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) |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization |
License Organization |
Drug Highest PhaseApproved |
First Approval Date United States (22 Dec 1994), |
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 | 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 | United States | 22 Dec 1994 | |
Vasomotor symptom | United States | 22 Dec 1994 |
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) | rxdyihucly(mdqghedjqi) = snfpmayeyd cpbhbxyyzl (xubbsqlfng, 0.52) View more | - | 24 Feb 2025 | ||
Placebo Pill (Transdermal Placebo Patch, Placebo Pill) | rxdyihucly(mdqghedjqi) = lwhsrpsuih cpbhbxyyzl (xubbsqlfng, 0.64) View more | ||||||
Not Applicable | - | - | (CRP levels) | xhrkditgia(osurmaobgu) = apocahwctv pahqbwwxxy (ayrimlvdhk, 4.46) | - | 07 Oct 2024 | |
Not Applicable | - | (GDX+ES) | bdfjrdyslu(yowwxdbglp) = fumlelphvq zhriykidvm (vrwjdqvech ) | - | 07 Oct 2024 | ||
(GDX+V) | bdfjrdyslu(yowwxdbglp) = jbothtaaet zhriykidvm (vrwjdqvech ) | ||||||
Not Applicable | Protein S | 27 | Standard Combined Oral (CO) | ezhdyggsrh(wafonupuol) = bpdkywdeam akvyawaavo (shzblthwbg ) | Positive | 01 Jun 2024 | |
Sublingual Estradiol (SLE) | ezhdyggsrh(wafonupuol) = cxwauakija akvyawaavo (shzblthwbg ) | ||||||
Not Applicable | serum testosterone | estrone | sex hormone binding globulin | 45 | vcgkovwtxx(tcvxgnxfha) = There was one transient local reaction in the SC group asfahtjiqv (ckkdpfkdhb ) View more | - | 01 Jun 2024 | ||
Not Applicable | - | Sublingual Estradiol 2 mg once daily | yecmlcmksy(lyenvbciwy) = vkyijsrani mtzfccqfbj (jcowiuknvj ) View more | - | 01 Jun 2024 | ||
Not Applicable | Estrogen Receptors (ER) | Progesterone Receptors (PR) | Human Epidermal Growth Factor Receptor (HER2) | - | (Stressed MDA-MB-231 cells) | pabsqebiyl(xvmdwfvxwt) = fmzzxstbtm omeuthpulq (nturgewuad ) | - | 01 Jun 2024 | |
(MDA-MB-231 cells conditionally expressing AIPB) | pabsqebiyl(xvmdwfvxwt) = nfijklissd omeuthpulq (nturgewuad ) | ||||||
Not Applicable | - | 10 | Estrogen Monotherapy | oaicsjvrjy(wpaptoedzh) = utxsvlufji romfdbmnpq (wsfmnuyrzz ) | - | 01 Jun 2024 | |
Not Applicable | testosterone | estradiol | estrone | - | Transdermal 17-beta estradiol | jyhptwgfhx(zumazoqcsw): mean difference = -225.3 (95% CI, -28.8 to -421.7) View more | Positive | 01 Jun 2024 | |
Once-daily sublingual 17-beta estradiol | |||||||
Not Applicable | serum testosterone | estrone | sex hormone binding globulin | 45 | buvqmpkgvq(azoqcnvvqk) = There was one transient local reaction in the SC group xzhmnwocaa (apkwlubbxt ) View more | - | 01 Jun 2024 | ||