Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D00519)
Name
Perampanel
Synonyms    Click to Show/Hide the Synonyms of This API
Perampanel; 380917-97-5; Fycompa; ER-155055-90; 3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one; E 2007; E-2007; UNII-H821664NPK; CHEBI:71013; Benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)-; H821664NPK; Fycompa (TN); C23H15N3O; 2-(2-oxo-1-phenyl-5-pyridin-2-ylpyridin-3-yl)benzonitrile; 5'-(2-cyanophenyl)-1'-phenyl-2,3'-bipyridinyl-6'(1'H)-one; 2-(6'-oxo-1'-phenyl-1',6'-dihydro-2,3'-bipyridin-5'-yl)benzonitrile; 2-(6'-Oxo-1'-Phenyl[1',6'-Dihydro[2,3'-Bipyridine]]-5'-Yl)benzonitrile; Perampanel (USAN); Perampanel [USAN:INN]; perampanelum; Benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl(2,3'-bipyridin)-5'-yl)-; Perampanel(E2007; SCHEMBL194370; GTPL7050; CHEMBL1214124; DTXSID80191501; AOB87762; BCP06505; EX-A2128; 3964AH; BDBM50184410; ZINC30691797; AKOS016340421; CH-0056; CS-1160; DB08883; SB16816; NCGC00378863-02; AC-27375; AM806751; HY-14745; D08964; W-5817; Q868658; 2-(6-Oxo-1-phenyl-1,6-dihydro-[2,3-bipyridin]-5-yl)benzonitrile; 3-(2-Cyanophenyl)-1-phenyl-5-(2-pyridyl)-1,2-dihydropyridin-2-one; 1174302-51-2
Clinical Status
Approved
Disease Indication Focal seizure ICD-11: 8A68 [1]
PubChem CID
9924495
Formula
C23H15N3O
Canonical SMILES
C1=CC=C(C=C1)N2C=C(C=C(C2=O)C3=CC=CC=C3C#N)C4=CC=CC=N4
InChI
1S/C23H15N3O/c24-15-17-8-4-5-11-20(17)21-14-18(22-12-6-7-13-25-22)16-26(23(21)27)19-9-2-1-3-10-19/h1-14,16H
InChIKey
PRMWGUBFXWROHD-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=9924495"></iframe>
3D MOL 2D MOL
Physicochemical Properties Molecular Weight 349.4 Topological Polar Surface Area 57
XlogP 3.4 Complexity 664
Heavy Atom Count 27 Rotatable Bond Count 3
Hydrogen Bond Donor Count 0 Hydrogen Bond Acceptor Count 3
Full List of Drug Formulations (DFMs) Containing This API
          Perampanel 10 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; Fd&c blue no. 2; Magnesium stearate; Ferric oxide yellow; Talc; Titanium dioxide; Povidone; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Perampanel 12 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; Fd&c blue no. 2; Magnesium stearate; Talc; Titanium dioxide; Povidone; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
FD&C blue no. 2 DIG Info Adenosine receptor A3 (IC50 = 1 uM) [2]
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Perampanel 2 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; Magnesium stearate; Ferric oxide red; Ferric oxide yellow; Talc; Titanium dioxide; Povidone; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Perampanel 8 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; Magnesium stearate; Ferric oxide red; Ferrosoferric oxide; Talc; Titanium dioxide; Povidone; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Perampanel 4 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; Magnesium stearate; Ferric oxide red; Talc; Titanium dioxide; Povidone; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
          Perampanel 6 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; Magnesium stearate; Ferric oxide red; Talc; Titanium dioxide; Povidone; Cellulose, microcrystalline; Hydroxypropyl cellulose (type h); Hypromelloses; Polyethylene glycol 8000
                   Dosage Form Oral Tablet
                   Company Eisai
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Povidone DIG Info Cholesterol 25-hydroxylase (IC50 = 78.3 uM) [3]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [4]
References
1 FDA label for approved perampanel from the official website of the U.S. Food and Drug Administration.
2 The activities of drug inactive ingredients on biological targets. Science. 2020 Jul 24;369(6502):403-413.
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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