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Estradiol (E2)
Estradiol binds to estrogen receptors (ERα and ERβ) in target tissues to modulate gene expression and produce estrogenic effects.
Estradiol binds to estrogen receptors (ERα and ERβ) in target tissues to modulate gene expression and produce estrogenic effects. Used for Menopausal vasomotor symptoms, Hormone replacement therapy, Hypogonadism.
At a glance
| Generic name | Estradiol (E2) |
|---|---|
| Also known as | Estreva, E2, Estrofem, Vaginal Estradiol |
| Sponsor | Martin Blomberg Jensen |
| Drug class | Estrogen receptor agonist |
| Target | Estrogen receptor alpha (ERα), Estrogen receptor beta (ERβ) |
| Modality | Small molecule |
| Therapeutic area | Endocrinology |
| Phase | Phase 3 |
Mechanism of action
Estradiol is the primary endogenous estrogen hormone that acts as a ligand for nuclear estrogen receptors, triggering downstream signaling cascades that regulate reproductive, cardiovascular, bone, and metabolic functions. It is used therapeutically in hormone replacement therapy and other endocrine conditions to restore or supplement estrogen levels.
Approved indications
- Menopausal vasomotor symptoms
- Hormone replacement therapy
- Hypogonadism
- Transgender hormone therapy
Common side effects
- Breast tenderness
- Nausea
- Headache
- Vaginal bleeding/spotting
- Fluid retention
- Thromboembolic events
Key clinical trials
- Impact Of FET Preparation Protocol On Endometrial Peristalsis: A Prospective Cohort Study
- COMPASS - COpenhagen MenoPAuSe Study (PHASE2)
- Assessing the Convenience of Natural Proliferative Phase Frozen Embryo Transfer
- Vaginal Estradiol and Oral Guaifenesin in Clomiphene Ovulation Induction (NA)
- The Role of Estrogen and Testosterone in Determining Brain Blood Flow and Metabolic Regulation in Humans (NA)
- Study of the Safety and Contraceptive Efficacy of Relugolix Combination Therapy in Women With Uterine Fibroids or Endometriosis Who Are at Risk for Pregnancy (PHASE3)
- A Dose-finding Study to Evaluate the Effect of a Contraceptive Vaginal Ring, Releasing Nestorone® and Estradiol, on Cycle Control, Ovulation Inhibition, and Pharmacokinetics in Normal Cycling Women (PHASE2)
- Understanding Cycles to Improve Women's Health
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |