triazole-4-carboxamide; E 2080; E-2080; 1H-1,2,3-Triazole-4-carboxamide, 1-[(2,6-difluorophenyl)methyl]-; WFW942PR79; MFCD00865314; NCGC00165883-02; DSSTox_CID_26506; DSSTox_RID_81675; DSSTox_GSID_46506; 1-[(2,6-difluorophenyl)methyl]-1H-1,2,3-triazole-4 carboxamide; 1H-1,2,3-Triazole-4-carboxamide, 1-((2,6-difluorophenyl)methyl)-; SMR000857122; CAS-106308-44-5; Rufinamide [USAN:INN:BAN]; SYN111; SYN-111; CGP33101; Banzel (TN); Rufinamide (Banzel); CGP 33,101; PubChem14896; Rufinamide (JAN/USP/INN); MLS001332513; MLS001332514; SCHEMBL230448; GTPL7470; ZINC7782; CHEMBL1201754; DTXSID1046506; CHEBI:134966; HMS2232M19; HMS3262O14; HMS3371A06; HMS3651O05; HMS3884G07; BCP21828; HY-A0042; Tox21 112267; Tox21_112267; Tox21_500796; BDBM50515492; AKOS005145897; Rufinamide, >=98% (HPLC), powder; Tox21_112267_1; AC-1429; AS07135; CCG-222100; CS-1455; DB06201; LP00796; MCULE-6872329028; SB18904; SDCCGSBI-0633757.P001; NCGC00165883-01; NCGC00165883-03; NCGC00165883-04; NCGC00165883-11; NCGC00261481-01; AS-13861; AB0017630; AK00592772; FT-0656828; FT-0674479; SW219770-1; 1-(2,6-difluorobenzyl)triazole-4-carboxamide; D05775; J10459; W-5135; AB00918347-05; AB00918347_06; 308R445; A801414; Q408565; SR-01000842156; J-001568; SR-01000842156-4; 1-[(2,6-difluorophenyl)methyl]-4-triazolecarboxamide; F0001-2404; Z1541638521; 1-(2,6-Difluorobenzyl)-1H-1,2,3-triazol-4-carboxamide; Rufinamide, United States Pharmacopeia (USP) Reference Standard; 1-[[2,6-bis(fluoranyl)phenyl]methyl]-1,2,3-triazole-4-carboxamide
Clinical Status
Approved
Disease Indication Lennox-gastaut syndrome ICD-11: 8A62 [1]
PubChem CID
129228
Formula
C10H8F2N4O
Canonical SMILES
C1=CC(=C(C(=C1)F)CN2C=C(N=N2)C(=O)N)F
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
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=129228"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 238.19 Topological Polar Surface Area 73.8
XlogP 0.7 Complexity 282
Heavy Atom Count 17 Rotatable Bond Count 3
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 5
Full List of Drug Formulations (DFMs) Containing This API
          Rufinamide 200 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Talc; Titanium dioxide; Carboxymethylcellulose sodium; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Carboxymethylcellulose sodium DIG Info Albendazole monooxygenase (EC50 = 12.6 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Rufinamide 400 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Lactose monohydrate; Sodium lauryl sulfate; Magnesium stearate; Ferric oxide red; Talc; Titanium dioxide; Carboxymethylcellulose sodium; Silicon dioxide; Cellulose, microcrystalline; Hypromelloses; Polyethylene glycols; Starch, corn
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Sodium lauryl sulfate DIG Info Solute carrier SLCO2B1 (Ki = 1.98 uM) [2]
Carboxymethylcellulose sodium DIG Info Albendazole monooxygenase (EC50 = 12.6 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
Silicon dioxide DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved rufinamide from the official website of the U.S. Food and Drug Administration.
2 Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives. Proc Natl Acad Sci U S A. 2020 Jul 7;117(27):16009-16018.
3 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
4 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.

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