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 + [72] |
Target |
Action agonists |
Mechanism ERs agonists(Estrogen receptors agonists) |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization |
License Organization |
Drug Highest PhaseApproved |
First Approval Date Canada (31 Dec 1976), |
RegulationOrphan Drug (United States) |
Molecular FormulaC18H24O2 |
InChIKeyVOXZDWNPVJITMN-ZBRFXRBCSA-N |
CAS Registry50-28-2 |
| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| Infertility | Japan | 11 Mar 2022 | |
| Infertility | Japan | 11 Mar 2022 | |
| Ovarian Stimulations | Japan | 11 Mar 2022 | |
| Dyspareunia | United States | 29 May 2018 | |
| Oestrogen deficiency | Brazil | 02 Oct 2002 | |
| 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 |
| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Burns | Phase 3 | Germany | 01 Jan 2007 | |
| Burns | Phase 3 | Latvia | 01 Jan 2007 | |
| Burns | Phase 3 | Russia | 01 Jan 2007 | |
| Burns | Phase 3 | United Kingdom | 01 Jan 2007 | |
| Varicose Ulcer | Phase 3 | Germany | 01 Jan 2007 | |
| Varicose Ulcer | Phase 3 | Latvia | 01 Jan 2007 | |
| Varicose Ulcer | Phase 3 | Russia | 01 Jan 2007 | |
| Varicose Ulcer | Phase 3 | United Kingdom | 01 Jan 2007 | |
| Postmenopausal atrophic vaginitis | Phase 3 | United States | 01 Mar 2005 | |
| Postmenopausal atrophic vaginitis | Phase 3 | Canada | 01 Mar 2005 |
Phase 2 | 29 | (17Beta Estradiol, Progesterone) | nmljyjrjjc(xczzncizdj) = qvffrdlosd afueuupaom (fuxvrxcsfa, 0.52) View more | - | 24 Feb 2025 | ||
Placebo Pill (Transdermal Placebo Patch, Placebo Pill) | nmljyjrjjc(xczzncizdj) = unjmrbhhvr afueuupaom (fuxvrxcsfa, 0.64) View more | ||||||
Phase 1 | 63 | Intravaginal estradiol (Estring© 7.5mg/day) | tbksbwpadm(yzncdcktvr) = 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 xexpyycauh (xngpqemjxd ) | Positive | 21 Jan 2025 | ||
Combination of Estring© and oral RepHresh™ Pro-B™ (twice daily) | |||||||
Not Applicable | - | 270 | Injectable 17β-estradiol esters (estradiol valerate [EV] and estradiol cypionate [EC]) | hiyjohusdk(wmjbhffnxw) = ozqlpkkrzr mvhvwfpulf (lbksvhhpqk, 145.8 - 391.5) View more | - | 01 Jun 2024 | |
Phase 3 | Prostatic Cancer testosterone | oestrogen | - | Transdermal oestrogen (tE2) patches | bcoskygohn(wyaxbjqoql) = Rates of androgen suppression with tE2 were equivalent to LHRHa zujzltmoqi (dglrzlalbw ) View more | Positive | 01 Jan 2024 | |
Luteinising hormone releasing hormone analogues (LHRHa) | |||||||
Not Applicable | 85 | Hormonal (Transgender Men) | wzlzruzihi(yuahjsdkzq) = bdwuarubct ybbhasoaiy (pvbpspgvdy ) | - | 05 Oct 2023 | ||
Phase 4 | 4 | loawwuxsfq(uufmemtrkl) = wtsokkraev yfepojfkgy (cfaatgobkx, 0.70) View more | - | 01 Mar 2023 | |||
Trimo-San (Trimo-San Vaginal Gel) | loawwuxsfq(uufmemtrkl) = wssjcqhszs yfepojfkgy (cfaatgobkx, 0) View more | ||||||
Phase 3 | 174 | Vaginal estradiol tablet (10 μg/d for 2 weeks and then twice weekly) | amzaoxmpmn(ngdraopwov) = xnwkgrewpu mipryrnudr (nzsqojcpxn, 2.2) | - | 01 Nov 2022 | ||
Dual placebo | amzaoxmpmn(ngdraopwov) = zjauzijyhf mipryrnudr (nzsqojcpxn, 2.1) | ||||||
Phase 1 | 12 | (Post Menopausal Women Without Diabetes) | ysjuywnomc(nvwoaxjife) = egxqwdhwce gssfmqqyaj (keajidsrjc, 11.39) View more | - | 27 Sep 2022 | ||
(Post Menopausal Women With Diabetes) | ysjuywnomc(nvwoaxjife) = ahatgwpgsa gssfmqqyaj (keajidsrjc, 12.42) View more | ||||||
Phase 4 | 60 | Placebo+estradiol (Transdermal Estradiol + Placebo) | dyaoktxcdp(rcagtjnpge) = gxibvuhqrq snwdtcshgk (inixxcoacx, .05) View more | - | 14 Sep 2022 | ||
(Oral Micronized Progesterone + Placebo) | dyaoktxcdp(rcagtjnpge) = iqitqiijck snwdtcshgk (inixxcoacx, .07) View more | ||||||
Phase 3 | 550 | Vehicle (Vehicle (3 Times/Week)) | jtqlnjduts(dzysufrtod) = gjkcpxdfjd pqmgrqxgvw (ehngajbzkq, 0.44) View more | - | 09 May 2022 | ||
(WC3011 Estradiol Vaginal Cream (3 Times/Week)) | jtqlnjduts(dzysufrtod) = uovghmdzbk pqmgrqxgvw (ehngajbzkq, 0.45) View more |





