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Last update 07 May 2026
Estriol
Last update 07 May 2026
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms (16α,17β)-estra-1,3,5(10)-triene-3,16,17-triol, 1,3,5(10)-Estratriene-3,16-alpha,17beta-triol, 16-alpha-Hydroxyestradiol + [18] |
Target |
Action agonists |
Mechanism ERs agonists(Estrogen receptors agonists) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Inactive Organization |
License Organization |
Drug Highest PhaseApproved |
First Approval Date Japan (18 Nov 1960), |
Regulation- |
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Structure/Sequence
Molecular FormulaC18H24O3 |
InChIKeyPROQIPRRNZUXQM-ZXXIGWHRSA-N |
CAS Registry50-27-1 |
Related
39
Clinical Trials associated with EstriolNCT06873971
Effects of Erbium:YAG Laser Combined With Vaginal Estriol Therapy in Postmenopausal Women With Genitourinary Syndrome of Menopause: A Protocol for a Randomised, Double-blind Controlled Trial
ACTRN12625000085471
Safety and Efficacy of the Estriol Eluting Vaginal Pessary (E-Leviate) to Treat Pelvic Organ Prolapse in Postmenopausal Women with Symptomatic Pelvic Organ Prolapse.
ChiCTR2500097448
A randomized controlled trial of platelet-rich plasma therapy for genitourinary syndrome of menopause.
100 Clinical Results associated with Estriol
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100 Translational Medicine associated with Estriol
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100 Patents (Medical) associated with Estriol
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7,672
Literatures (Medical) associated with Estriol01 May 2026MOLECULAR AND CELLULAR ENDOCRINOLOGY
2-Hydroxyestradiol regulates extracellular matrix deposition through estrogen receptor beta activation in airway smooth muscle cells
Article
Author: Kumar, Ashish ; Prakash, Y S ; Sathish, Venkatachalem ; Pabelick, Christina M ; Reza, Mohammad Irshad ; Layek, Buddhadev ; Ambhore, Nilesh Sudhakar ; Balraj, Premanand ; Hawse, John R ; Banerjee, Anurag ; Thompson, Michael A
Airway remodeling in asthma is characterized by increased extracellular matrix (ECM) production and deposition by airway smooth muscle (ASM) cells. Existing studies have shown contrasting effects of 17β-estradiol (E2) in regulating ASM cellular remodeling via differential activation of estrogen receptors (ERs: α and β). Even though downstream metabolites of E2 (2-hydroxyestradiol: 2-HE and 16-hydroxyestradiol: 16αHE2) are gaining recognition for their biological roles in various cellular systems, their role in ASM remodeling remains largely unexplored. Here, we explore the effects of 2-HE and 16αHE2, a highly potent metabolites, on ECM remodeling in ASM. ECM mRNA's/proteins expression and deposition were determined by Western blotting, qRT-PCR, and In-Cell Western analysis. Interaction of metabolites with ERs was performed using a docking study and their impact on regulation of an estrogen response element (ERE) was monitored via a luciferase reporter assay. Further, the ER-specific effect of metabolites was validated using shRNA-mediated ERα and ERβ knockdown ASM cells. 16αHE2 exposure showed no notable changes in transforming growth factor-β (TGF-β)-induced ECM proteins expression and deposition, whereas 2-HE exposure blunted the TGF-β effects. Molecular docking unveiled the binding of 16αHE2 with ERα, while 2-HE more strongly bound to ERβ, which was also confirmed by ERE-luciferase assay. In ERβ knockdown ASM cells, 2-HE inhibited the TGF-β-induced phosphorylation of SMAD2/3, AKT, and ERK1/2. However, 16αHE2 failed to elicit any of these effects. Furthermore, 2-HE significantly decreased the TGF-β-induced transcriptional activities of AP-1 and NF-κB. Overall, our findings suggest 2-HE blunts TGF-β-induced ECM through ERβ; therefore, it may serve as a novel therapeutic target for airway remodeling and asthma.
01 Apr 2026CURRENT OPINION IN OBSTETRICS & GYNECOLOGY
A review of estrogens used in menopausal hormone therapy
Review
Author: Soltani, Amythis ; Voedisch, Amy J.
Purpose of review:
To provide an overview of endogenous and therapeutic estrogens, their receptor biology, clinical applications, and evolving safety considerations, with emphasis on how estrogen type, timing, and route of administration influence outcomes in menopausal hormone therapy (MHT).
Recent findings:
Emerging research shows that estrogen receptor (ER)α, ERβ, and G protein-coupled estrogen receptor mediate distinct and sometimes opposing physiological effects. Updated analyses support the timing hypothesis, showing that starting MHT closer to menopause may yield cardiovascular and neurological benefits not observed with later initiation. Comparative studies demonstrate that estradiol has a more favorable thrombotic and metabolic profile than conjugated equine estrogens. Newer agents such as estetrol provide selective ERα activation with reduced hepatic stimulation and promising effects on vasomotor symptoms, bone turnover, and metabolic markers. Estriol has gained attention for its safety and effectiveness in treating genitourinary syndrome of menopause.
Summary:
Estrogen therapy reflects a nuanced approach informed by receptor selectivity, pharmacologic diversity, and timing of initiation. Estradiol-based and transdermal formulations remain preferred for systemic therapy, while low-dose vaginal estrogen is first line for urogenital symptoms. Novel estrogens and deeper mechanistic insights continue to refine therapeutic options, supporting more targeted and safer use of estrogen across the menopausal transition.
03 Mar 2026ENVIRONMENTAL SCIENCE & TECHNOLOGY
Beyond Nephrotoxicity: Maternal–Fetal Transfer of Melamine and Potential Disruption of Placental Steroid Hormones
Article
Author: Wu, Mingzhu ; Teng, Cuiliu ; Kannan, Kurunthachalam ; Shi, Yumeng ; Zhou, Yichen ; Zhu, Hongkai ; Zhao, Leicheng ; Shen, Ripei ; Xu, Ke ; Chen, Jiangnan
The widespread use of melamine (MEL) and its derivatives has resulted in pervasive human exposure, yet their transplacental transfer and developmental consequences remain insufficiently characterized. In a mother-infant cohort, we quantified four MEL derivatives in matched maternal urine (median: 31.9 ng/mL), maternal blood (1.10 ng/mL), amniotic fluid (15.0 ng/mL), and cord blood (2.01 ng/mL), demonstrating substantial fetal exposure. Transplacental transfer efficiencies of MEL, ammelide, and cyanuric acid (CYA) were 1.46, 1.36, and 1.64, respectively, and were inversely correlated with their log Kow values. Maternal MEL concentration was negatively associated with birth weight, particularly in female infants (10β = 90.5%, 95% CI: 83.0%, 98.9%), estriol mediating approximately 30.7% of this effect. BeWo assays demonstrated that MEL derivatives cross the placental barrier via combined passive diffusion and transporter-modulated processes, involving folate-related transporters together with multiple xenobiotic transport systems. In trophoblast cells, coexposure to MEL and CYA (1:9) at environmentally relevant concentrations suppressed estradiol and estriol secretion in a nonmonotonic, dose-dependent manner, accompanied by down-regulation of key steroidogenic enzymes and compensatory up-regulation of estrogen receptors. Overall, this study provides integrated evidence that MEL analogues may cross the placenta via nutrient-mimicking transport pathways and disrupt placental steroidogenesis, potentially impairing fetal growth.
2
News (Medical) associated with Estriol
100 Deals associated with Estriol
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R&D Status
Approved
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| Indication | Country/Location | Organization | Date |
|---|---|---|---|
| Infertility | China | - | 01 Jan 2000 |
| Vulvovaginal atrophy | United Kingdom | 20 Aug 1982 | |
| Osteoporosis | Japan | 28 Dec 1981 | |
| Female Urogenital Diseases | Japan | 27 Sep 1972 | |
| Menopausal symptoms | Japan | 18 Nov 1960 | |
| Uterine Cervical Erosion | Japan | 18 Nov 1960 | |
| Uterine Cervicitis | Japan | 18 Nov 1960 | |
| Vaginitis | Japan | 18 Nov 1960 |
Developing
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| Urinary Tract Infections | Phase 3 | Spain | - | 04 Oct 2018 |
| vaginal mucosa dry | Phase 2 | Czechia | 01 Oct 2016 | |
| vaginal mucosa dry | Phase 2 | Hungary | 01 Oct 2016 | |
| vaginal mucosa dry | Phase 2 | Italy | 01 Oct 2016 | |
| vaginal mucosa dry | Phase 2 | Spain | 01 Oct 2016 | |
| vaginal mucosa dry | Phase 2 | Sweden | 01 Oct 2016 | |
| Atrophic Vaginitis | Phase 2 | Spain | 16 Oct 2015 | |
| Atrophic Vaginitis | Phase 2 | Sweden | 16 Oct 2015 | |
| Early Stage Breast Carcinoma | Phase 2 | Spain | 16 Oct 2015 | |
| Early Stage Breast Carcinoma | Phase 2 | Sweden | 16 Oct 2015 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
View All Results
Not Applicable | 760 | fwkfcwnwtj(nsqadnzrij) = sensitivity (4.4%), seborrhea (1.5%), rash (1.5%), pigmentation (2.9%), breast pain (6.7%), vaginal bleeding (0.7%), increased breast volume (0.7%) dwcjgpupzu (gtvekrehfb ) View more | Positive | 27 Mar 2026 | |||
Phase 3 | 167 | (0.005% Estriol Group) | jvivqwigtu(dacpeobujk) = sdzkmsykwg wyrgpjkuie (ucvjjmjpqh, 23.33) View more | - | 11 Dec 2020 | ||
Placebo (Placebo Group) | jvivqwigtu(dacpeobujk) = rsuduocxly wyrgpjkuie (ucvjjmjpqh, 16.48) View more | ||||||
Phase 2 | 283 | (Estriol 0.005%) | hakcidtpst = tsiakoooly ekacgqyapn (grjuhkjnqz, wemljylfaq - jyelyrwbtc) View more | - | 25 Sep 2019 | ||
(Estriol 0.002%) | hakcidtpst = xpttactwbj ekacgqyapn (grjuhkjnqz, rbifdayxdm - sovzscvnwp) View more | ||||||
Phase 2 | 61 | (0.005% Estriol Vaginal Gel) | tbfakdtoqr(pgnqypplns) = emmyfwjjlh spnxgqbmsu (jnkhkpnqrs, fldyelaekc - hpmskpcqcf) View more | - | 05 Aug 2019 | ||
Placebo (Placebo Vaginal Gel) | tbfakdtoqr(pgnqypplns) = pcjmmjmpjk spnxgqbmsu (jnkhkpnqrs, ndfeoeutdg - ugbklgnqxd) View more | ||||||
Phase 2 | 123 | (Bevacizumab Spray) | qcjxdrgtiz(rtliiiilxg) = sorpwsyhwc undfgicern (tdbzwzvtvh, pwrdmlwyip - mrntmrnhxh) View more | - | 19 Oct 2018 | ||
(Estriol Spray) | qcjxdrgtiz(rtliiiilxg) = jhjudfbbqg undfgicern (tdbzwzvtvh, mnxelskdob - nsoguakvcx) View more | ||||||
Phase 2 | - | 21 | (Study Arm 1) | ymwqbnznss(ixztjtrrjs) = ybbfhntnev oudekhtrnf (mhtknqkryq, 12.5) View more | - | 16 May 2018 | |
(Study Arm 2) | ymwqbnznss(ixztjtrrjs) = ehjctbwhqo oudekhtrnf (mhtknqkryq, 0) View more | ||||||
Phase 2 | 70 | Estriol vaginal gel | dwurwhiqoh(wpmtbbncbh) = One serious adverse event emerged before the patient initiated treatment thoqsxpyev (bwsjykmuwm ) View more | Positive | 15 Feb 2018 | ||
Placebo gel | |||||||
Phase 2 | 158 | ogpdckjqcu(ocneilmrnp) = hlqqkdnpif uyhuvvvlpm (lbomfaqgre, fcleskqzhq - ylnlxythwx) View more | - | 16 Jun 2016 | |||
Placebo+Copaxone (Placebo Capsules Plus Copaxone Injections) | ogpdckjqcu(ocneilmrnp) = ybzxbkpwjv uyhuvvvlpm (lbomfaqgre, bkxpvjhvkz - txfayynmgt) View more | ||||||
Phase 2 | 164 | jojhnsrxux(bpmtnvbplr) = chhbizqzwv oezxmcahtv (guvhzhkilb, 0.17 - 0.37) View more | Positive | 01 Jan 2016 | |||
Placebo | jojhnsrxux(bpmtnvbplr) = wegsdklcsw oezxmcahtv (guvhzhkilb, 0.25 - 0.53) View more | ||||||
Phase 2 | - | Estriol 8 mg per day + Glatiramer Acetate | rcvivtotpg(ivozfijrnu) = Trends for improvement at 24 months in the estriol plus glatiramer acetate group, but not in the placebo plus glatiramer acetate group xifmsliicm (bvxywhezsh ) | Positive | 09 Sep 2014 | ||
Placebo + Glatiramer Acetate |
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