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

General Information of Drug (ID: DMXOELT)

Drug Name

Midazolam Drug Info

Synonyms

Dazolam; Dormicum; Midanium; Midazolamum; Midosed; Versed; Midazolam Base; Dormicum (TN); Hypnovel (TN); Midacum (TN); Midazolamum [INN-Latin]; Ro 21-3981; Versed (TN); Midazolam (JAN/INN); Midazolam [INN:BAN:JAN]; 4H-Imidazo[1,5-a][1,4]benzodiazepine, 8-chloro-6-(2-fluoro-phenyl)-1-methyl-, (Z)-2-butenedioate; 8-Chlor-6-(2-fluorphenyl)-1-methyl-4H-imidazo(1,5-a)(1,4)benzodiazepin; 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]benzodiazepine; 8-Chloro-6-(2-fluorophenyl)-1-methyl-4H-imidazo[1,5a][1,4]benzodiazepine hydrochloride; 8-Chloro-6-(O-fluorophenyl)-1-methyl-4H-imidazo[1,5-a][1,4]-benzodiazepine; 8-Chloro-6-(o-fluorophenyl)-1-methyl-4H-imidazo(1,5-a)(1,4)benzodiazepine

Indication

Disease Entry	ICD 11	Status	REF
Irritability	MB24	Approved	[1] , [2]
Epilepsy	8A60-8A68	Phase 3	[3]

Therapeutic Class

Hypnotics and Sedatives

Cross-matching ID

PubChem CID: 4192
ChEBI ID: CHEBI:6931
CAS Number: CAS 59467-70-8
TTD Drug ID: DMXOELT
VARIDT Drug ID: DR00684
INTEDE Drug ID: DR1086

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Translocator protein (TSPO)	TTPTXIN	TSPO_HUMAN	Modulator	[4]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[5]

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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	[6]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[7]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Approved	[8]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Approved	[9]
Cytochrome P450 4B1 (CYP4B1)	DEMF740	CP4B1_HUMAN	Approved	[9]

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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
Translocator protein (TSPO)	DTT	TSPO	7.51	8.89	7.64	8.008
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 4B1 (CYP4B1)	DME	CYP4B1	2.202	6.302	4.178	2.036
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

Irritability

ICD Disease Classification

MB24

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Translocator protein (TSPO)	DTT	TSPO	3.93E-10	0.43	1.02
P-glycoprotein 1 (ABCB1)	DTP	P-GP	9.39E-02	1.07E-01	2.80E-01
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	4.88E-01	-1.69E-05	-1.28E-04
Cytochrome P450 4B1 (CYP4B1)	DME	CYP4B1	3.90E-02	5.64E-02	3.35E-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: 3342).
2	FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075154.
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	A novel screening strategy to identify ABCB1 substrates and inhibitors. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jan;379(1):11-26.
6	Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation. Drug Metab Dispos. 2010 Jun;38(6):981-7.
7	In vitro metabolism of midazolam, triazolam, nifedipine, and testosterone by human liver microsomes and recombinant cytochromes p450: role of cyp3a4 and cyp3a5. Drug Metab Dispos. 2003 Jul;31(7):938-44.
8	Further characterization of the expression in liver and catalytic activity of CYP2B6. J Pharmacol Exp Ther. 1998 Sep;286(3):1253-9.
9	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.