estetrol
Trade name: NEXTSTELLIS
Approved
Apr 15, 2021
Estetrol (E4), or oestetrol, is one of the four natural estrogenic steroid hormones found in humans, along with estrone (E1), estradiol (E2), and estriol (E3). Estetrol is a major estrogen in the body. In contrast to estrone and estradiol, estetrol is a native estrogen of fetal life. Estetrol is produced exclusively by the fetal liver and is found in detectable levels only during pregnancy, with relatively high levels in the fetus and lower levels in the maternal circulation. — Wikipedia
Clinical trial activity
28 trials · 16 clinical orgs · 1 marketing orgs
Earliest trial started Jun 1, 2005 (NCT00163033)
Timeline
2010s
- Jan 1, 2016
Earliest Phase 3 Sponsor(trial)
2020s
- Apr 15, 2021
Mayne Pharma — Earliest FDA Approval
- Apr 15, 2021
Mayne Pharma — NDA Secondary Org
- Apr 15, 2021
Mayne Pharma — NDA Organization
Indications
Approved for
Studied for
- Breast Neoplasms · Phase 2
- Contraception · Phase 3
- COVID-19 · Phase 2
- Endometrial Neoplasms · Phase 4
- Endometriosis · Phase 4
- Flushing · Phase 2
- Healthy Volunteers · Phase 2
- Heart · Phase 1
- Hemostasis · Phase 1/Phase 2
- Menopause · Phase 3
- Metabolism · Phase 1/Phase 2
- Ovarian Neoplasms · Phase 4
- Pharmacokinetics · Phase 1
- Pharmacology · Phase 1
- Prostatic Neoplasms · Phase 2
- Safety · Phase 3
- Sexual Dysfunction, Physiological · Phase 2
- Uterine Diseases · Phase 4
- Vasomotor System · Phase 3
Mechanism of action
- Estrogen receptorAGONIST
ESR1 agonist
- Estrogen receptorAGONIST
Estrogen receptor agonist
Combination products
nextstellis
with drospirenone
Also known as drospirenone and estetrol, e4/drsp 15/3 mg combined tablet
Approval history
- approvedApr 15, 2021
Chemistry & pharmacology
SMILES
C[C@]12CC[C@@H]3c4ccc(O)cc4CC[C@H]3[C@@H]1[C@@H](O)[C@@H](O)[C@@H]2O- Mol. weight
- 304.39 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
- Delivery
- Oral
- Availability
- Prescription Only
Oral
Yes
Parenteral
No
Topical
No
Sources
- WikipediaEstetrol ↗
- ChEMBLCHEMBL6068423 ↗
- ChEMBLCHEMBL1230314 ↗
Also known as
- estetrol
- estetrol
- estetrol
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06396221 | N/A | May 1, 2024 | Chulalongkorn University |
| NCT05837624 | Phase 4 | Feb 29, 2024 | McGill University |
| NCT06308614 | Phase 2 | Jan 29, 2024 | Estetra |
| NCT06316180 | Phase 4 | Jan 1, 2023 | University of Palermo, University of Roma La Sapienza |
| NCT05460065 | Phase 1 | Apr 4, 2022 | Neurelis, Inc. |
| NCT05677035 | Phase 1 | Jan 11, 2022 | Hyundai |
| NCT04819906 | Phase 1 | Mar 9, 2021 | Estetra |
| NCT04792385 | Phase 3 | Dec 28, 2020 | Estetra |
| NCT04801836 | Phase 2 | Nov 19, 2020 | Neurelis, Inc. |
| NCT04209543 | Phase 3 | Dec 31, 2019 | Estetra, ICON |
| NCT04090957 | Phase 3 | Sep 30, 2019 | Estetra, ICON |
| NCT03798197 | Phase 1 | Jan 30, 2019 | Comac Medical, Pantarhei Bioscience |
| NCT03361969 | Phase 2 | Apr 16, 2018 | Pantarhei Bioscience |
| NCT03512860 | Phase 1 | Mar 28, 2018 | Estetra, Quotient |
| NCT02718144 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2017 | Pantarhei Bioscience |
| NCT03075956 | Phase 1 | Jan 31, 2017 | Comac Medical, Estetra |
| NCT02957630 | Phase 1/Phase 2 (Phase 2) | Sep 1, 2016 | Dinox BV, Estetra |
| NCT02817841 | Phase 3 | Aug 1, 2016 | Estetra, Pharmaceutical Research Associates, Inc. (PRA) |
| NCT02817828 | Phase 3 | Jun 1, 2016 | Estetra, Pharmaceutical Research Associates, Inc. (PRA) |
| NCT02834312 | Phase 2 | May 1, 2016 | Pantarhei Bioscience, Synteract, Inc. |
Organizations
Research & Development (16)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Estetra | For profit | 14 | 14 | 3 | 2010 |
| Pantarhei Bioscience | For profit | 8 | 8 | 2 | 2005 |
| Comac Medical | For profit | 3 | 0 | 1 | 2015 |
| Pharmaceutical Research Associates, Inc. (PRA) | For profit | 3 | 0 | 2 | 2016 |
| ICON | For profit | 2 | 0 | 1 | 2019 |
| Neurelis, Inc. | For profit | 2 | 2 | 2 | 2020 |
| Quotient | For profit | 2 | 0 | 1 | 2016 |
| Chulalongkorn University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| Dinox BV | For profit | 1 | 0 | 1 | 2016 |
| Hyundai | For profit | 1 | 1 | 1 | 2022 |
| McGill University | Academic/Hospital | 1 | 1 | 1 | 2024 |
| QPS | For profit | 1 | 0 | 1 | 2016 |
| Synteract, Inc. | For profit | 1 | 0 | 1 | 2016 |
| University of Palermo | Academic/Hospital | 1 | 1 | 1 | 2023 |
| University of Roma La Sapienza | Academic/Hospital | 1 | 0 | 1 | 2023 |
| University of Vienna | Academic/Hospital | 1 | 0 | 1 | 2007 |
Marketing (2)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Mayne Pharma | For profit | NDA2 | Apr 15, 2021 |
| Mayne Pharma | For profit | NDA | Apr 15, 2021 |