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

General Information of Drug (ID: DME7VZD)

Drug Name

Vilaprisan Drug Info

Synonyms

Vilaprisan; UNII-IN59K53GI9; BAY1002670; IN59K53GI9; 1262108-14-4; Vilaprisan [INN]; BAY 1002670; Vilaprisan [USAN:INN]; Vilaprisan (USAN/INN); SCHEMBL2121854; CHEMBL3989936; BCP24069; DB11971; 20,20,21,21,21-Pentafluoro-17-hydroxy-11beta-(4-(methanesulfonyl)phenyl)-19-nor-17alpha-pregna-4,9-dien-3-one; 19-Norpregna-4,9-dien-3-one, 20,20,21,21,21-pentafluoro-17-hydroxy-11-(4-(methylsulfonyl)phenyl)-, (11beta,17alpha)-

Indication

Disease Entry	ICD 11	Status	REF
Endometriosis	GA10	Phase 2	[1]

Cross-matching ID

PubChem CID: 50915138
CAS Number: CAS 1262108-14-4
TTD Drug ID: DME7VZD
INTEDE Drug ID: DR1831

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Progesterone receptor (PGR)	TTUV8G9	PRGR_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	Phase 2	[3]
Succinic semialdehyde reductase (AKR7A2)	DE4G629	ARK72_HUMAN	Phase 2	[3]

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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
Progesterone receptor (PGR)	DTT	PGR	1.848	1.888	1.263	0.138
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089
Succinic semialdehyde reductase (AKR7A2)	DME	AKR7A2	7.567	8.118	7.837	7.993

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

Endometriosis

ICD Disease Classification

GA10

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Progesterone receptor (PGR)	DTT	PGR	3.26E-38	-3.79	-2.5
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	2.20E-02	-1.08E-01	-2.31E-01
Succinic semialdehyde reductase (AKR7A2)	DME	AKR7A2	2.53E-22	-6.86E-01	-9.08E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	ClinicalTrials.gov (NCT02465814) Assess Safety and Efficacy of Vilaprisan in Patients With Uterine Fibroids.
2	Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800033939)
3	Characterization of the pharmacokinetics of vilaprisan: bioavailability, excretion, biotransformation, and drug-drug interaction potential. Clin Pharmacokinet. 2018 Aug;57(8):1001-1015.