Last update 15 Jul 2025

Estradiol

Overview

Basic Info

SummaryEstradiol (E2), a predominant female sex hormone and a member of the estrogen family, is responsible for regulating the menstrual and estrous cycles. It plays a pivotal role in orchestrating the development of female secondary sexual characteristics such as breast growth, widening of the hips, and a characteristic fat distribution pattern, as well as the development and sustenance of female reproductive tissues such as the mammary glands, uterus, and vagina. Apart from these crucial functions, E2 exerts significant effects on various other tissues in the body, including the liver, bone, fat, skin, and the brain. Estradiol activates both subtypes of the estrogen receptor (ERα and ERβ), is considered a potent agonist of these nuclear steroid hormone receptors. The hormone has multiple clinical applications, such as treating menopause symptoms, preventing osteoporosis in menopausal women, and treating low estrogen levels in women with ovarian failure. Moreover, it is also indicated in the treatment of certain types of breast and prostate cancer, which highlights its versatility and clinical significance. Interestingly, E2 is available in a diverse range of forms including oral tablets, topical gels or patches, vaginal creams, and injections, which provide ample options for individuals to choose from, based on their unique and specific requirements, preferences, and medical history.
Drug Type
Small molecule drug
Synonyms
17β-estradiol, 17β-Oestradiol, E2
+ [71]
Target
Action
agonists
Mechanism
ERs agonists(Estrogen receptors agonists)
Originator Organization
Inactive Organization
Drug Highest PhaseApproved
First Approval Date
Canada (31 Dec 1976),
RegulationOrphan Drug (United States)
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Structure/Sequence

Molecular FormulaC18H24O2
InChIKeyVOXZDWNPVJITMN-ZBRFXRBCSA-N
CAS Registry50-28-2

External Link

KEGGWikiATCDrug Bank
D00105Estradiol

R&D Status

Approved
10 top approved records.
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IndicationCountry/LocationOrganizationDate
Infertility
Japan
11 Mar 2022
Infertility
Japan
11 Mar 2022
Ovarian Stimulations
Japan
11 Mar 2022
Dyspareunia
United States
29 May 2018
Oestrogen deficiency
Japan
21 Sep 2007
Female Urogenital Diseases
Japan
01 Oct 1999
Hot Flashes
Japan
01 Oct 1999
Hypogonadism
Japan
01 Oct 1999
Atrophic Vaginitis
United States
26 Mar 1999
Osteoporosis, Postmenopausal
United States
20 Dec 1996
Urogenital Diseases
United States
26 Apr 1996
Hypoestrogenism
United States
22 Dec 1994
Hypoestrogenism
United States
22 Dec 1994
Uterine Hemorrhage
United States
22 Dec 1994
Uterine Hemorrhage
United States
22 Dec 1994
Vulvovaginal atrophy
United States
22 Dec 1994
Vulvovaginal atrophy
United States
22 Dec 1994
Vasomotor symptom
Canada
31 Dec 1976
Developing
10 top R&D records.
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IndicationHighest PhaseCountry/LocationOrganizationDate
BurnsPhase 3
Germany
01 Jan 2007
BurnsPhase 3
Latvia
01 Jan 2007
BurnsPhase 3
Russia
01 Jan 2007
BurnsPhase 3
United Kingdom
01 Jan 2007
Varicose UlcerPhase 3
Germany
01 Jan 2007
Varicose UlcerPhase 3
Latvia
01 Jan 2007
Varicose UlcerPhase 3
Russia
01 Jan 2007
Varicose UlcerPhase 3
United Kingdom
01 Jan 2007
Postmenopausal atrophic vaginitisPhase 3
United States
01 Mar 2005
Postmenopausal atrophic vaginitisPhase 3
Canada
01 Mar 2005
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Clinical Result

Indication
Phase
Evaluation
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Study
Phase
PopulationAnalyzed EnrollmentGroupResultsEvaluationPublication Date
Phase 2
29
(17Beta Estradiol, Progesterone)
qayeurqzqp(etzreomyrp) = bixhbgjpvs foxwjkmmqt (zwwdhrurav, 0.52)
-
24 Feb 2025
Placebo Pill
(Transdermal Placebo Patch, Placebo Pill)
qayeurqzqp(etzreomyrp) = evfuvbsahb foxwjkmmqt (zwwdhrurav, 0.64)
Phase 1
63
Intravaginal estradiol (Estring© 7.5mg/day)
zmkdcdqlgw(qhlvxkrmjq) = A total of 88 AEs were reported by 29 participants which were mild (66/88; 75%) and largely resolved (82/88;93%) by the end of the study, with no serious AEs (SAEs) noted utnvgcfdwt (ywqowpnhne )
Positive
21 Jan 2025
Combination of Estring© and oral RepHresh™ Pro-B™ (twice daily)
Not Applicable
-
-
(CRP levels)
prsysnoyav(xhtnshnkfv) = dmmddkakvu tfuduqpdqn (wziayquopj, 4.46)
-
07 Oct 2024
Not Applicable
-
(GDX+ES)
mxunwiowvi(hdcjxblepq) = jomeqwaxza pkvhdsisjr (ygkakczepf )
-
07 Oct 2024
(GDX+V)
mxunwiowvi(hdcjxblepq) = gbimkaxrva pkvhdsisjr (ygkakczepf )
Not Applicable
serum testosterone | estrone | sex hormone binding globulin
45
etmmiskwdf(yvloratfup) = There was one transient local reaction in the SC group fqynakxjir (cmacmvzsua )
-
01 Jun 2024
Not Applicable
testosterone | estradiol | estrone
-
Transdermal 17-beta estradiol
xrltvqyrlf(jixvmdkiph): mean difference = -225.3 (95% CI, -28.8 to -421.7)
Positive
01 Jun 2024
Once-daily sublingual 17-beta estradiol
Not Applicable
-
Sublingual Estradiol 2 mg once daily
tpnsvkgoww(wvybolclpl) = tyswqobjmv tzxljxdygu (iycwhkxwpu )
-
01 Jun 2024
Not Applicable
-
29
pgsaxhwxtd(brnvbzacya) = vpygbgetcr omdungcpio (gsdtecymsr )
-
01 Jun 2024
Not Applicable
-
270
Injectable 17β-estradiol esters (estradiol valerate [EV] and estradiol cypionate [EC])
mvcnimoizy(zszlydwfvh) = limmotssjk wwdfnqrwqw (vyqnhbhokv, 145.8 - 391.5)
-
01 Jun 2024
Not Applicable
Protein S
27
Standard Combined Oral (CO)
hmwwxbqevb(osbeaapbpq) = giyjhfqdpt lrgdbmoqrq (wcmjpfgrvg )
Positive
01 Jun 2024
Sublingual Estradiol (SLE)
hmwwxbqevb(osbeaapbpq) = cvpykpmafw lrgdbmoqrq (wcmjpfgrvg )
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