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

General Information of Drug (ID: DMC4GEI)

Drug Name

Ospemifene Drug Info

Synonyms

Ospemifene; 128607-22-7; Osphena; FC-1271a; Deamino-hydroxytoremifene; Fc-1271; 2-(4-(4-chloro-1,2-diphenyl-but-1-enyl)phenoxy)ethanol; UNII-B0P231ILBK; CCRIS 9205; B0P231ILBK; CHEBI:73275; 2-(p-((Z)-4-Chloro-1,2-diphenyl-1-butenyl)phenoxy)ethanol; senshio; Ethanol, 2-[4-[(1Z)-4-chloro-1,2-diphenyl-1-butenyl]phenoxy]-; 2-{4-[(1Z)-4-chloro-1,2-diphenylbut-1-en-1-yl]phenoxy}ethanol; Ophena; Ospemifene [USAN:INN:BAN]; Deaminotoremifene; Osphena (TN); Deaminohydroxytoremifene; AC1MI19T; C24H23ClO2

Indication

Disease Entry	ICD 11	Status	REF
Dyspareunia	GA12	Approved	[1]
Postmenopausal vaginal atrophy	GA30.2	Phase 3	[1]

Cross-matching ID

PubChem CID: 3036505
ChEBI ID: CHEBI:73275
CAS Number: CAS 128607-22-7
TTD Drug ID: DMC4GEI
INTEDE Drug ID: DR1208
ACDINA Drug ID: D00496

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor (ESR)	TTZAYWL	ESR1_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 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[3]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[3]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Approved	[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
Estrogen receptor (ESR)	DTT	ESR1	3.728	3.17	4.897	4.505
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
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

Dyspareunia

ICD Disease Classification

GA12

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Cytochrome P450 2B6 (CYP2B6)	DME	CYP2B6	3.97E-02	-1.72E-01	-9.29E-01
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	3.44E-01	-1.85E-01	-5.25E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	9.09E-01	-9.26E-02	-3.68E-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: 7349).
2	Clinical pipeline report, company report or official report of Shionogi (2011).
3	Ospemifene metabolism in humans in vitro and in vivo: metabolite identification, quantitation, and CYP assignment of major hydroxylations. Drug Metabol Drug Interact. 2013;28(3):153-61.