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Depo-testadiol, Zoely(estradiol)
Activella, Angeliq, Bijuva, Climara, Combipatch, Delestrogen, Depo-testadiol, Ditate, Divigel, Elestrin, Estrasorb, Estring, Estrogel, Evamist, Femring, Imvexxy, Ioa, Lunelle, Menostar, Minivelle, Myfembree, Natazia, Prefest, Ryeqo, Vagifem, Vivelle-dot, Zoely (estradiol) is a small molecule pharmaceutical. Estradiol was first approved as Estrace on 1982-01-01. It is used to treat breast neoplasms, hot flashes, hypogonadism, menorrhagia, and premature menopause amongst others in the USA. It has been approved in Europe to treat contraception and leiomyoma. It is known to target estrogen receptor beta, nuclear receptor subfamily 1 group I member 2, estrogen receptor, Calcium-activated potassium channel subunit alpha-1; calcium-activated potassium channel subunit alpha-1, and G-protein coupled estrogen receptor 1.
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Searched
Commercial
Therapeutic Areas
Therapeutic Area
MeSH
neoplasmsD009369
urogenital diseasesD000091642
skin and connective tissue diseasesD017437
endocrine system diseasesD004700
signs and symptoms pathological conditionsD013568
therapeuticsD013812
reproductive and urinary physiological phenomenaD012101
Trade Name
FDA
EMA
Climara, Delestrogen, Divigel, Elestrin, Estring, Estrogel, Evamist, Femring, Imvexxy, Menostar, Minivelle, Vagifem, Vivelle-dot (generic drugs available since 1982-01-01, discontinued: Alora, Esclim, Estrace, Estraderm, Estrasorb, Fempatch, Femtrace, Gynodiol, Innofem, Vivelle)
Combinations
Activella, Angeliq, Bijuva, Climara, Combipatch, Myfembree, Natazia (generic drugs available since 1982-01-01, discontinued: Depo-testadiol, Ditate, Lunelle, Prefest)
Drug Products
FDA
EMA
New Drug Application (NDA)
New Drug Application (NDA)
Abbreviated New Drug Application (ANDA)
Abbreviated New Drug Application (ANDA)
Dienogest
+
Estradiol valerate
Tradename
Company
Number
Date
Products
NATAZIABayerN-022252 RX2010-05-06
1 products, RLD, RS
Drospirenone
+
Estradiol
Tradename
Company
Number
Date
Products
ANGELIQBayerN-021355 RX2005-09-28
2 products, RLD, RS
Estradiol
Tradename
Company
Number
Date
Products
ESTROGELAscend TherapeuticsN-021166 RX2004-02-09
1 products, RLD, RS
CLIMARABayerN-020375 RX1994-12-22
6 products, RLD, RS
MENOSTARBayerN-021674 RX2004-06-08
1 products, RLD, RS
IMVEXXYMayne GroupN-208564 RX2018-05-29
2 products, RLD, RS
ELESTRINMylanN-021813 RX2006-12-15
1 products, RLD, RS
MINIVELLENoven PharmaceuticalsN-203752 RX2012-10-29
5 products, RLD, RS
VAGIFEMNovo NordiskN-020908 RX2009-11-25
1 products, RLD, RS
EVAMISTPadagisN-022014 RX2007-07-27
1 products, RLD, RS
ESTRINGMylanN-020472 RX1996-04-26
1 products, RLD, RS
VIVELLE-DOTSandozN-020538 RX1999-01-08
5 products, RLD, RS
Show 1 marketed
Show 8 discontinued
Estradiol
+
Levonorgestrel
Tradename
Company
Number
Date
Products
CLIMARA PROBayerN-021258 RX2003-11-21
1 products, RLD, RS
Estradiol
+
Norethindrone acetate
Tradename
Company
Number
Date
Products
ACTIVELLAAmneal PharmaceuticalsN-020907 RX1998-11-18
1 products, RLD, RS
COMBIPATCHNoven PharmaceuticalsN-020870 RX1998-08-07
2 products, RLD, RS
Show 1 discontinued
Estradiol
+
Norethindrone acetate
+
Relugolix
Tradename
Company
Number
Date
Products
MYFEMBREEMyovant SciencesN-214846 RX2021-05-26
1 products, RLD, RS
Estradiol
+
Norgestimate
Tradename
Company
Number
Date
Products
PREFESTTevaN-021040 DISCN1999-10-22
1 products, RLD
Hide discontinued
Estradiol
+
Progesterone
Tradename
Company
Number
Date
Products
BIJUVAMayne GroupN-210132 RX2018-10-28
2 products, RLD, RS
Estradiol acetate
Tradename
Company
Number
Date
Products
FEMRINGMillicent PharmaN-021367 RX2003-03-20
2 products, RLD, RS
Show 1 discontinued
Estradiol cypionate
+
Medroxyprogesterone acetate
Tradename
Company
Number
Date
Products
LUNELLEPharmacia & UpjohnN-020874 DISCN2000-10-05
1 products
Hide discontinued
Estradiol cypionate
+
Testosterone cypionate
Tradename
Company
Number
Date
Products
DEPO-TESTADIOLPharmacia & UpjohnN-017968 DISCN1982-01-01
1 products
Hide discontinued
Estradiol hemihydrate
Tradename
Company
Number
Date
Products
ESTRASORBExeltisN-021371 DISCN2003-10-09
1 products, RLD
Hide discontinued
Estradiol valerate
Tradename
Company
Number
Date
Products
DELESTROGENPar PharmaceuticalN-009402 RX1982-01-01
3 products, RLD, RS
Labels
FDA
EMA
Brand Name
Status
Last Update
activellaNew Drug Application2021-08-26
alora OTC monograph not final2022-01-07
amabelzANDA2021-12-01
angeliqNew Drug Application2017-11-14
bijuvaNew Drug Application2021-06-30
climara proNew Drug Application2023-03-29
combipatch (estradiol/norethindrone acetate transdermal system)New Drug Application2019-03-25
delestrogenNew Drug Application2018-09-12
divigelNew Drug Application2020-10-21
elestrinNew Drug Application2020-10-15
Show 14 more
Indications
FDA
EMA
Indication
Ontology
MeSH
ICD-10
breast neoplasmsEFO_0003869D001943C50
hot flashes—D019584—
hypogonadismHP_0000815D007006E23.0
menorrhagiaHP_0000132D008595N92.0
premature menopauseHP_0008209D008594E28.31
primary ovarian insufficiencyEFO_0004266D016649E28.3
prostatic neoplasms—D011471C61
Agency Specific
FDA
EMA
Expiration
Code
ESTRADIOL / NORETHINDRONE ACETATE / RELUGOLIX, MYFEMBREE, MYOVANT SCIENCES
2026-01-27M-289
2025-12-18NCE
2025-08-05I-898
2024-05-26NP
ESTRADIOL, ESTRADIOL, CHEMO RESEARCH SL
2023-04-08CGT
Patent Expiration
Patent
Expires
Flag
FDA Information
Estradiol / Norethindrone Acetate / Relugolix, Myfembree, Myovant Sciences
110335512037-09-29U-3129
93468222024-02-17U-3129
73009352024-01-28DP
80582802024-01-28DP
Estradiol, Imvexxy, Mayne Pharma
112666612034-02-02U-2316, U-2317
91800912033-12-20DPU-2316, U-2317
102586302033-12-20U-2316, U-2317
103987082033-12-20U-2317, U-2614
104710722033-06-18U-2316, U-2317
105688912033-06-18U-2316, U-2317
106680822033-06-18U-2316, U-2317
108885162033-06-18U-2316, U-2317
110651972033-06-18DP
111167172033-06-18DP
111232832033-06-18DP
92893822032-11-21DP
105375812032-11-21DPU-2316, U-2317
108066972032-11-21DP
108354872032-11-21U-2316, U-2317
112414452032-11-21U-2316, U-2317
112468752032-11-21U-2316, U-2317
113049592032-11-21DP
113511822032-11-21U-2316, U-2317
114977092032-11-21U-2316, U-2317
Estradiol / Progesterone, Bijuva, Mayne Pharma
86331782032-11-21DP
88466482032-11-21U-2439
88466492032-11-21DPU-2439
89330592032-11-21DPU-2439
89872372032-11-21DP
89935482032-11-21DP
89935492032-11-21DP
90062222032-11-21DPU-2439
91141452032-11-21U-2439
91141462032-11-21DPU-2439
93019202032-11-21DPU-2439
100523862032-11-21DP
102069322032-11-21U-2439
106393752032-11-21DP
106752882032-11-21U-2439
108067402032-11-21DPU-2439
110336262032-11-21DPU-2439
111035132032-11-21U-2439
111035162032-11-21DP
111100992032-11-21DP
111669632032-11-21DP
115293602032-11-21DP
Drospirenone / Estradiol, Angeliq, Bayer Hlthcare
89068902031-10-22DP
Estradiol, Minivelle, Noven
82319062030-07-04DS, DP
97243102028-07-10DS, DP
97309002028-07-10U-2086
98334192028-07-10DP
Dienogest / Estradiol Valerate, Natazia, Bayer Hlthcare
81536162028-01-30U-1240
80715772026-05-13DPU-1
Estradiol Acetate, Femtrace, Apil
75727792025-10-02U-904
ATC Codes
G: Genito urinary system and sex hormones
— G03: Sex hormones and modulators of the genital system
— G03A: Hormonal contraceptives for systemic use
— G03AA: Progestogens and estrogen systemic contraceptives, fixed combinations
— G03AA14: Nomegestrol and estradiol
— G03AA17: Medroxyprogesterone and estradiol
— G03AB: Progestogens and estrogens systemic contraceptives, sequential preparations
— G03AB08: Dienogest and estradiol
— G03C: Estrogens, sex hormones and modulators of the genital system
— G03CA: Natural and semisynthetic estrogens, plain
— G03CA03: Estradiol
— G03CA53: Estradiol, combinations
H: Systemic hormonal preparations, excl. sex hormones and insulins
— H01: Pituitary and hypothalamic hormones and analogues
— H01C: Hypothalamic hormones
— H01CC: Anti-gonadotropin-releasing hormones
— H01CC54: Relugolix, estradiol and norethisterone
HCPCS
Code
Description
A9591
Fluoroestradiol f 18, diagnostic, 1 millicurie
J1000
Injection, depo-estradiol cypionate, up to 5 mg
J1380
Injection, estradiol valerate, up to 10 mg
J7294
Segesterone acetate and ethinyl estradiol 0.15mg, 0.013mg per 24 hours; yearly vaginal system, each
J7295
Ethinyl estradiol and etonogestrel 0.015mg, 0.12mg per 24 hours; monthly vaginal ring, each
Clinical
Clinical Trials
603 clinical trials
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Indications Phases 4
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
ContraceptionD00326712522141063
MenopauseD008593EFO_0003922N95971314647
InfertilityD007246EFO_0000545224121938
Healthy volunteers/patients—28423—34
Polycystic ovary syndromeD011085EFO_0000660E28.24—271225
Breast neoplasmsD001943EFO_0003869C5011321521
Hot flashesD019584—393318
PostmenopauseD0176982364316
EndometriosisD004715EFO_0001065N80—373214
Female infertilityD007247EFO_0008560N971—13510
Show 69 more
Indications Phases 3
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Premenstrual syndromeD011293N94.3114—28
Prostatic neoplasmsD011471C61—52——6
Anorexia nervosaD000856EFO_0004215F50.0221——5
SchizophreniaD012559EFO_0000692F20—32——5
AtrophyD001284—22——4
AdenomyosisD062788EFO_1001757N80.01—1—13
Metabolic bone diseasesD001851HP_0000938—12——3
Premenstrual dysphoric disorderD065446F32.81—21——3
Migraine disordersD008881EFO_0003821G43121——3
ObesityD009765EFO_0001073E66.9——1—12
Show 17 more
Indications Phases 2
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Covid-19D000086382U07.1—3———3
NeoplasmsD009369C8011———2
Feeding and eating disordersD001068F50—2———2
Bulimia nervosaD052018EFO_0005204F50.2—2———2
Temporomandibular joint disordersD013705M26.6—1——12
FibromyalgiaD005356EFO_0005687M79.1—1——12
Endometrial neoplasmsD016889EFO_0004230—2———2
Orthostatic intoleranceD054971—1———1
Ovarian diseasesD010049—1———1
HemostasisD006487—1———1
Show 20 more
Indications Phases 1
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Therapeutic equivalencyD01381010———111
PharmacokineticsD0105995————5
Drug interactionsD0043473———14
Type 1 diabetes mellitusD003922EFO_0001359E101———12
Type 2 diabetes mellitusD003924EFO_0001360E112————2
Hepatitis cD006526B19.22————2
Systemic lupus erythematosusD008180EFO_0002690M321———12
TransgenesD0190761————1
Cerebral arterial diseasesD002539EFO_10008591————1
InfectionsD007239EFO_00005441————1
Show 10 more
Indications Without Phase
Indication
MeSH
Ontology
ICD-10
Ph 1
Ph 2
Ph 3
Ph 4
Other
Total
Psychological sexual dysfunctionsD020018F52.0————22
Heart disease risk factorsD000082742————11
Premature menopauseD008594HP_0008209E28.31————11
Breast densityD000071060————11
Cognitive dysfunctionD060825G31.84————11
Blood pressureD001794EFO_0004325————11
Pulmonary embolismD011655EFO_0003827I26————11
Intracranial sinus thrombosisD012851————11
Postmenopausal osteoporosisD015663EFO_0003854————11
HemorrhageD006470MP_0001914R58————11
Show 15 more
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common nameESTRADIOL
INNestradiol valerate
Description
17beta-estradiol is the 17beta-isomer of estradiol. It has a role as an estrogen, a human metabolite, an EC 1.2.3.1 (aldehyde oxidase) inhibitor, a Daphnia magna metabolite, a mouse metabolite and a geroprotector. It is a 17beta-hydroxy steroid and an estradiol.
Classification
Small molecule
Drug classestrogens
Image (chem structure or protein)
Structure (InChI/SMILES or Protein Sequence)
C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1CC[C@@H]2O
Identifiers
PDB7AXK
CAS-ID50-28-2
RxCUI4083
ChEMBL IDCHEMBL135
ChEBI ID16469
PubChem CID5757
DrugBankDB00783
UNII IDOKG364O896 (ChemIDplus, GSRS)
Target
Agency Approved
No data
Alternate
ESR2
ESR2
NR1I2
NR1I2
ESR1
ESR1
KCNMA1
KCNMA1
GPER1
GPER1
Organism
Homo sapiens
Gene name
ESR2
Gene synonyms
ESTRB, NR3A2
NCBI Gene ID
Protein name
estrogen receptor beta
Protein synonyms
estrogen receptor beta 2, estrogen receptor beta 4, Nuclear receptor subfamily 3 group A member 2, oestrogen receptor beta
Uniprot ID
Mouse ortholog
Esr2 (13983)
estrogen receptor beta (O08537)
Variants
Clinical Variant
No data
Financial
Imvexxy - TherapeuticsMD
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Bijuva - TherapeuticsMD
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Myfembree - Myovant Sciences
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Ryeqo - Myovant Sciences
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Estradiol - Amneal Pharmaceuticals
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Divigel - RVL Pharmaceuticals
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Tabular view
Trends
PubMed Central
Top Terms for Disease or Syndrome:
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Additional graphs summarizing 119,134 documents
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Safety
Black-box Warning
Black-box warning for: Activella, Amabelz, Angeliq, Bijuva, Climara pro, Combipatch (estradiol/norethindrone acetate transdermal system), Delestrogen, Divigel, Elestrin, Estrace, Estring, Estrogel, Evamist, Femring, Imvexxy, Menostar, Minivelle, Myfembree, Natazia, Vagifem, Vivelle-dot, Yaz
Adverse Events
Top Adverse Reactions
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111,864 adverse events reported
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