perampanel 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

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 hydrate
  • 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: 3.87
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 0
  • TPSA: 56.99
  • ALOGS: -4.80
  • ROTB: 3
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
8 mg O

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 2 Hosey CM, Chan R, Benet LZ
Vd (Volume of distribution) 1.36 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 0.10 mL/min/kg Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma) 0.05 % Lombardo F, Berellini G, Obach RS
t_half (Half-life) 183 hours Lombardo F, Berellini G, Obach RS
BA (Bioavailability) 1 % Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,DDR1,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,PDK4,PIK3CB,PRKDC,SIK2,SIK3 21
kinase-selectivity-class AXL,PDK4 2
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

DateAgencyCompanyOrphan
Jan. 23, 2020 PMDA Eisai Co., Ltd.
Oct. 22, 2012 FDA EISAI INC
July 23, 2012 EMA EISAI GMBH

FDA Adverse Event Reporting System (Female)

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
Multiple-drug resistance 701.17 36.39 154 6906 7622 90613765
Aggression 478.42 36.39 146 6914 26522 90594865
Seizure 439.89 36.39 221 6839 152408 90468979
Status epilepticus 419.57 36.39 122 6938 18752 90602635
Drug ineffective 333.25 36.39 466 6594 1383832 89237555
Irritability 226.34 36.39 90 6970 35572 90585815
Drug resistance 211.35 36.39 82 6978 30367 90591020
Suicidal ideation 186.21 36.39 98 6962 73757 90547630
Somnolence 163.55 36.39 133 6927 208951 90412436
Drug interaction 148.40 36.39 142 6918 276311 90345076
Anticonvulsant drug level increased 143.13 36.39 32 7028 1704 90619683
Off label use 121.83 36.39 265 6795 1101987 89519400
Suicide attempt 114.63 36.39 72 6988 75327 90546060
Psychotic disorder 112.92 36.39 53 7007 31177 90590210
Epilepsy 106.51 36.39 71 6989 82135 90539252
Abnormal behaviour 105.94 36.39 46 7014 22582 90598805
Agitation 104.32 36.39 65 6995 67033 90554354
Intentional overdose 98.02 36.39 71 6989 93763 90527624
Generalised tonic-clonic seizure 95.56 36.39 49 7011 34854 90586533
Drug ineffective for unapproved indication 94.71 36.39 61 6999 66583 90554804
Cerebral salt-wasting syndrome 85.86 36.39 15 7045 217 90621170
Altered state of consciousness 85.54 36.39 44 7016 31488 90589899
Petit mal epilepsy 79.68 36.39 25 7035 4933 90616454
Dizziness 71.91 36.39 148 6912 589136 90032251
Ataxia 69.48 36.39 32 7028 18010 90603377
Anger 67.85 36.39 29 7031 13691 90607696
Cognitive disorder 66.77 36.39 50 7010 69357 90552030
Myoclonic epilepsy 66.43 36.39 17 7043 1610 90619777
Mood altered 64.75 36.39 30 7030 17114 90604273
Partial seizures 62.83 36.39 23 7037 7237 90614150
Pain 62.14 36.39 4 7056 996337 89625050
Rebound effect 57.09 36.39 23 7037 9361 90612026
Atonic seizures 56.24 36.39 13 7047 803 90620584
Hallucination 55.74 36.39 44 7016 65915 90555472
Abortion spontaneous 54.35 36.39 40 7020 54016 90567371
Lipids abnormal 49.98 36.39 10 7050 310 90621077
Seizure cluster 48.03 36.39 10 7050 379 90621008
Arthralgia 40.98 36.39 6 7054 778516 89842871
Dyspnoea 39.61 36.39 10 7050 880945 89740442
Drug withdrawal convulsions 39.12 36.39 11 7049 1489 90619898
Psychomotor hyperactivity 38.00 36.39 19 7041 12794 90608593
Behaviour disorder 37.58 36.39 14 7046 4621 90616766

FDA Adverse Event Reporting System (Male)

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 573.32 32.55 225 6322 43938 42570850
Multiple-drug resistance 423.92 32.55 116 6431 7206 42607582
Seizure 343.62 32.55 219 6328 120342 42494446
Status epilepticus 341.49 32.55 117 6430 15461 42599327
Drug ineffective 234.34 32.55 374 6173 629823 41984965
Epilepsy 188.13 32.55 88 6459 26083 42588705
Suicide attempt 167.21 32.55 98 6449 46002 42568786
Irritability 161.19 32.55 81 6466 28047 42586741
Somnolence 151.52 32.55 144 6403 140961 42473827
Anger 109.91 32.55 49 6498 12969 42601819
Excessive eye blinking 86.34 32.55 20 6527 623 42614165
Intentional overdose 84.37 32.55 67 6480 51389 42563399
Anticonvulsant drug level above therapeutic 84.29 32.55 20 6527 693 42614095
Partial seizures 83.25 32.55 32 6515 5827 42608961
Psychotic disorder 77.62 32.55 51 6496 29157 42585631
Tonic convulsion 76.37 32.55 22 6525 1637 42613151
Off label use 75.38 32.55 241 6306 638094 41976694
Pneumonia aspiration 75.31 32.55 62 6485 50016 42564772
Generalised tonic-clonic seizure 74.86 32.55 48 6499 26331 42588457
Petit mal epilepsy 74.37 32.55 26 6521 3624 42611164
Ataxia 73.86 32.55 40 6507 16085 42598703
Homicidal ideation 73.05 32.55 24 6523 2770 42612018
Suicidal ideation 62.91 32.55 55 6492 48106 42566682
Gaze palsy 60.61 32.55 19 6528 1886 42612902
Agitation 58.31 32.55 60 6487 64254 42550534
Focal dyscognitive seizures 56.74 32.55 17 6530 1450 42613338
Posture abnormal 55.38 32.55 19 6528 2502 42612286
Drug interaction 54.74 32.55 124 6423 266875 42347913
Sudden unexplained death in epilepsy 53.07 32.55 13 6534 516 42614272
Hyperammonaemia 51.99 32.55 25 6522 7841 42606947
Behaviour disorder 51.47 32.55 24 6523 7030 42607758
Drug withdrawal convulsions 49.58 32.55 15 6532 1323 42613465
Abnormal behaviour 48.88 32.55 37 6510 26414 42588374
Physical assault 43.85 32.55 13 6534 1069 42613719
Altered state of consciousness 43.48 32.55 36 6511 29223 42585565
Haematuria traumatic 42.46 32.55 10 6537 335 42614453
Intensive care unit acquired weakness 41.72 32.55 13 6534 1265 42613523
Postictal paralysis 41.58 32.55 10 6537 367 42614421
Dyspnoea 41.06 32.55 9 6538 442612 42172176
Cognitive disorder 40.58 32.55 37 6510 34135 42580653
Muscle contracture 40.24 32.55 13 6534 1422 42613366
Anticonvulsant drug level increased 38.51 32.55 13 6534 1630 42613158
Seizure cluster 38.41 32.55 9 6538 295 42614493
Drug level decreased 38.18 32.55 22 6525 9955 42604833
Dysarthria 34.01 32.55 36 6511 39771 42575017
Quadriparesis 33.96 32.55 13 6534 2337 42612451

FDA Adverse Event Reporting System (Geriatric)

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
Multiple-drug resistance 996.66 29.96 243 12315 12992 110563749
Aggression 922.84 29.96 319 12239 58891 110517850
Seizure 663.36 29.96 373 12185 220812 110355929
Status epilepticus 625.63 29.96 204 12354 31367 110545374
Drug ineffective 468.20 29.96 703 11855 1519837 109056904
Somnolence 327.25 29.96 270 12288 297179 110279562
Irritability 311.39 29.96 137 12421 47672 110529069
Suicide attempt 247.20 29.96 151 12407 103243 110473498
Epilepsy 246.39 29.96 149 12409 100060 110476681
Suicidal ideation 196.31 29.96 126 12432 93811 110482930
Off label use 195.76 29.96 484 12074 1499701 109077040
Drug resistance 184.38 29.96 101 12457 56273 110520468
Petit mal epilepsy 183.23 29.96 57 12501 7490 110569251
Drug interaction 180.29 29.96 251 12307 499932 110076809
Intentional overdose 168.08 29.96 131 12427 132370 110444371
Agitation 154.82 29.96 117 12441 112934 110463807
Generalised tonic-clonic seizure 151.79 29.96 88 12470 54592 110522149
Anger 145.13 29.96 61 12497 18946 110557795
Abnormal behaviour 133.32 29.96 72 12486 38967 110537774
Ataxia 127.06 29.96 64 12494 30044 110546697
Psychotic disorder 125.73 29.96 76 12482 50861 110525880
Anticonvulsant drug level increased 124.53 29.96 34 12524 2824 110573917
Partial seizures 123.41 29.96 47 12511 11302 110565439
Altered state of consciousness 112.22 29.96 74 12484 57552 110519189
Seizure cluster 98.00 29.96 22 12536 811 110575930
Behaviour disorder 97.91 29.96 38 12520 9609 110567132
Tonic convulsion 95.15 29.96 28 12530 3046 110573695
Excessive eye blinking 89.70 29.96 24 12534 1846 110574895
Drug ineffective for unapproved indication 89.70 29.96 82 12476 102756 110473985
Anticonvulsant drug level above therapeutic 88.91 29.96 22 12536 1240 110575501
Pneumonia aspiration 81.24 29.96 70 12488 81163 110495578
Focal dyscognitive seizures 80.69 29.96 26 12532 3823 110572918
Pain 79.99 29.96 8 12550 954947 109621794
Hyperammonaemia 78.62 29.96 36 12522 13696 110563045
Sudden unexplained death in epilepsy 76.80 29.96 18 12540 805 110575936
Cerebral salt-wasting syndrome 76.41 29.96 15 12543 284 110576457
Cognitive disorder 74.79 29.96 69 12489 87442 110489299
Dyspnoea 71.25 29.96 19 12539 1106853 109469888
Drug withdrawal convulsions 70.11 29.96 21 12537 2428 110574313
Postictal paralysis 65.48 29.96 15 12543 606 110576135
Drug level decreased 62.72 29.96 34 12524 18514 110558227
Dizziness 62.15 29.96 197 12361 697996 109878745
Atonic seizures 61.02 29.96 16 12542 1138 110575603
Gaze palsy 59.31 29.96 20 12538 3387 110573354
Arthralgia 59.21 29.96 9 12549 779623 109797118
Myoclonic epilepsy 55.69 29.96 18 12540 2673 110574068
Hostility 55.65 29.96 18 12540 2678 110574063
Posture abnormal 54.14 29.96 20 12538 4418 110572323
Intensive care unit acquired weakness 53.84 29.96 17 12541 2342 110574399
Prescribed underdose 53.00 29.96 50 12508 65124 110511617
Mood altered 50.42 29.96 31 12527 21344 110555397
Homicidal ideation 50.42 29.96 18 12540 3609 110573132
Haematuria traumatic 50.14 29.96 11 12547 364 110576377
Gait disturbance 49.34 29.96 102 12456 278106 110298635
Vagal nerve stimulator implantation 48.68 29.96 10 12548 240 110576501
Physical assault 46.77 29.96 14 12544 1614 110575127
Product administered to patient of inappropriate age 45.79 29.96 21 12537 8015 110568726
Malaise 42.26 29.96 12 12546 671807 109904934
Abdominal pain 41.09 29.96 5 12553 512984 110063757
Partial seizures with secondary generalisation 41.08 29.96 11 12547 848 110575893
Hyperammonaemic encephalopathy 40 29.96 17 12541 5417 110571324
Hallucination, auditory 39.84 29.96 29 12529 26368 110550373
Hallucination 39.48 29.96 53 12505 101379 110475362
Muscle contracture 39.28 29.96 14 12544 2794 110573947
Pruritus 39.23 29.96 9 12549 581551 109995190
Lipids abnormal 38.65 29.96 10 12548 675 110576066
Psychomotor hyperactivity 36.94 29.96 25 12533 20252 110556489
Drug reaction with eosinophilia and systemic symptoms 36.80 29.96 46 12512 82049 110494692
Intellectual disability 35.96 29.96 12 12546 1967 110574774
Disturbance in attention 34.85 29.96 39 12519 61956 110514785
Electroencephalogram abnormal 34.76 29.96 16 12542 6157 110570584
Dysarthria 34.35 29.96 45 12513 84076 110492665
Myoclonus 34.12 29.96 29 12529 32969 110543772
Overdose 33.81 29.96 79 12479 233715 110343026
Rebound effect 33.72 29.96 21 12537 14785 110561956
Abdominal discomfort 33.69 29.96 3 12555 393855 110182886
Delusion 33.38 29.96 25 12533 23730 110553011
Psychomotor skills impaired 32.71 29.96 16 12542 7042 110569699
Diarrhoea 32.11 29.96 50 12508 1139455 109437286
Change in seizure presentation 32.09 29.96 9 12549 825 110575916
Pain in extremity 31.94 29.96 8 12550 487110 110089631
Chest pain 31.83 29.96 3 12555 376372 110200369
Hypernatraemia 30.16 29.96 21 12537 17812 110558929

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC N03AX22 NERVOUS SYSTEM
ANTIEPILEPTICS
ANTIEPILEPTICS
Other antiepileptics
FDA MoA N0000020016 AMPA Receptor Antagonists
FDA MoA N0000182141 Cytochrome P450 3A4 Inhibitors
FDA EPC N0000186106 Noncompetitive AMPA Glutamate Receptor Antagonist
FDA MoA N0000187062 Cytochrome P450 2C8 Inhibitors
FDA MoA N0000191273 UGT2B7 Inhibitors
FDA MoA N0000191278 UGT1A9 Inhibitors
CHEBI has role CHEBI:35469 antidepressant
CHEBI has role CHEBI:35476 antipsychotic agent
CHEBI has role CHEBI:35623 anticonvulsant
CHEBI has role CHEBI:48407 antiparkinson drug
CHEBI has role CHEBI:71014 AMPA receptor antagonist

Related Drugs by ATC class:

N03AX Other antiepileptics 18 drugs
beclamidebrivaracetamcannabidiolcarisbamatecenobamatefelbamatefenfluramineganaxolonelacosamidelamotriginelevetiracetamphenacemide show all 18 →

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Secondarily generalized seizures indication 20544001
Partial seizure indication 29753000
Idiopathic generalized epilepsy indication 36803009




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.89 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
0.5MG/ML PERAMPANEL MSN A218152 July 11, 2025 RX SUSPENSION ORAL June 14, 2026 PATENT CHALLENGE

Bioactivity Summary:

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

External reference:

IDSource
D08964 KEGG_DRUG
4032964 VUID
N0000189940 NUI
4032964 VANDF
CHEBI:71013 CHEBI
CHEMBL1214124 ChEMBL_ID
C551441 MESH_SUPPLEMENTAL_RECORD_UI
7050 IUPHAR_LIGAND_ID
8834 INN_ID
DB08883 DRUGBANK_ID
H821664NPK UNII
1356552 RXNORM
192918 MMSL
28817 MMSL
395327 MMSL
d07904 MMSL
014644 NDDF
703127006 SNOMEDCT_US
703728005 SNOMEDCT_US
C2698764 UMLSCUI
6ZP PDB_CHEM_ID
9924495 PUBCHEM_CID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 0480-7062 TABLET, FILM COATED 2 mg ORAL ANDA 30 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 0480-7063 TABLET, FILM COATED 4 mg ORAL ANDA 30 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 0480-7065 TABLET, FILM COATED 6 mg ORAL ANDA 30 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 0480-7066 TABLET, FILM COATED 8 mg ORAL ANDA 30 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 0480-7067 TABLET, FILM COATED 10 mg ORAL ANDA 30 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 0480-7068 TABLET, FILM COATED 12 mg ORAL ANDA 30 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 51672-4204 TABLET, FILM COATED 2 mg ORAL ANDA 36 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 51672-4205 TABLET, FILM COATED 4 mg ORAL ANDA 36 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 51672-4206 TABLET, FILM COATED 6 mg ORAL ANDA 36 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 51672-4207 TABLET, FILM COATED 8 mg ORAL ANDA 36 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 51672-4208 TABLET, FILM COATED 10 mg ORAL ANDA 36 sections
Perampanel HUMAN PRESCRIPTION DRUG LABEL 1 51672-4209 TABLET, FILM COATED 12 mg ORAL ANDA 36 sections
PERAMPANEL HUMAN PRESCRIPTION DRUG LABEL 1 51672-4256 SUSPENSION 0.50 mg ORAL ANDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-272 TABLET 2 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-274 TABLET 4 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-276 TABLET 6 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-278 TABLET 8 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-280 TABLET 10 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-282 TABLET 12 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 62856-290 SUSPENSION 0.50 mg ORAL NDA 38 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-272 TABLET 2 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-274 TABLET 4 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-276 TABLET 6 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-278 TABLET 8 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-280 TABLET 10 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-282 TABLET 12 mg ORAL NDA 21 sections
Fycompa HUMAN PRESCRIPTION DRUG LABEL 1 69616-290 SUSPENSION 0.50 mg ORAL NDA 21 sections
PERAMPANEL Human Prescription Drug Label 1 72205-071 SUSPENSION 0.50 mg ORAL ANDA 30 sections
Perampanel Human Prescription Drug Label 1 72205-221 TABLET, FILM COATED 2 mg ORAL ANDA 29 sections
Perampanel Human Prescription Drug Label 1 72205-222 TABLET, FILM COATED 4 mg ORAL ANDA 29 sections