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

General Information of Drug (ID: DMLT0E1)

Drug Name

Conjugated Estrogens Drug Info

Synonyms

Par Estro; evex; Premarin; Conestoral; NSC18313; Sodium estrone 3-monosulfate; Estrone, hydrogen sulfate sodium salt; AC1NS0NL; NSC-18313; sodium [(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate; Estra-1,5(10)-trien-17-one, 3-(sulfooxy)-, sodium; Carentil; Congest; Estroplus; Evex; Menotabs; Oestrogen; Prelestrin; Presomil; Progens; Conjugated Equine Estrogens; Conjugated Estrogenic Substances; Conjugated estrogenic hormones; Conjugated oestrogens; Conjugated oestrogens [Steroidal oestrogens]; Steroidal estrogens; ASTA Medica Brand of Estrogens, Conjugated; Almirall Brand of Estrogens, Conjugated; Equine Estrogens, Conjugated; Estro-Feminal; Estrogenic Hormones, Conjugated; Estrogenic substances, conjugated; Estrogens, conjugated USP; Estrogens, conjugated [USP]; Estrogens, conjugated synthetic A; Estrogens, steroidal; Solvay Brand of Estrogens, Conjugated; Trianon Brand of Estrogens, Conjugated; Wyeth Brand of Estrogens, Conjugated; Estrogens, conjugated (USP); Estrogens, conjugated-equine; Mack Brand of Estrogens, Conjugated (USP); Major Brand of Estrogens, Conjugated (USP); Pasadena Brand of Estrogens, Conjugated (USP); Pharmacia Brand of Estrogens, Conjugated (USP); CES; Estra-1,3,5(10)-trien-17-one, 3-(sulfooxy)-, sodium salt; Sodium [(8R,9S,13S,14S)-13-methyl-17-oxo-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-3-yl] hydrogen sulfate

Indication

Disease Entry	ICD 11	Status	REF
Dyspareunia	GA12	Approved	[1]
Hot flushes	GA30	Approved	[2]
Menopause symptom	GA30.0	Approved	[3]
Vasomotor symptom	CA08	Approved	[4]

Therapeutic Class

Estrogens

Cross-matching ID

PubChem CID: 45357473
TTD Drug ID: DMLT0E1
VARIDT Drug ID: DR00673
INTEDE Drug ID: DR0377

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor beta (ESR2)	TTOM3J0	ESR2_HUMAN	Antagonist	[5]

------------------------------------------------------------------------------------

Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[6]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_HUMAN	Approved	[7]
Beta-glucuronidase (uidA)	DE9RA0I	BGLR_ECOLI	Approved	[8]

------------------------------------------------------------------------------------

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 beta (ESR2)	DTT	ESR2	3.365	3.776	3.485	3.036
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
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
Estrogen receptor beta (ESR2)	DTT	ESR2	2.09E-01	-0.06	-0.17
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	4.89E-02	-3.74E-01	-6.96E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.10E-01	-1.23E-01	-2.88E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	Drugs for menopausal symptoms. Med Lett Drugs Ther. 2020 Aug 10;62(1604):124-128.
2	Raloxifene. Drugs Aging. 1998 Apr;12(4):335-41; discussion 342.
3	ClinicalTrials.gov (NCT01613170) Premarin Versus Toviaz for Treatment of Overactive Bladder. U.S. National Institutes of Health.
4	Roles of hormone replacement therapy and iron in proliferation of breast epithelial cells with different estrogen and progesterone receptor status. Breast. 2008 Apr;17(2):172-9.
5	Differential biochemical and cellular actions of Premarin estrogens: distinct pharmacology of bazedoxifene-conjugated estrogens combination. Mol Endocrinol. 2009 Jan;23(1):74-85.
6	Conjugated oestrogens/bazedoxifene. Aust Prescr. 2017 Jun;40(3):114-115.
7	Effect of conjugated equine estrogens on oxidative metabolism in middle-aged and elderly postmenopausal women. J Clin Pharmacol. 2006 Nov;46(11):1299-307.
8	Long-term administration of conjugated estrogen and bazedoxifene decreased murine fecal beta-glucuronidase activity without impacting overall microbiome community. Sci Rep. 2018 May 25;8(1):8166.