perampanel indications/contra

Stem definitionDrug idCAS RN
antagonists of the ionotropic non-NMDA (N-methyl-D-aspartate) glutamate receptors (Namely the AMPA (amino-hydroxymethyl-isoxazole-propionic acid) and/or KA (kainite antagonist) receptors) 4684 380917-97-5

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • perampanel
  • fycompa
  • E2007
  • E-2007
a non-competitive AMPA glutamate receptor antagonist indicated as adjunctive therapy for the treatment of seizures
  • Molecular weight: 349.39
  • Formula: C23H15N3O
  • CLOGP: 4.17
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 56.99
  • ALOGS: -4.80
  • ROTB: 3

Drug dosage:

DoseUnitRoute
8 mg O

Approvals:

DateAgencyCompanyOrphan
Oct. 22, 2012 FDA EISAI INC

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Aggression 510.81 68.14 108 649 11277 3373825
Irritability 247.52 68.14 60 697 11156 3373946
Seizure 207.13 68.14 69 688 40331 3344771
Suicide attempt 130.32 68.14 39 718 15808 3369294
Suicidal ideation 130.31 68.14 40 717 17665 3367437
Somnolence 125.52 68.14 45 712 32159 3352943
Status epilepticus 114.89 68.14 26 731 3509 3381593
Homicidal ideation 113.54 68.14 21 736 1036 3384066
Dizziness 109.02 68.14 52 705 76460 3308642
Psychotic disorder 91.54 68.14 26 731 8708 3376394
Agitation 89.78 68.14 31 726 19675 3365427
Anger 82.99 68.14 21 736 4530 3380572
Intentional overdose 77.30 68.14 26 731 15199 3369903
Abnormal behaviour 75.01 68.14 23 734 10005 3375097
Sudden unexplained death in epilepsy 69.20 68.14 11 746 216 3384886

Pharmacologic Action:

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SourceCodeDescription
ATC N03AX22 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Other antiepileptics
FDA EPC N0000186106 Noncompetitive AMPA Glutamate Receptor Antagonist
FDA MoA N0000020016 AMPA Receptor Antagonists
CHEBI has role CHEBI:35623 anticonvulsant

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Partial seizure indication 29753000 DOID:2234

Acid dissociation constants calculated using MoKa v3.0.0

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Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.89 Basic

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
10MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
10MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
10MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY
12MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
12MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
12MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY
2MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
2MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
2MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY
4MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
4MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
4MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY
6MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
6MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
6MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY
8MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
8MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
8MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY
0.5MG/ML FYCOMPA EISAI INC N208277 April 29, 2016 RX SUSPENSION ORAL 6949571 June 8, 2021 TREATMENT OF EPILEPSY
0.5MG/ML FYCOMPA EISAI INC N208277 April 29, 2016 RX SUSPENSION ORAL 6949571 June 8, 2021 TREATMENT OF PARTIAL-ONSET SEIZURES WITH OR WITHOUT SECONDARILY GENERALIZED SEIZURES IN PATIENTS WITH EPILEPSY
0.5MG/ML FYCOMPA EISAI INC N208277 April 29, 2016 RX SUSPENSION ORAL 6949571 June 8, 2021 TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC SEIZURES AS ADJUNCTIVE THERAPY IN PATIENTS WITH EPILEPSY

Orange Book exclusivity data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
10MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL June 19, 2018 ADJUNCTIVE THERAPY FOR THE TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC (PG TC) SEIZURES IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE OR OLDER.
12MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL June 19, 2018 ADJUNCTIVE THERAPY FOR THE TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC (PG TC) SEIZURES IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE OR OLDER.
2MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL June 19, 2018 ADJUNCTIVE THERAPY FOR THE TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC (PG TC) SEIZURES IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE OR OLDER.
4MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL June 19, 2018 ADJUNCTIVE THERAPY FOR THE TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC (PG TC) SEIZURES IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE OR OLDER.
6MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL June 19, 2018 ADJUNCTIVE THERAPY FOR THE TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC (PG TC) SEIZURES IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE OR OLDER.
8MG FYCOMPA EISAI INC N202834 Oct. 22, 2012 RX TABLET ORAL June 19, 2018 ADJUNCTIVE THERAPY FOR THE TREATMENT OF PRIMARY GENERALIZED TONIC-CLONIC (PG TC) SEIZURES IN PATIENTS WITH EPILEPSY 12 YEARS OF AGE OR OLDER.

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glutamate receptor ionotropic AMPA Ion channel ANTAGONIST IC50 6.61 CHEMBL CHEMBL

External reference:

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IDSource
7050 IUPHAR_LIGAND_ID
D08964 KEGG_DRUG
4032964 VUID
N0000189940 NUI
C2698764 UMLSCUI
CHEMBL1214124 ChEMBL_ID
C551441 MESH_SUPPLEMENTAL_RECORD_UI
DB08883 DRUGBANK_ID
H821664NPK UNII
8834 INN_ID
014644 NDDF
1356552 RXNORM
28817 MMSL
d07904 MMSL
4032964 VANDF
N0000189940 NDFRT
703127006 SNOMEDCT_US
703728005 SNOMEDCT_US
9924495 PUBCHEM_CID
CHEBI:71013 CHEBI
6ZP PDB_CHEM_ID

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 60213-290 SUSPENSION 0.50 mg ORAL Approved Drug Product Manufactured Under Contract 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-272 TABLET 2 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-274 TABLET 4 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-276 TABLET 6 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-278 TABLET 8 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-280 TABLET 10 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-282 TABLET 12 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-290 SUSPENSION 0.50 mg ORAL NDA 21 sections