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

General Information of Drug (ID: DMODJ40)

Drug Name

Ethinyl Estradiol Drug Info

Synonyms

Aethinyloestradiolum; Aethinyoestradiol; Amenoron; Amenorone; Anovlar; Certostat; Cyclosa; Dicromil; Diprol; Dyloform; Ertonyl; Esteed; Estigyn; Estinyl; Estopherol; Estoral; Estorals; Ethidol; Ethinoral; Ethinylestradiolum; Ethinylestriol; Ethinyloestradiol; Ethynylestradiol; Ethynyloestradiol; Eticyclin; Eticyclol; Eticylol; Etinestrol; Etinestryl; Etinilestradiol; Etinilestradiolo; Etinoestryl; Etistradiol; Etivex; Feminone; Follicoral; Ginestrene; Inestra; Kolpolyn; Linoral; Lynoral; Menolyn; Microfollin; Novestrol; Oradiol; Orestralyn; Orestrayln; Palonyl; Perovex; Primogyn; Prosexol; Spanestrin; Ylestrol; Aethinyoestradiol [German]; Component of Demulen; Component of Oracon; Component of Ortrel; Diogyn E; Effik Brand of Ethinyl Estradiol; Estoral [Orion]; Ethinyl Estradiol Hemihydrate; Ethinyl Estradiol [USP]; Ethinyl Oestradiol Effik; Ethinylestradiol Jenapharm; Ethinyloestradiol [Steroidal oestrogens]; Ethynyl estradiol; Etinilestradiolo [DCIT]; Jenapharm Brand of Ethinyl Estradiol; Microfollin Forte; Organon Brand of Ethinyl Estradiol; PUBERTAL ETHINYL ESTRADIOL STUDY; Primogyn C; Primogyn M; Progynon C; Progynon M; Schering Brand of Ethinyl Estradiol; EE2; Ethinyl E2; Ethy 11; Diognat-E; Diogyn-E; EE(sub 2); Estinyl (TN); Eston-E; Estoral (Orion); Estoral (VAN); Estradiol, Ethinyl; Estradiol, Ethynyl; Ethinyl estradiol (USP); Ethinyl-Oestradiol Effik; Ethinyl-oestranol; Ethinylestradiolum [INN-Latin]; Ethynylestradiol, Ethinyl Estradiol; Etinilestradiol [INN-Spanish]; Hemihydrate, Ethinyl Estradiol; Jenapharm, Ethinylestradiol; Neo-Estrone; Nogest-S; OVULEN-21; OVULEN-28; Ortho-Cyclen; Chee-O-Gen; Chee-O-Genf; Ethinylestradiol (JP15/INN); Ethinylestradiol [INN:BAN:JAN]; Ethinyl Estradiol, (8 alpha)-Isomer; 17 alpha-Ethinylestradiol; 17 alpha-Ethynylestradiol; 17 alpha-Ethynyloestradiol; 17 alpha-ethinyestradiol; 17-Ethinyl-3,17-estradiol; 17-Ethinyl-3,17-oestradiol; 17-Ethinylestradiol; 17-Ethynylestradiol; 17-Ethynyloestradiol; 17-alpha-Ethinyl-17-beta-estradiol; 17-alpha-Ethynyl-17-beta-oestradiol; 17-alpha-Ethynylestradiol; 17-alpha-Ethynylestradiol-17-beta; 17-alpha-Ethynylestradiol-l7-beta; 17-alpha-Ethynyloestradiol-17-beta; 17-alpha-ethynyl estradiol; 17.alpha.-Ethinyl-17.beta.-estradiol; 17.alpha.-Ethinylestradiol; 17.alpha.-Ethynyl-17.beta.-oestradiol; 17.alpha.-Ethynylestradiol; 17.alpha.-Ethynyloestradiol; 17a-Ethynylestradiol; 17alpha-Ethinyl estradiol; 17alpha-Ethinylestradiol; 17alpha-Ethinylestradiol-17beta; 17alpha-Ethynylestradiol; 17alpha-Ethynyloestradiol; 17alpha-Ethynyloestradiol-17beta

Indication

Disease Entry	ICD 11	Status	REF
Acne vulgaris	ED80	Approved	[1]
Female hypogonadism	GA30.6	Approved	[2]
Hot flushes	GA30	Approved	[1]
Obsolete atrophic vulva		Approved	[1]

Therapeutic Class

Estrogens

Cross-matching ID

PubChem CID: 5991
ChEBI ID: CHEBI:4903
CAS Number: CAS 57-63-6
TTD Drug ID: DMODJ40
VARIDT Drug ID: DR00103
INTEDE Drug ID: DR0656

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Estrogen receptor (ESR)	TTZAYWL	ESR1_HUMAN	Agonist	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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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	[5]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[6]
Cytochrome P450 1A1 (CYP1A1)	DE6OQ3W	CP1A1_HUMAN	Approved	[6]
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DEYGVN4	UD11_HUMAN	Approved	[7]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[8]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[9]

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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
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	5.952	6.384	4.897	6.293
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

Acne vulgaris

ICD Disease Classification

ED80

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.23E-01	-8.20E-02	-3.22E-01
UDP-glucuronosyltransferase 1A1 (UGT1A1)	DME	UGT1A1	7.69E-01	1.91E-02	5.45E-02
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.78E-01	-3.38E-03	-5.71E-02
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	3.44E-01	-1.85E-01	-5.25E-01
Cytochrome P450 1A1 (CYP1A1)	DME	CYP1A1	5.01E-01	-1.01E-02	-6.05E-02
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	Ethinyl estradiol FDA Label
2	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: 7071).
3	17alpha-Ethinylestradiol hinders nucleotide excision repair in zebrafish liver cells. Aquat Toxicol. 2009 Dec 13;95(4):273-8.
4	P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93.
5	Rifampicin, a keystone inducer of drug metabolism: from Herbert Remmer's pioneering ideas to modern concepts. Drug Metab Rev. 2004 Oct;36(3-4):497-509.
6	The involvement of CYP3A4 and CYP2C9 in the metabolism of 17 alpha-ethinylestradiol. Drug Metab Dispos. 2004 Nov;32(11):1209-12.
7	Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios. Drug Metab Dispos. 2004 Nov;32(11):1201-8.
8	The effect of ethinyloestradiol and levonorgestrel on the CYP2C19-mediated metabolism of omeprazole in healthy female subjects. Br J Clin Pharmacol. 2003 Aug;56(2):232-7.
9	Examination of 209 drugs for inhibition of cytochrome P450 2C8. J Clin Pharmacol. 2005 Jan;45(1):68-78.