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

General Information of Drug (ID: DMGNYIH)

Drug Name

Retigabine Drug Info

Synonyms

Ezogabine; Potiga; Trobalt; Retigabine [USAN]; D 20443; D 23129; ADD-230001; D-20443; D-23129; GKE-841; KE-0201; Ethyl 2-amino-4-((p-fluorobenzyl)amino)carbanilate; Ethyl N-[2-amino-4-[(4-fluorophenyl)methylamino]phenyl]carbamate; [2-Amino-4-[[(4-fluorophenyl)methyl]amino]phenyl]-carbamate; Ethyl N-(2-amino-4-(4-fluorobenzylamino)phenyl)carbamate hydrochloride; N-(2-Amino-4-(4-fluorobenzylamino)phenyl)carbamic acid ethyl ester; Ethyl (2-amino-4-(((4-fluorophenyl)methyl)amino)phenyl)carbamate; N-(2-Amino-4-(4-fluorobenzylamino)-phenyl) carbamic acid ethyl ester; Carbamic acid, (2-amino-4-(((4-fluorophenyl)methyl)amino)phenyl)-, ethyl ester

Indication

Disease Entry	ICD 11	Status	REF
Behcet disease	4A62	Approved	[1]
Epilepsy	8A60-8A68	Withdrawn from market	[2]

Therapeutic Class

Anticonvulsants

Cross-matching ID

PubChem CID: 121892
ChEBI ID: CHEBI:68584
CAS Number: CAS 150812-12-7
TTD Drug ID: DMGNYIH
VARIDT Drug ID: DR00700
INTEDE Drug ID: DR1407
ACDINA Drug ID: D00263

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated potassium channel Kv7 (KCNQ)	TTQ29KF	NOUNIPROTAC	Activator	[2]
Voltage-gated potassium channel Kv7.3 (KCNQ3)	TTIVDM3	KCNQ3_HUMAN	Modulator	[3]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 1A1 (CYP1A1)	DE6OQ3W	CP1A1_HUMAN	Phase 4	[4]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Phase 4	[5]
UDP-glucuronosyltransferase 1A9 (UGT1A9)	DE85D2P	UD19_HUMAN	Phase 4	[4]
UDP-glucuronosyltransferase 1A3 (UGT1A3)	DEF2WXN	UD13_HUMAN	Phase 4	[4]

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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
Voltage-gated potassium channel Kv7.3 (KCNQ3)	DTT	KCNQ3	4.912	5.057	3.459	6.135
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	5.952	6.384	4.897	6.293

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

Behcet disease

ICD Disease Classification

4A62

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Voltage-gated potassium channel Kv7 (KCNQ)	DTT	NO-GeName	6.24E-01	0.11	0.85
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	4.53E-01	4.14E-02	1.83E-01
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	7.84E-01	-1.03E-01	-4.48E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Clinical pipeline report, company report or official report of GlaxoSmithKline.
2	Antibodies and venom peptides: new modalities for ion channels. Nat Rev Drug Discov. 2019 May;18(5):339-357.
3	The urinary safety profile and secondary renal effects of retigabine (ezogabine): a first-in-class antiepileptic drug that targets KCNQ (K(v)7) potassium channels. Epilepsia. 2012 Apr;53(4):606-12.
4	Retigabine N-glucuronidation and its potential role in enterohepatic circulation. Drug Metab Dispos. 1999 May;27(5):605-12.
5	N-Glucuronidation of the antiepileptic drug retigabine: results from studies with human volunteers, heterologously expressed human UGTs, human liver, kidney, and liver microsomal membranes of Crigler-Najjar type II. Metabolism. 2006 Jun;55(6):711-21.