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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Commercial
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)
CombinationsActivella, 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 |
---|---|---|---|---|
NATAZIA | Bayer | N-022252 RX | 2010-05-06 | 1 products, RLD, RS |
Drospirenone
+
Estradiol
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
ANGELIQ | Bayer | N-021355 RX | 2005-09-28 | 2 products, RLD, RS |
Estradiol
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
ESTROGEL | Ascend Therapeutics | N-021166 RX | 2004-02-09 | 1 products, RLD, RS |
CLIMARA | Bayer | N-020375 RX | 1994-12-22 | 6 products, RLD, RS |
MENOSTAR | Bayer | N-021674 RX | 2004-06-08 | 1 products, RLD, RS |
IMVEXXY | Mayne Group | N-208564 RX | 2018-05-29 | 2 products, RLD, RS |
ELESTRIN | Mylan | N-021813 RX | 2006-12-15 | 1 products, RLD, RS |
MINIVELLE | Noven Pharmaceuticals | N-203752 RX | 2012-10-29 | 5 products, RLD, RS |
VAGIFEM | Novo Nordisk | N-020908 RX | 2009-11-25 | 1 products, RLD, RS |
EVAMIST | Padagis | N-022014 RX | 2007-07-27 | 1 products, RLD, RS |
ESTRING | Mylan | N-020472 RX | 1996-04-26 | 1 products, RLD, RS |
VIVELLE-DOT | Sandoz | N-020538 RX | 1999-01-08 | 5 products, RLD, RS |
Show 1 marketed
Show 8 discontinued
Estradiol
+
Levonorgestrel
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
CLIMARA PRO | Bayer | N-021258 RX | 2003-11-21 | 1 products, RLD, RS |
Estradiol
+
Norethindrone acetate
Estradiol
+
Norethindrone acetate
+
Relugolix
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
MYFEMBREE | Myovant Sciences | N-214846 RX | 2021-05-26 | 1 products, RLD, RS |
Estradiol
+
Norgestimate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
PREFEST | Teva | N-021040 DISCN | 1999-10-22 | 1 products, RLD |
Hide discontinued
Estradiol
+
Progesterone
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
BIJUVA | Mayne Group | N-210132 RX | 2018-10-28 | 2 products, RLD, RS |
Estradiol acetate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
FEMRING | Millicent Pharma | N-021367 RX | 2003-03-20 | 2 products, RLD, RS |
Show 1 discontinued
Estradiol cypionate
+
Medroxyprogesterone acetate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
LUNELLE | Pharmacia & Upjohn | N-020874 DISCN | 2000-10-05 | 1 products |
Hide discontinued
Estradiol cypionate
+
Testosterone cypionate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
DEPO-TESTADIOL | Pharmacia & Upjohn | N-017968 DISCN | 1982-01-01 | 1 products |
Hide discontinued
Estradiol hemihydrate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
ESTRASORB | Exeltis | N-021371 DISCN | 2003-10-09 | 1 products, RLD |
Hide discontinued
Estradiol valerate
Tradename | Company | Number | Date | Products |
---|---|---|---|---|
DELESTROGEN | Par Pharmaceutical | N-009402 RX | 1982-01-01 | 3 products, RLD, RS |
Labels
FDA
EMA
Brand Name | Status | Last Update |
---|---|---|
activella | New Drug Application | 2021-08-26 |
alora | OTC monograph not final | 2022-01-07 |
amabelz | ANDA | 2021-12-01 |
angeliq | New Drug Application | 2017-11-14 |
bijuva | New Drug Application | 2021-06-30 |
climara pro | New Drug Application | 2023-03-29 |
combipatch (estradiol/norethindrone acetate transdermal system) | New Drug Application | 2019-03-25 |
delestrogen | New Drug Application | 2018-09-12 |
divigel | New Drug Application | 2020-10-21 |
elestrin | New Drug Application | 2020-10-15 |
Show 14 more
Indications
FDA
EMA
Indication | Ontology | MeSH | ICD-10 |
---|---|---|---|
breast neoplasms | EFO_0003869 | D001943 | C50 |
hot flashes | — | D019584 | — |
hypogonadism | HP_0000815 | D007006 | E23.0 |
menorrhagia | HP_0000132 | D008595 | N92.0 |
premature menopause | HP_0008209 | D008594 | E28.31 |
primary ovarian insufficiency | EFO_0004266 | D016649 | E28.3 |
prostatic neoplasms | — | D011471 | C61 |
Agency Specific
FDA
EMA
Expiration | Code | ||
---|---|---|---|
ESTRADIOL / NORETHINDRONE ACETATE / RELUGOLIX, MYFEMBREE, MYOVANT SCIENCES | |||
2026-01-27 | M-289 | ||
2025-12-18 | NCE | ||
2025-08-05 | I-898 | ||
2024-05-26 | NP | ||
ESTRADIOL, ESTRADIOL, CHEMO RESEARCH SL | |||
2023-04-08 | CGT |
Patent Expiration
Patent | Expires | Flag | FDA Information |
---|---|---|---|
Estradiol / Norethindrone Acetate / Relugolix, Myfembree, Myovant Sciences | |||
11033551 | 2037-09-29 | U-3129 | |
9346822 | 2024-02-17 | U-3129 | |
7300935 | 2024-01-28 | DP | |
8058280 | 2024-01-28 | DP | |
Estradiol, Imvexxy, Mayne Pharma | |||
11266661 | 2034-02-02 | U-2316, U-2317 | |
9180091 | 2033-12-20 | DP | U-2316, U-2317 |
10258630 | 2033-12-20 | U-2316, U-2317 | |
10398708 | 2033-12-20 | U-2317, U-2614 | |
10471072 | 2033-06-18 | U-2316, U-2317 | |
10568891 | 2033-06-18 | U-2316, U-2317 | |
10668082 | 2033-06-18 | U-2316, U-2317 | |
10888516 | 2033-06-18 | U-2316, U-2317 | |
11065197 | 2033-06-18 | DP | |
11116717 | 2033-06-18 | DP | |
11123283 | 2033-06-18 | DP | |
9289382 | 2032-11-21 | DP | |
10537581 | 2032-11-21 | DP | U-2316, U-2317 |
10806697 | 2032-11-21 | DP | |
10835487 | 2032-11-21 | U-2316, U-2317 | |
11241445 | 2032-11-21 | U-2316, U-2317 | |
11246875 | 2032-11-21 | U-2316, U-2317 | |
11304959 | 2032-11-21 | DP | |
11351182 | 2032-11-21 | U-2316, U-2317 | |
11497709 | 2032-11-21 | U-2316, U-2317 | |
Estradiol / Progesterone, Bijuva, Mayne Pharma | |||
8633178 | 2032-11-21 | DP | |
8846648 | 2032-11-21 | U-2439 | |
8846649 | 2032-11-21 | DP | U-2439 |
8933059 | 2032-11-21 | DP | U-2439 |
8987237 | 2032-11-21 | DP | |
8993548 | 2032-11-21 | DP | |
8993549 | 2032-11-21 | DP | |
9006222 | 2032-11-21 | DP | U-2439 |
9114145 | 2032-11-21 | U-2439 | |
9114146 | 2032-11-21 | DP | U-2439 |
9301920 | 2032-11-21 | DP | U-2439 |
10052386 | 2032-11-21 | DP | |
10206932 | 2032-11-21 | U-2439 | |
10639375 | 2032-11-21 | DP | |
10675288 | 2032-11-21 | U-2439 | |
10806740 | 2032-11-21 | DP | U-2439 |
11033626 | 2032-11-21 | DP | U-2439 |
11103513 | 2032-11-21 | U-2439 | |
11103516 | 2032-11-21 | DP | |
11110099 | 2032-11-21 | DP | |
11166963 | 2032-11-21 | DP | |
11529360 | 2032-11-21 | DP | |
Drospirenone / Estradiol, Angeliq, Bayer Hlthcare | |||
8906890 | 2031-10-22 | DP | |
Estradiol, Minivelle, Noven | |||
8231906 | 2030-07-04 | DS, DP | |
9724310 | 2028-07-10 | DS, DP | |
9730900 | 2028-07-10 | U-2086 | |
9833419 | 2028-07-10 | DP | |
Dienogest / Estradiol Valerate, Natazia, Bayer Hlthcare | |||
8153616 | 2028-01-30 | U-1240 | |
8071577 | 2026-05-13 | DP | U-1 |
Estradiol Acetate, Femtrace, Apil | |||
7572779 | 2025-10-02 | U-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 |
---|---|---|---|---|---|---|---|---|---|
Contraception | D003267 | 12 | 5 | 22 | 14 | 10 | 63 | ||
Menopause | D008593 | EFO_0003922 | N95 | 9 | 7 | 13 | 14 | 6 | 47 |
Infertility | D007246 | EFO_0000545 | 2 | 2 | 4 | 12 | 19 | 38 | |
Healthy volunteers/patients | — | 28 | 4 | 2 | 3 | — | 34 | ||
Polycystic ovary syndrome | D011085 | EFO_0000660 | E28.2 | 4 | — | 2 | 7 | 12 | 25 |
Breast neoplasms | D001943 | EFO_0003869 | C50 | 1 | 13 | 2 | 1 | 5 | 21 |
Hot flashes | D019584 | — | 3 | 9 | 3 | 3 | 18 | ||
Postmenopause | D017698 | 2 | 3 | 6 | 4 | 3 | 16 | ||
Endometriosis | D004715 | EFO_0001065 | N80 | — | 3 | 7 | 3 | 2 | 14 |
Female infertility | D007247 | EFO_0008560 | N97 | 1 | — | 1 | 3 | 5 | 10 |
Show 69 more
Indications Phases 3
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
---|---|---|---|---|---|---|---|---|---|
Premenstrual syndrome | D011293 | N94.3 | 1 | 1 | 4 | — | 2 | 8 | |
Prostatic neoplasms | D011471 | C61 | — | 5 | 2 | — | — | 6 | |
Anorexia nervosa | D000856 | EFO_0004215 | F50.0 | 2 | 2 | 1 | — | — | 5 |
Schizophrenia | D012559 | EFO_0000692 | F20 | — | 3 | 2 | — | — | 5 |
Atrophy | D001284 | — | 2 | 2 | — | — | 4 | ||
Adenomyosis | D062788 | EFO_1001757 | N80.0 | 1 | — | 1 | — | 1 | 3 |
Metabolic bone diseases | D001851 | HP_0000938 | — | 1 | 2 | — | — | 3 | |
Premenstrual dysphoric disorder | D065446 | F32.81 | — | 2 | 1 | — | — | 3 | |
Migraine disorders | D008881 | EFO_0003821 | G43 | 1 | 2 | 1 | — | — | 3 |
Obesity | D009765 | EFO_0001073 | E66.9 | — | — | 1 | — | 1 | 2 |
Show 17 more
Indications Phases 2
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
---|---|---|---|---|---|---|---|---|---|
Covid-19 | D000086382 | U07.1 | — | 3 | — | — | — | 3 | |
Neoplasms | D009369 | C80 | 1 | 1 | — | — | — | 2 | |
Feeding and eating disorders | D001068 | F50 | — | 2 | — | — | — | 2 | |
Bulimia nervosa | D052018 | EFO_0005204 | F50.2 | — | 2 | — | — | — | 2 |
Temporomandibular joint disorders | D013705 | M26.6 | — | 1 | — | — | 1 | 2 | |
Fibromyalgia | D005356 | EFO_0005687 | M79.1 | — | 1 | — | — | 1 | 2 |
Endometrial neoplasms | D016889 | EFO_0004230 | — | 2 | — | — | — | 2 | |
Orthostatic intolerance | D054971 | — | 1 | — | — | — | 1 | ||
Ovarian diseases | D010049 | — | 1 | — | — | — | 1 | ||
Hemostasis | D006487 | — | 1 | — | — | — | 1 |
Show 20 more
Indications Phases 1
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
---|---|---|---|---|---|---|---|---|---|
Therapeutic equivalency | D013810 | 10 | — | — | — | 1 | 11 | ||
Pharmacokinetics | D010599 | 5 | — | — | — | — | 5 | ||
Drug interactions | D004347 | 3 | — | — | — | 1 | 4 | ||
Type 1 diabetes mellitus | D003922 | EFO_0001359 | E10 | 1 | — | — | — | 1 | 2 |
Type 2 diabetes mellitus | D003924 | EFO_0001360 | E11 | 2 | — | — | — | — | 2 |
Hepatitis c | D006526 | B19.2 | 2 | — | — | — | — | 2 | |
Systemic lupus erythematosus | D008180 | EFO_0002690 | M32 | 1 | — | — | — | 1 | 2 |
Transgenes | D019076 | 1 | — | — | — | — | 1 | ||
Cerebral arterial diseases | D002539 | EFO_1000859 | 1 | — | — | — | — | 1 | |
Infections | D007239 | EFO_0000544 | 1 | — | — | — | — | 1 |
Show 10 more
Indications Without Phase
Indication | MeSH | Ontology | ICD-10 | Ph 1 | Ph 2 | Ph 3 | Ph 4 | Other | Total |
---|---|---|---|---|---|---|---|---|---|
Psychological sexual dysfunctions | D020018 | F52.0 | — | — | — | — | 2 | 2 | |
Heart disease risk factors | D000082742 | — | — | — | — | 1 | 1 | ||
Premature menopause | D008594 | HP_0008209 | E28.31 | — | — | — | — | 1 | 1 |
Breast density | D000071060 | — | — | — | — | 1 | 1 | ||
Cognitive dysfunction | D060825 | G31.84 | — | — | — | — | 1 | 1 | |
Blood pressure | D001794 | EFO_0004325 | — | — | — | — | 1 | 1 | |
Pulmonary embolism | D011655 | EFO_0003827 | I26 | — | — | — | — | 1 | 1 |
Intracranial sinus thrombosis | D012851 | — | — | — | — | 1 | 1 | ||
Postmenopausal osteoporosis | D015663 | EFO_0003854 | — | — | — | — | 1 | 1 | |
Hemorrhage | D006470 | MP_0001914 | R58 | — | — | — | — | 1 | 1 |
Show 15 more
Epidemiology
Epidemiological information for investigational and approved indications
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Drug
General
Drug common name | ESTRADIOL |
INN | estradiol 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 class | estrogens |
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 |
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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Trends
PubMed Central
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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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