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

General Information of Drug (ID: DMF0NQR)

Drug Name

Eplerenone Drug Info

Synonyms

Epoxymexrenone; Inspra; Selara; CGP-30083; Inspra (TN); SC-66110; Eplerenone (JAN/USAN/INN); Inspra, Epoxymexrenone, CGP30083, SC-66110,Eplerenone; 7alpha-methoxycarbonyl-3-oxo-9,11alpha-epoxy-17alpha-pregn-4-ene-21,17-carbolactone

Indication

Disease Entry	ICD 11	Status	REF
Heart failure	BD10-BD13	Approved	[1]
Coronavirus Disease 2019 (COVID-19)	1D6Y	Investigative	[2]

Therapeutic Class

Antihypertensive Agents

Cross-matching ID

PubChem CID: 443872
ChEBI ID: CHEBI:31547
CAS Number: CAS 107724-20-9
TTD Drug ID: DMF0NQR
INTEDE Drug ID: DR0592
ACDINA Drug ID: D00235

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Mineralocorticoid receptor (MR)	TT26PHO	MCR_HUMAN	Modulator	[3]
HUMAN mineralocorticoid receptor (MR)	TT9P1CK	MCR_HUMAN	Antagonist	[2]

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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 3A5 (CYP3A5)	DEIBDNY	CP3A5_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
Mineralocorticoid receptor (MR)	DTT	NR3C2	5.85	7.414	6.42	7.379
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

Heart failure

ICD Disease Classification

BD10-BD13

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Mineralocorticoid receptor (MR)	DTT	NR3C2	7.31E-01	-5.31E-04	-1.53E-03
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	8.58E-01	-3.73E-03	-1.00E-02
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.76E-01	-4.64E-01	-9.16E-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: 2876).
2	Network-based drug repurposing for novel coronavirus 2019-nCoV/SARS-CoV-2. Cell Discov. 2020 Mar 16;6:14.
3	Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
4	Eplerenone: a selective aldosterone receptor antagonist for hypertension and heart failure. Heart Dis. 2003 Sep-Oct;5(5):354-63.
5	The relative role of CYP3A4 and CYP3A5 in eplerenone metabolism. Toxicol Lett. 2019 Oct 15;315:9-13.