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estradiol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
estrogens	1057	50-28-2

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: estradiol 17Beta-Estradiol 17Beta-Oestradiol Beta-Estradiol estradiol hemihydrate	The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. Molecular weight: 272.39 Formula: C18H24O2 CLOGP: 3.78 LIPINSKI: 0 HAC: 2 HDO: 2 TPSA: 40.46 ALOGS: -4.11 ROTB: 0 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

estradiol
17Beta-Estradiol
17Beta-Oestradiol
Beta-Estradiol
estradiol hemihydrate

The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.

Molecular weight: 272.39
Formula: C18H24O2
CLOGP: 3.78
LIPINSKI: 0
HAC: 2
HDO: 2
TPSA: 40.46
ALOGS: -4.11
ROTB: 0

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.30	mg	N
2	mg	O
1	mg	P
0.30	mg	P
5	mg	R
50	mcg	TD
1	mg	TD
1.53	mg	TD
25	mcg	V
7.50	mcg	V

ADMET properties:

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Property	Value	Reference
BA (Bioavailability)	5 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
CL (Clearance)	30 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.84 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
t_half (Half-life)	1.70 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	1.20 L/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
July 23, 1975	FDA	BRISTOL MYERS SQUIBB
Nov. 25, 2011	PMDA	Shiseido Company, Limited

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product adhesion issue	4001.61	9.76	1019	99585	3700	63384718
Hot flush	939.96	9.76	722	99882	50437	63337981
Application site rash	857.54	9.76	266	100338	2232	63386186
Application site erythema	560.34	9.76	230	100374	4605	63383813
Application site pruritus	494.19	9.76	199	100405	3785	63384633
Product quality issue	459.62	9.76	411	100193	35454	63352964
Application site irritation	404.07	9.76	138	100466	1612	63386806
Meningioma	403.73	9.76	171	100433	3714	63384704
Vulvovaginal discomfort	351.98	9.76	135	100469	2243	63386175
Pemphigus	244.49	9.76	11	100593	183715	63204703

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Meningioma	140.91	40.55	26	1020	1410	34954475
Off label use	68.06	40.55	72	974	419452	34536433
Invasive ductal breast carcinoma	60.24	40.55	8	1038	45	34955840
Keratoconus	53.25	40.55	8	1038	119	34955766
Foetal exposure during pregnancy	50.52	40.55	24	1022	38077	34917808
Product use issue	49.68	40.55	28	1018	63188	34892697
Gynaecomastia	47.80	40.55	16	1030	10164	34945721
Prolactin-producing pituitary tumour	45.61	40.55	6	1040	31	34955854
Hyperprolactinaemia	43.54	40.55	10	1036	1586	34954299
Oestradiol increased	42.04	40.55	6	1040	61	34955824

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Product adhesion issue	1415.18	10.57	357	73872	2347	79667812
Meningioma	532.33	10.57	186	74043	4112	79666047
Application site rash	415.77	10.57	130	74099	2002	79668157
Hot flush	359.93	10.57	342	73887	54535	79615624
Vulvovaginal discomfort	264.46	10.57	89	74140	1749	79668410
Application site pruritus	257.75	10.57	106	74123	3704	79666455
Application site erythema	240.34	10.57	110	74119	5000	79665159
Product quality issue	208.29	10.57	204	74025	33736	79636423
Death	175.04	10.57	162	74067	566352	79103807
Application site irritation	172.81	10.57	64	74165	1680	79668479

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	G03AA14	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens and estrogens, fixed combinations
ATC	G03AA17	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens and estrogens, fixed combinations
ATC	G03AB08	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE Progestogens and estrogens, sequential preparations
ATC	G03CA03	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ESTROGENS Natural and semisynthetic estrogens, plain
ATC	G03CA53	GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ESTROGENS Natural and semisynthetic estrogens, plain
ATC	H01CC53	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones
ATC	H01CC54	SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES HYPOTHALAMIC HORMONES Anti-gonadotropin-releasing hormones
CHEBI has role	CHEBI:50114	estrogens
CHEBI has role	CHEBI:62872	quinoline oxidase inhibitors
CHEBI has role	CHEBI:75771	Mus musculus metabolites

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID
Premenstrual dysphoric disorder	indication	596004
Contraception	indication	13197004
Female hypogonadism syndrome	indication	16041008
Atrophic vaginitis	indication	52441000
Urethral atrophy	indication	52620003
Primary ovarian failure	indication	65846009
Acne vulgaris	indication	88616000
Postmenopausal osteoporosis	indication	102447009
Ovarian deficiency symptoms	indication	111550004
Vasomotor symptoms associated with menopausal disorder	indication	123756000

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🐶 Veterinary Drug Use

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Species	Use	Relation
Cattle	To increase rate of weight gain	Indication
Cattle	To improve feed efficiency	Indication
Cattle	Synchronization of estrus/ovulation	Indication

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🐶 Veterinary products

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Product	Applicant	Ingredients
Component E-H with Tylan	Elanco US Inc.	3
Component TE-200 with Tylan, Component TE-H with Tylan, Component TE-IH with Tylan	Elanco US Inc.	3
Component TE-G, Component TE-G with Tylan, Component TE-ID with Tylan, Component TE-IS, Component TE-IS with Tylan, Component TE-S, Component TE-S with Tylan	Elanco US Inc.	3
Compudose 200, Encore (Compudose 400 )	Elanco US Inc.	2
Revalor-200, Revalor-H, Revalor-IH	Intervet Inc.	2
Revalor-G, Revalor-IS, Revalor-S	Intervet Inc.	2
Revalor-XH, Revalor-XS	Intervet Inc.	2
Revalor-XR	Intervet Inc.	2
Synovex T120, Synovex T40, Synovex T80	Zoetis Inc.	2

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.13	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	10537581	Nov. 21, 2032	TREATMENT OF A SYMPTOM OF VULVAR AND VAGINAL ATROPHY
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	10537581	Nov. 21, 2032	TREATMENT OF DYSPAREUNIA
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	10835487	Nov. 21, 2032	TREATMENT OF A SYMPTOM OF VULVAR AND VAGINAL ATROPHY
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	10835487	Nov. 21, 2032	TREATMENT OF DYSPAREUNIA
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	11241445	Nov. 21, 2032	TREATMENT OF A SYMPTOM OF VULVAR AND VAGINAL ATROPHY
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	11241445	Nov. 21, 2032	TREATMENT OF DYSPAREUNIA
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	11246875	Nov. 21, 2032	TREATMENT OF A SYMPTOM OF VULVAR AND VAGINAL ATROPHY
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	11246875	Nov. 21, 2032	TREATMENT OF DYSPAREUNIA
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	11351182	Nov. 21, 2032	TREATMENT OF A SYMPTOM OF VULVAR AND VAGINAL ATROPHY
0.004MG	IMVEXXY	MAYNE PHARMA	N208564	May 29, 2018	RX	INSERT	VAGINAL	11351182	Nov. 21, 2032	TREATMENT OF DYSPAREUNIA

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.1%	ESTRADIOL	CHEMO RESEARCH SL	A211783	Aug. 10, 2022	RX	GEL	TRANSDERMAL	April 8, 2023	COMPETITIVE GENERIC THERAPY
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	May 26, 2024	NEW PRODUCT
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	Aug. 5, 2025	FOR THE MANAGEMENT OF MODERATE TO SEVERE PAIN ASSOCIATED WITH ENDOMETRIOSIS
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	Dec. 18, 2025	NEW CHEMICAL ENTITY
1MG;0.5MG;40MG	MYFEMBREE	MYOVANT SCIENCES	N214846	May 26, 2021	RX	TABLET	ORAL	Jan. 27, 2026	INFORMATION ADDED TO THE LABELING TO DESCRIBE THE RESULTS OF MVT-601-035
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	May 29, 2023	NEW PRODUCT
EQ 300MG BASE,1MG,0.5MG; EQ 300MG BASE	ORIAHNN (COPACKAGED)	ABBVIE	N213388	May 29, 2020	RX	CAPSULE	ORAL	July 23, 2023	NEW CHEMICAL ENTITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Estrogen receptor	Nuclear hormone receptor	P03372	ESR1_HUMAN	AGONIST	EC50	10.30	WOMBAT-PK	CHEMBL
Aldehyde oxidase	Enzyme	Q06278	AOXA_HUMAN		IC50	6.54	WOMBAT-PK
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN		Ki	4.73	DRUG MATRIX
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN		Ki	4.93	DRUG MATRIX
Androgen receptor	Nuclear hormone receptor	P10275	ANDR_HUMAN		IC50	7.72	CHEMBL
Calcium-activated potassium channel subunit alpha-1	Ion channel	Q12791	KCMA1_HUMAN	ACTIVATOR	EC50	5.60	IUPHAR
Estrogen receptor beta	Nuclear hormone receptor	Q92731	ESR2_HUMAN		EC50	9.70	WOMBAT-PK
G-protein coupled estrogen receptor 1	GPCR	Q99527	GPER1_HUMAN		EC50	9.52	WOMBAT-PK
Corticosteroid-binding globulin	Secreted	P08185	CBG_HUMAN		Ki	5	CHEMBL
Steryl-sulfatase	Enzyme	P08842	STS_HUMAN		IC50	4.08	CHEMBL

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External reference:

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ID	Source
EST	PDB_CHEM_ID
001265	NDDF
007018	NDDF
116070003	SNOMEDCT_US
126172005	SNOMEDCT_US
12839006	SNOMEDCT_US
160774	MMSL
18201	MMSL
236859	RXNORM
35380-71-3	SECONDARY_CAS_RN

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Alora	HUMAN PRESCRIPTION DRUG LABEL	1	0023-5885	PATCH	0.03 mg	TRANSDERMAL	NDA	35 sections
Alora	HUMAN PRESCRIPTION DRUG LABEL	1	0023-5886	PATCH	0.05 mg	TRANSDERMAL	NDA	35 sections
Alora	HUMAN PRESCRIPTION DRUG LABEL	1	0023-5887	PATCH	0.08 mg	TRANSDERMAL	NDA	35 sections
Alora	HUMAN PRESCRIPTION DRUG LABEL	1	0023-5888	PATCH	0.10 mg	TRANSDERMAL	NDA	35 sections
ELESTRIN	HUMAN PRESCRIPTION DRUG LABEL	1	0037-4801	GEL, METERED	0.52 mg	TOPICAL	NDA	33 sections
ELESTRIN	HUMAN PRESCRIPTION DRUG LABEL	1	0037-4801	GEL, METERED	0.52 mg	TOPICAL	NDA	33 sections
Estradiol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3223	INSERT	10 ug	VAGINAL	ANDA	29 sections
Estradiol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3223	INSERT	10 ug	VAGINAL	ANDA	29 sections
Estradiol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3541	CREAM	0.10 mg	VAGINAL	ANDA	25 sections
Estradiol	HUMAN PRESCRIPTION DRUG LABEL	1	0093-3541	CREAM	0.10 mg	VAGINAL	ANDA	25 sections

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