erteberel
Erteberel is a synthetic, nonsteroidal estrogen which acts as a selective ERβ agonist and was under development by Eli Lilly for the treatment of schizophrenia. It was specifically under investigation for the treatment of negative symptoms and cognitive impairment associated with the condition. It managed to reach phase II clinical trials for this indication in the United States in 2015. As of 2021 development has been discontinued. Erteberel was also under investigation for the treatment of benign prostatic hyperplasia and reached phase II clinical studies for this use but failed to improve symptoms in men with the condition and development for this indication was discontinued. The drug has also been proposed as a potential novel treatment for glioblastoma. — Wikipedia
Clinical trial activity
2 trials · 2 clinical orgs · 0 marketing orgs
Earliest trial started Apr 1, 2010 (NCT01097707)
Timeline
2010s
- Jan 1, 2010
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- Estrogen receptor betaAGONIST
ESR2 agonist
Ph2 study for indication Benign Prostatic Hyperplasia was terminated, drug in Ph2 trial for Schizophrenia.
Chemistry & pharmacology
SMILES
Oc1ccc([C@@H]2Oc3ccc(O)cc3[C@@H]3CCC[C@@H]32)cc1- Mol. weight
- 282.34 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaErteberel ↗
- ChEMBLCHEMBL278703 ↗
Also known as
- (3as,4r,9br)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta(c)(1) benzopyran-8-ol
- (3as,4r,9br)-4-(4-hydroxyphenyl)-1,2,3,3a,4,9b-hexahydrocyclopenta(c)(1) benzopyran-8-ol
- erteberel
- erteberel
- erteberel
- erteberel
- ly500307
- ly500307
- ly500307
- ly-500307
- ly-500307
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT01874756 | Phase 2 | Jun 1, 2013 | Eli Lilly, Indiana University |
| NCT01097707 | Phase 2 | Apr 1, 2010 | Eli Lilly |
Organizations
Research & Development (2)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Eli Lilly | For profit | 2 | 1 | 1 | 2010 |
| Indiana University | Academic/Hospital | 1 | 1 | 1 | 2013 |