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Estetrol oral tablet
Estetrol is a selective estrogen receptor modulator (SERM) that binds to estrogen receptors to provide estrogenic activity with a potentially improved safety profile.
Estetrol is a selective estrogen receptor modulator (SERM) that binds to estrogen receptors to provide estrogenic activity with a potentially improved safety profile. Used for Oral contraception, Hormone replacement therapy in menopausal women.
At a glance
| Generic name | Estetrol oral tablet |
|---|---|
| Also known as | E4 oral tablet |
| Sponsor | Estetra |
| Drug class | Selective estrogen receptor modulator (SERM) |
| Target | Estrogen receptor alpha (ERα) and estrogen receptor beta (ERβ) |
| Modality | Small molecule |
| Therapeutic area | Gynecology / Contraception / Women's Health |
| Phase | Phase 3 |
Mechanism of action
Estetrol is a naturally occurring estrogen metabolite that acts as a selective estrogen receptor modulator, activating estrogen receptors in a tissue-selective manner. Unlike conventional estrogens used in hormone therapy, estetrol may provide beneficial estrogenic effects while potentially reducing risks associated with traditional estrogen-based therapies. It is being developed as an oral contraceptive and for hormone replacement therapy applications.
Approved indications
- Oral contraception
- Hormone replacement therapy in menopausal women
Common side effects
- Headache
- Nausea
- Breast tenderness
- Vaginal bleeding irregularities
Key clinical trials
- Estetrol for the Treatment of Moderate to Severe Vasomotor Symptoms in Postmenopausal Women (E4Comfort II) (PHASE3)
- Estetrol for the Treatment of Moderate to Severe Vasomotor Symptoms in Postmenopausal Women (E4Comfort Study I) (PHASE3)
- Safety, Compliance and Pharmacokinetics of Estetrol Monohydrate/Drospirenone 15/3 mg in Post-menarchal Female Adolescents (PHASE3)
- Effect of Estetrol Monohydrate (E4) on QTc Interval (PHASE1)
- E4/DRSP Ovarian Function Inhibition Study (PHASE2)
- Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of LINO-1713 in Healthy Korean Female Subjects (PHASE1)
- Estetrol (E4) for the Treatment of Patients With Confirmed SARS-COV-2 Infection (PHASE2)
- Evaluation of Effects of Estetrol on Testosterone Suppression and Quality of Life in Prostate Cancer Patients Treated With an LHRH Agonist. (PHASE2)
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 |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Estetrol oral tablet CI brief — competitive landscape report
- Estetrol oral tablet updates RSS · CI watch RSS
- Estetra portfolio CI