Details of the Drug

General Information of Drug (ID: DMJDYNQ)

Drug Name

E-2007

Synonyms

Perampanel; E 2007; Perampanel (USAN); 2-(2-oxo-1-phenyl-5-pyridin-2-yl-pyridin-3-yl)benzonitrile; 3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one

Indication

Disease Entry	ICD 11	Status	REF
Diabetic neuropathy	8C0Z	Approved	[1], [2]
Parkinson disease	8A00.0	Discontinued in Phase 3	[1], [3]

Drug Type

Small molecular drug

Structure

3D MOL

2D MOL

#Ro5 Violations (Lipinski): 0

Molecular Weight (mw)

349.4

Topological Polar Surface Area (xlogp)

3.4

Rotatable Bond Count (rotbonds)

Hydrogen Bond Donor Count (hbonddonor)

Hydrogen Bond Acceptor Count (hbondacc)

ADMET Property

Absorption: The drug is rapidly and completely absorbed following oral administration [4]
BDDCS Class: Biopharmaceutics Drug Disposition Classification System (BDDCS) Class 2: low solubility and high permeability [5]
Clearance: The drug present in the plasma can be removed from the body at the rate of 0.1 mL/min/kg [6]
Half-life: The concentration or amount of drug in body reduced by one-half in 105 hours [6]
Metabolism: The drug is metabolized via the CYP3A4 and/or CYP3A5 primary oxidation and by sequential glucuronidation [4]
Unbound Fraction: The unbound fraction of drug in plasma is 0.05% [6]
Vd: Fluid volume that would be required to contain the amount of drug present in the body at the same concentration as in the plasma 1.36 L/kg [6]

Chemical Identifiers

Formula: C23H15N3O
IUPAC Name: 2-(2-oxo-1-phenyl-5-pyridin-2-ylpyridin-3-yl)benzonitrile
Canonical SMILES: C1=CC=C(C=C1)N2C=C(C=C(C2=O)C3=CC=CC=C3C#N)C4=CC=CC=N4
InChI: 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

Cross-matching ID

PubChem CID: 9924495
ChEBI ID: CHEBI:71013
CAS Number: 380917-97-5
DrugBank ID: DB08883
TTD ID: D0U3ED
INTEDE ID: DR1256
ACDINA ID: D00519

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glutamate receptor AMPA (GRIA)	TTAN6JD	NOUNIPROTAC	Modulator	[2]
Glutamate receptor AMPA 1 (GRIA1)	TTVPQTF	GRIA1_HUMAN	Inhibitor	[7]
Glutamate receptor AMPA 2 (GRIA2)	TT9HLZ0	GRIA2_HUMAN	Inhibitor	[7]
Glutamate receptor AMPA 3 (GRIA3)	TT82EZV	GRIA3_HUMAN	Inhibitor	[7]
Glutamate receptor AMPA 4 (GRIA4)	TTPJR0G	GRIA4_HUMAN	Inhibitor	[7]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	MOA	REF
Cytochrome P450 3A4 (CYP3A4)_{Main DME}	DE4LYSA	CP3A4_HUMAN	Substrate	[8]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Substrate	[9]
Cytochrome P450 3A5 (CYP3A5)_{Main DME}	DEIBDNY	CP3A5_HUMAN	Substrate	[10]

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Molecular Interaction Atlas (MIA)

MIA Detail

Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease

Diabetic neuropathy

ICD Disease Classification

8C0Z

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Glutamate receptor AMPA 1 (GRIA1)	DTT	GRIA1	1.46E-06	-0.63	-0.78
Glutamate receptor AMPA (GRIA)	DTT	NO-GeName	1.79E-04	-0.69	-0.58
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	7.36E-01	1.62E-02	1.08E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	9.96E-01	-3.17E-03	-1.84E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.04E-02	6.29E-02	3.54E-01

Molecular Expression Atlas (MEA)

MEA Detail

Jump to Detail Molecular Expression Atlas of This Drug

Drug-Drug Interaction (DDI) Information of This Drug

Coadministration of a Drug Treating the Disease Different from E-2007 (Comorbidity)

DDI Drug Name	DDI Drug ID	Severity	Mechanism	Comorbidity	REF
Ivosidenib	DM8S6T7	Moderate	Increased metabolism of E-2007 caused by Ivosidenib mediated induction of CYP450 enzyme.	Acute myeloid leukaemia [2A60]	[61]
Pexidartinib	DMS2J0Z	Moderate	Increased metabolism of E-2007 caused by Pexidartinib mediated induction of CYP450 enzyme.	Bone/articular cartilage neoplasm [2F7B]	[61]
Levomilnacipran	DMV26S8	Moderate	Antagonize the effect of E-2007 when combined with Levomilnacipran.	Chronic pain [MG30]	[62]
Vortioxetine	DM6F1PU	Moderate	Antagonize the effect of E-2007 when combined with Vortioxetine.	Depression [6A70-6A7Z]	[62]
Esketamine	DMVU687	Moderate	Additive CNS depression effects by the combination of E-2007 and Esketamine.	Depression [6A70-6A7Z]	[63]
Oestradiol valerate and dienogest	DMZK0FQ	Moderate	Increased metabolism of E-2007 caused by Oestradiol valerate and dienogest mediated induction of CYP450 enzyme.	Endometriosis [GA10]	[61]
PF-06463922	DMKM7EW	Moderate	Increased metabolism of E-2007 caused by PF-06463922 mediated induction of CYP450 enzyme.	Lung cancer [2C25]	[61]
Allopregnanolone	DMNLHAC	Moderate	Additive CNS depression effects by the combination of E-2007 and Allopregnanolone.	Mental/behavioural/neurodevelopmental disorder [6E20-6E8Z]	[64]
Lasmiditan	DMXLVDT	Moderate	Additive CNS depression effects by the combination of E-2007 and Lasmiditan.	Migraine [8A80]	[65]
Elagolix	DMB2C0E	Moderate	Increased metabolism of E-2007 caused by Elagolix mediated induction of CYP450 enzyme.	Uterine fibroid [2E86]	[61]
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⏷ Show the Full List of 10 DDI Information of This Drug

Drug Inactive Ingredient(s) (DIG) and Formulation(s) of This Drug

DIG

DIG Name	DIG ID	PubChem CID	Functional Classification
FD&C blue no. 2	E00446	2723854	Colorant
Eisenoxyd	E00585	56841934	Colorant
Ferric hydroxide oxide yellow	E00539	23320441	Colorant
Ferrosoferric oxide	E00231	14789	Colorant
Lactose monohydrate	E00393	104938	Binding agent; Diluent; Dry powder inhaler carrier; Lyophilization aid
Magnesium stearate	E00208	11177	lubricant
Povidone	E00667	Not Available	Binding agent; Coating agent; Disintegrant; Film/membrane-forming agent; Solubilizing agent; Suspending agent
Talc	E00520	16211421	Anticaking agent; Diluent; Glidant; lubricant
Titanium dioxide	E00322	26042	Coating agent; Colorant; Opacifying agent
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⏷ Show the Full List of 9 Pharmaceutical Excipients of This Drug

Pharmaceutical Formulation

Formulation Name	Drug Dosage	Dosage Form	Route
Perampanel 10 mg tablet	10 mg	Oral Tablet	Oral
Perampanel 12 mg tablet	12 mg	Oral Tablet	Oral
Perampanel 2 mg tablet	2 mg	Oral Tablet	Oral
Perampanel 8 mg tablet	8 mg	Oral Tablet	Oral
Perampanel 4 mg tablet	4 mg	Oral Tablet	Oral
Perampanel 6 mg tablet	6 mg	Oral Tablet	Oral

Jump to Detail Pharmaceutical Formulation Page of This Drug

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