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

General Information of Drug (ID: DM4PRFC)

Drug Name

Bupivacaine Drug Info

Synonyms

Anekain; Bloqueina; Bucaine; Bupivacaina; Bupivacainum; Bupivan; CBupivacaine; Carbostesin; DepoBupivacaine; Marcaina; Marcaine; Sensorcaine; Bupivacaine Carbonate; Bupivacaine HCL; Bupivacaine HCL KIT; Marcaine HCL; Marcaine Spinal; AH 250; Win 11318; Win 11318 HCl; Bucaine (TN); Bupivacaina [INN-Spanish]; Bupivacaine (INN); Bupivacaine Monohydrochloride, Monohydrate; Bupivacaine [INN:BAN]; Bupivacainum [INN-Latin]; DL-Bupivacaine; DUR-843; Marcain (TN); Marcaine (TN); Sensorcaine (TN); Sensorcaine-MPF; Sensorcaine-MPFSpinal; Transdur-Bupivacaine; Vivacaine (TN); Dl-1-Butyl-2',6'-pipecoloxylidide; (1)-1-Butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide; (inverted exclamation markA)-bupivacaine; 1-Butyl-2',6'-pipecoloxylidide; 1-Butyl-N-(2,6-dimethylphenyl)-2-piperidinecarboxamide; 1-butyl-N-(2,6-dimethylphenyl)piperidine-2-carboxamide

Indication

Disease Entry	ICD 11	Status	REF
Anaesthesia	9A78.6	Approved	[1]
Articular cartilage disorder	FA34.Y	Approved	[2]
Periodontitis	DA0C	Approved	[2]
Pain	MG30-MG3Z	Phase 2	[3]
Chronic pain	MG30	Investigative	[2]
Pruritus	EC90	Investigative	[2]

Therapeutic Class

Anesthetics

Cross-matching ID

PubChem CID: 2474
ChEBI ID: CHEBI:77431
CAS Number: CAS 38396-39-3
TTD Drug ID: DM4PRFC
INTEDE Drug ID: DR0243

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Voltage-gated sodium channel alpha Nav1.8 (SCN10A)	TT90XZ8	SCNAA_HUMAN	Modulator	[4]

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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	[5]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[5]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[5]

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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 sodium channel alpha Nav1.8 (SCN10A)	DTT	SCN10A	6.276	5.928	6.19	6.363
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
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

Anaesthesia

ICD Disease Classification

9A78.6

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Voltage-gated sodium channel alpha Nav1.8 (SCN10A)	DTT	SCN10A	9.89E-01	-0.16	-0.31
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	1.65E-02	-4.37E-02	-7.84E-02
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	1.21E-04	-2.33E-01	-5.09E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	6.90E-01	2.35E-02	7.88E-02

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: 2397).
2	Bupivacaine FDA Label
3	Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
5	Oxidative metabolism of bupivacaine into pipecolylxylidine in humans is mainly catalyzed by CYP3A. Drug Metab Dispos. 2000 Apr;28(4):383-5.