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

General Information of Drug (ID: DMGZQEF)

Drug Name

Mifepristone Drug Info

Synonyms

Mifedren; HRA-052015; Mifepristone (Cushing's disease); ACTH modulator (Cushing's disease), HRA; Adrenocorticotropic hormone modulator (Cushing's disease), HRA Pharma; Mifepristone (Cushing's disease), HRA pharma

Indication

Disease Entry	ICD 11	Status	REF
Cushing disease	5A70	Approved	[1]

Cross-matching ID

PubChem CID: 55245
ChEBI ID: CHEBI:50692
CAS Number: CAS 84371-65-3
TTD Drug ID: DMGZQEF
VARIDT Drug ID: DR00714
INTEDE Drug ID: DR1091
ACDINA Drug ID: D00432

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Glucocorticoid receptor (NR3C1)	TTYRL6O	GCR_HUMAN	Modulator	[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	[3]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Approved	[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
Glucocorticoid receptor (NR3C1)	DTT	NR3C1	7.153	7.278	7.017	7.331
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

Cushing disease

ICD Disease Classification

5A70

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	5.82E-01	-6.00E-02	-2.69E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	9.85E-01	2.24E-02	7.33E-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: 2805).
2	The glucocorticoid agonist activities of mifepristone (RU486) and progesterone are dependent on glucocorticoid receptor levels but not on EC50 values. Steroids. 2007 Jun;72(6-7):600-8.
3	Evaluation of strategies for the assessment of drug-drug interactions involving cytochrome P450 enzymes. Eur J Drug Metab Pharmacokinet. 2018 Dec;43(6):737-750.
4	Comparative analysis of substrate and inhibitor interactions with CYP3A4 and CYP3A5. Xenobiotica. 2006 Apr;36(4):287-99.