Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMJDYNQ)

Drug Name

E-2007 Drug Info

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]
Parkinson disease	8A00.0	Discontinued in Phase 3	[1]

Cross-matching ID

PubChem CID: 9924495
ChEBI ID: CHEBI:71013
CAS Number: CAS 380917-97-5
TTD Drug ID: DMJDYNQ
INTEDE Drug ID: DR1256
ACDINA Drug ID: D00519

Molecule(s) Related to 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	[3]
Glutamate receptor AMPA 2 (GRIA2)	TT9HLZ0	GRIA2_HUMAN	Inhibitor	[3]
Glutamate receptor AMPA 3 (GRIA3)	TT82EZV	GRIA3_HUMAN	Inhibitor	[3]
Glutamate receptor AMPA 4 (GRIA4)	TTPJR0G	GRIA4_HUMAN	Inhibitor	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[4]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[5]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[6]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Glutamate receptor AMPA 1 (GRIA1)	DTT	GRIA1	3.209	3.365	3.194	3.379
Glutamate receptor AMPA (GRIA)	DTT	GRIA	3.07	2.907	2.945	3.485
Glutamate receptor AMPA 2 (GRIA2)	DTT	GRIA2	1.263	0.379	0.848	1.585
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

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 between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7050).
2	Nat Rev Drug Discov. 2013 Feb;12(2):87-90.
3	Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
4	The clinical pharmacology profile of the new antiepileptic drug perampanel: A novel noncompetitive AMPA receptor antagonist. Epilepsia. 2015 Jan;56(1):12-27.
5	Perampanel (Fycompa): a review of clinical efficacy and safety in epilepsy. P T. 2016 Nov;41(11):683-698.
6	FDA label of Perampanel. The 2020 official website of the U.S. Food and Drug Administration.