perampanel Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS 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:

Molecule

Description

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: 4.17
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:

Dose	Unit	Route
8	mg	O

ADMET properties:

Property	Value	Reference
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

Approvals:

Date	Agency	Company	Orphan
Oct. 22, 2012	FDA	EISAI INC
Jan. 23, 2020	PMDA	Eisai Co., Ltd.

FDA Adverse Event Reporting System (Female)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Aggression	372.42	37.79	111	2908	22633	46660410
Seizure	215.68	37.79	120	2899	122934	46560109
Irritability	197.16	37.79	73	2946	28873	46654170
Status epilepticus	193.21	37.79	60	2959	13919	46669124
Multiple-drug resistance	110.78	37.79	27	2992	2538	46680505
Suicidal ideation	106.61	37.79	58	2961	56324	46626719
Epilepsy	105.48	37.79	44	2975	23694	46659349
Mood altered	74.64	37.79	29	2990	12978	46670065
Suicide attempt	67.96	37.79	43	2976	54993	46628050
Psychotic disorder	65.27	37.79	31	2988	22590	46660453
Dizziness	63.87	37.79	93	2926	340321	46342722
Drug resistance	60.09	37.79	27	2992	17341	46665702
Somnolence	50.27	37.79	56	2963	156465	46526578
Drug ineffective	48.81	37.79	123	2896	677715	46005328
Drug interaction	44.65	37.79	60	2959	203034	46480009
Agitation	43.99	37.79	33	2986	55382	46627661
Intentional overdose	41.45	37.79	34	2985	64910	46618133
Generalised tonic-clonic seizure	38.02	37.79	23	2996	27099	46655944

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Aggression	430.42	40.86	152	2656	36755	29912915
Seizure	220.35	40.86	128	2680	98347	29851323
Suicide attempt	154.32	40.86	73	2735	36624	29913046
Status epilepticus	153.03	40.86	52	2756	11020	29938650
Irritability	119.21	40.86	53	2755	22997	29926673
Anger	107.21	40.86	40	2768	11080	29938590
Epilepsy	84.23	40.86	40	2768	20129	29929541
Intentional overdose	79.41	40.86	49	2759	41432	29908238
Homicidal ideation	78.57	40.86	22	2786	2441	29947229
Suicidal ideation	69.96	40.86	43	2765	36071	29913599
Somnolence	64.81	40.86	61	2747	96702	29852968
Pneumonia aspiration	58.33	40.86	39	2769	37741	29911929
Agitation	54.26	40.86	43	2765	54030	29895640
Multiple-drug resistance	53.39	40.86	17	2791	2924	29946746
Abnormal behaviour	48.28	40.86	30	2778	25593	29924077
Psychotic disorder	47.79	40.86	28	2780	21487	29928183
Sudden unexplained death in epilepsy	44.74	40.86	10	2798	440	29949230

Pharmacologic Action:

Source	Code	Description
ATC	N03AX22	NERVOUS SYSTEM ANTIEPILEPTICS ANTIEPILEPTICS Other antiepileptics
FDA MoA	N0000020016	AMPA Receptor Antagonists
FDA EPC	N0000186106	Noncompetitive AMPA Glutamate Receptor Antagonist
CHEBI has role	CHEBI:35623	antiepileptic
CHEBI has role	CHEBI:71014	alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor antagonist

Drug Use (View source of the data)

Disease	Relation	SNOMED_ID	DOID
Partial seizure	indication	29753000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	3.89	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Glutamate receptor ionotropic AMPA	Ion channel	P42261 P42262 P42263 P48058	GRIA1_HUMAN GRIA2_HUMAN GRIA3_HUMAN GRIA4_HUMAN	ANTAGONIST	IC50	6.61		CHEMBL	CHEMBL

External reference:

ID	Source
D08964	KEGG_DRUG
4032964	VUID
N0000189940	NUI
4032964	VANDF
C4721962	UMLSCUI
CHEBI:71013	CHEBI
6ZP	PDB_CHEM_ID
CHEMBL1214124	ChEMBL_ID
DB08883	DRUGBANK_ID
C551441	MESH_SUPPLEMENTAL_RECORD_UI
9924495	PUBCHEM_CID
7050	IUPHAR_LIGAND_ID
8834	INN_ID
H821664NPK	UNII
1356552	RXNORM
192918	MMSL
28817	MMSL
d07904	MMSL
014644	NDDF
703127006	SNOMEDCT_US
703728005	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-272	TABLET	2 mg	ORAL	NDA	35 sections
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-274	TABLET	4 mg	ORAL	NDA	35 sections
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-276	TABLET	6 mg	ORAL	NDA	35 sections
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-278	TABLET	8 mg	ORAL	NDA	35 sections
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-280	TABLET	10 mg	ORAL	NDA	35 sections
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-282	TABLET	12 mg	ORAL	NDA	35 sections
Fycompa	HUMAN PRESCRIPTION DRUG LABEL	1	62856-290	SUSPENSION	0.50 mg	ORAL	NDA	35 sections