Overview
Estradiol is a naturally occurring hormone circulating endogenously in females. It is commercially available in several hormone therapy products for managing conditions associated with reduced estrogen, such as vulvovaginal atrophy and hot flashes. Some available forms of estradiol include oral tablets, injections, vaginal rings, transdermal patches, sprays, gels, and creams. When used for oral or IM administration, estradiol is commonly synthesized as a pro-drug ester (such as Estradiol acetate, Estradiol benzoate, Estradiol cypionate, Estradiol dienanthate, and Estradiol valerate). Because it has a low oral bioavailability on its own, estradiol is commonly formulated with an ester side-chain. Ethinylestradiol (EE) is a synthetic form of estradiol commonly used as the estrogenic component of most combination oral contraceptive pills (OCPs). Ethinyl estradiol is different from estradiol due to its higher biovailability and increased resistance to metabolism, rendering it more suitable for oral administration.
Indication
Estradiol is indicated in various preparations for the treatment of moderate to severe vasomotor symptoms and vulvar and vaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, and for the prevention of postmenopausal osteoporosis. It is also used for the treatment of breast cancer (only for palliation therapy) in certain men or women with metastatic disease, and for the treatment of androgen-dependent prostate cancer (only for palliation therapy). It is also used in combination with other hormones as a component of oral contraceptive pills for preventing pregnancy (most commonly as Ethinylestradiol, a synthetic form of estradiol). A note on duration of treatment Recommendations for treatment of menopausal symptoms changed drastically following the release of results and early termination of the Women's Health Initiative (WHI) studies in 2002 as concerns were raised regarding estrogen use. Specifically, the combined estrogen–progestin group was discontinued after about 5 years of follow up due to a statistically significant increase in invasive breast cancer and in cardiovascular events. Following extensive critique of the WHI results, Hormone Replacement Therapy (HRT) is now recommended to be used only for a short period (for 3-5 years postmenopause) in low doses, and in women without a history of breast cancer or increased risk of cardiovascular or thromboembolic disease. Estrogen for postmenopausal symptoms should always be given with a progestin component due to estrogen's stimulatory effects on the endometrium; in women with an intact uterus, unopposed estrogen has been shown to promote the growth of the endometrium which can lead to endometrial hyperplasia and possibly cancer over the long-term.
Associated Conditions
- Atrophic Vaginitis
- Breast Cancer
- Breast engorgement caused by Postpartum state
- Heavy Menstrual Bleeding
- Hypogonadism female
- Kraurosis Vulvae
- Metastatic Breast Cancer
- Osteoporosis
- Postmenopausal Osteoporosis
- Premature Ovarian Failure (POF)
- Prostate Cancer
- Severe Pain
- Urogenital atrophy
- Vasomotor Symptoms Associated With Menopause
- Vulvo Vaginal Atrophy
- Advanced androgen dependent Prostate cancer
- Female castration
- Hypoestrogenism
Clinical Trials
Title | Posted | Study ID | Phase | Status | Sponsor |
|---|---|---|---|---|---|
2025/03/26 | Phase 4 | Recruiting | Fundacion Clinic per a la Recerca Biomédica | ||
2025/03/04 | Phase 4 | Not yet recruiting | Advancing Clinical Therapeutics Globally for HIV/AIDS and Other Infections | ||
2025/01/29 | Phase 4 | Recruiting | |||
2024/11/13 | Phase 2 | Recruiting | |||
2024/09/24 | Phase 4 | Recruiting | |||
2024/08/26 | Phase 4 | Recruiting | Aarhus University Hospital | ||
2024/08/09 | Phase 4 | Recruiting | Aarhus University Hospital | ||
2024/07/18 | Phase 4 | Completed | |||
2024/06/13 | Phase 4 | Recruiting | Bradley Nindl | ||
2024/04/23 | Phase 1 | Completed |
FDA Drug Approvals
Approved Product | Manufacturer | NDC Code | Route | Strength | Effective Date |
|---|---|---|---|---|---|
| Amneal Pharmaceuticals LLC | 65162-226 | VAGINAL | 10 ug in 1 1 | 1/23/2024 | |
| Amneal Pharmaceuticals LLC | 65162-150 | TRANSDERMAL | 0.075 mg in 1 d | 4/20/2022 | |
| PharmPak, Inc. | 54348-702 | ORAL | 2 mg in 1 1 | 10/9/2022 | |
| Noven Therapeutics, LLC | 68968-3410 | TRANSDERMAL | 0.10 mg in 1 d | 12/2/2021 | |
| Zydus Lifesciences Limited | 70771-1406 | TRANSDERMAL | 0.1 mg in 1 d | 4/21/2023 | |
| EPIC PHARMA, LLC | 42806-088 | ORAL | 1 mg in 1 1 | 2/2/2021 | |
| Zydus Pharmaceuticals USA Inc. | 68382-323 | TRANSDERMAL | 0.014 mg in 1 d | 3/20/2024 | |
| Amneal Pharmaceuticals NY LLC | 69238-1447 | TRANSDERMAL | 0.025 mg in 1 d | 12/30/2023 | |
| Preferred Pharmaceuticals Inc. | 68788-8566 | TRANSDERMAL | 0.0375 mg in 1 d | 1/12/2024 | |
| A-S Medication Solutions | 50090-6811 | VAGINAL | 0.1 mg in 1 g | 7/30/2021 |
EMA Drug Approvals
Approved Product | Authorization Holder | Status | Issued Date |
|---|---|---|---|
Authorised | 7/26/2011 |
HSA Drug Approvals
Approved Product | Manufacturer | Approval Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| FLEET ENEMA FOR CHILDREN | SIN03275P | ENEMA | 9.5 g/59 ml | 6/3/1989 | |
| DIVIGEL GEL 0.5mg/dose | SIN11644P | GEL | 0.5 mg | 8/22/2001 | |
| FEMOSTON 2/10 TABLET | SIN09530P | TABLET, FILM COATED | 2 mg | 11/11/1997 | |
| FEMOSTON CONTI 1/5 TABLET | SIN12121P | TABLET, FILM COATED | 1 mg | 11/13/2002 | |
| ESTROFEM TABLET 2 mg | SIN06009P | TABLET, FILM COATED | 2 mg | 6/3/1991 | |
| VAGIFEM® VAGINAL TABLET 10MCG | SIN14877P | TABLET, FILM COATED | 0.0100 mg | 10/21/2015 | |
| ESTROFEM TABLET 1 mg | SIN09922P | TABLET, FILM COATED | 1 mg | 7/31/1998 | |
| DIVIGEL GEL 1mg/dose | SIN11642P | GEL | 1 mg | 8/22/2001 | |
| FEMOSTON 1/10 TABLET | SIN11896P | TABLET, FILM COATED | 1 mg | 4/24/2002 | |
| FEMOSTON 1/10 TABLET | SIN11896P | TABLET, FILM COATED | 1 mg | 4/24/2002 |
NMPA Drug Approvals
Approved Product | Company | Approval Number | Drug Type | Dosage Form | Approval Date |
|---|---|---|---|---|---|
| No NMPA approvals found for this drug. | |||||
PPB Drug Approvals
Approved Product | Registration No. | Company | Licence No. | Strength | Registration Date |
|---|---|---|---|---|---|
| No PPB approvals found for this drug. | |||||
TGA Drug Approvals
Approved Product | ARTG ID | Sponsor | Registration Type | Status | Registration Date |
|---|---|---|---|---|---|
| CLIMARA 25 estradiol 25 microgram/day transdermal drug delivery system sachet | 73962 | Medicine | A | 10/16/2000 | |
| ESTALIS SEQUI 50/250 patches sachet composite pack | 338042 | Medicine | A | 10/17/2020 | |
| ESTRADOT 25 estradiol 25 microgram transdermal drug delivery system sachet | 338056 | Medicine | A | 10/17/2020 | |
| CLIMARA 50 estradiol 50 micrograms/day transdermal drug delivery system sachet | 56197 | Medicine | A | 11/15/1996 | |
| ESTALIS SEQUI 50/140 patches sachet composite pack | 479507 | Medicine | A | 4/14/2025 | |
| CLIMARA 75 estradiol 75 microgram/day transdermal drug delivery system sachet | 73963 | Medicine | A | 10/16/2000 | |
| ESTALIS CONTINUOUS 50/140 estradiol 50mcg/day norethisterone acetate 140mcg/day patch sachet | 479505 | Medicine | A | 4/14/2025 | |
| SANDRENA estradiol 0.1% gel 1g sachets | 93609 | Medicine | A | 4/8/2003 | |
| FEMOSTON 2/10 estradiol 2mg and estradiol 2mg with Dydrogesterone 10mg tablet blister pack (CP) | 75889 | Medicine | A | 9/8/2000 | |
| ESTALIS SEQUI 50/250 patches sachet composite pack | 479508 | Medicine | A | 4/14/2025 |
Health Canada Drug Approvals
Approved Product | Company | DIN | Dosage Form | Strength | Market Date |
|---|---|---|---|---|---|
| VIVELLE 75MCG | novartis pharmaceuticals canada inc | 02204436 | Patch - Transdermal | 6.56 MG | 12/31/1996 |
| OESCLIM | fournier pharma inc | 02237807 | Patch - Transdermal | 5 MG | 9/29/1998 |
| ESTALIS SEQUI | novartis pharmaceuticals canada inc | 02243529 | Patch - Transdermal | 0.62 MG | 6/26/2001 |
| ESTALIS SEQUI | novartis pharmaceuticals canada inc | 02243529 | Patch - Transdermal | 4.33 MG | 6/26/2001 |
| ESTRADERM-50 | novartis pharmaceuticals canada inc | 00756857 | Patch (Extended Release) - Transdermal | 4 MG / STRIP | 12/31/1987 |
| DIVIGEL | searchlight pharma inc | 02424924 | Gel - Transdermal | 0.1 % | 4/13/2015 |
| MYFEMBREE | 02541742 | Tablet - Oral | 1 MG | 1/29/2024 | |
| ESTRING | 02168898 | Ring (Slow-Release) - Vaginal | 2 MG | 12/31/1995 | |
| PMS-ESTRADIOL | 02225190 | Tablet - Oral | 0.5 MG | 7/10/1997 | |
| VIVELLE 50MCG | novartis pharmaceuticals canada inc | 02204428 | Patch - Transdermal | 4.33 MG | 12/31/1996 |
CIMA AEMPS Drug Approvals
Approved Product | Company | Registration Number | Pharmaceutical Form | Prescription Type | Status |
|---|---|---|---|---|---|
| BIJUVA 1 MG/100 MG CAPSULAS BLANDAS | 85988 | CÁPSULA BLANDA | Medicamento Sujeto A Prescripción Médica | Commercialized | |
| EVOPAD 75 microgramos/24 H PARCHES TRANSDERMICOS | 61701 | PARCHE TRANSDÉRMICO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized | |
| ESTRADERM MATRIX 100 microgramos/24 horas PARCHES TRANSDERMICOS | Merus Labs Luxco Ii S.À.R.L. | 59155 | PARCHE TRANSDÉRMICO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized |
| ESTRADERM MATRIX 25 microgramos/24 horas PARCHES TRANSDERMICOS | Merus Labs Luxco Ii S.À.R.L. | 59153 | PARCHE TRANSDÉRMICO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized |
| OESTRACLIN 0,6 MG/G GEL | Seid S.A. | 59577 | GEL | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized |
| EVOPAD 100 microgramos/24 H PARCHES TRANSDERMICOS | 61702 | PARCHE TRANSDÉRMICO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized | |
| ESTRADERM MATRIX 50 microgramos/24 horas PARCHES TRANSDERMICOS | Merus Labs Luxco Ii S.À.R.L. | 59154 | PARCHE TRANSDÉRMICO | Medicamento Sujeto A Prescripción Médica. Tratamiento De Larga Duración | Commercialized |
Philippines FDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Philippines FDA approvals found for this drug. | |||||
Saudi SFDA Drug Approvals
Approved Product | Company | License Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Saudi SFDA approvals found for this drug. | |||||
Malaysia NPRA Drug Approvals
Approved Product | Company | Registration Number | Dosage Form | Strength | Approval Date |
|---|---|---|---|---|---|
| No Malaysia NPRA approvals found for this drug. | |||||
UK EMC Drug Information
Medicine Name | MA Holder | MA Number | Pharmaceutical Form | Active Ingredient | Authorization Date |
|---|---|---|---|---|---|
| No UK EMC drug information found for this drug. | |||||
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