sepranolone
Isopregnanolone, also known as isoallopregnanolone and epiallopregnanolone, as well as sepranolone, and as 3β-hydroxy-5α-pregnan-20-one or 3β,5α-tetrahydroprogesterone (3β,5α-THP), is an endogenous neurosteroid and a natural 3β-epimer of allopregnanolone. It has been reported to act as a subunit-selective negative allosteric modulator of the GABAA receptor, and antagonizes in animals and humans some but not all of the GABAA receptor-mediated effects of allopregnanolone, such as anesthesia, sedation, and reduced saccadic eye movements, but not learning impairment. Isopregnanolone has no hormonal effects and appears to have no effect on the GABAA receptor by itself; it selectively antagonizes allopregnanolone and does not affect the effects of other types of GABAA receptor positive allosteric modulators such as benzodiazepines or barbiturates. — Wikipedia
Clinical trial activity
3 trials · 4 clinical orgs · 0 marketing orgs
Earliest trial started Apr 20, 2018 (NCT03697265)
Timeline
2010s
- Jan 1, 2018
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- Gamma-amino-N-butyrate transaminasePOSITIVE ALLOSTERIC MODULATOR
ABAT positive allosteric modulator
Chemistry & pharmacology
SMILES
CC(=O)[C@H]1CC[C@H]2[C@@H]3CC[C@H]4C[C@@H](O)CC[C@]4(C)[C@H]3CC[C@]12C- Mol. weight
- 318.5 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaIsopregnanolone ↗
- ChEMBLCHEMBL2057301 ↗
Also known as
- sepranolone
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05434546 | Phase 2 | Feb 16, 2022 | Asarina Pharma, University of Copenhagen |
| NCT04102995 | Phase 2 | Aug 27, 2019 | Asarina Pharma |
| NCT03697265 | Phase 2 | Apr 20, 2018 | Asarina Pharma, Ergomed, Keele University |
Organizations
Research & Development (4)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Asarina Pharma | For profit | 3 | 3 | 1 | 2018 |
| Ergomed | For profit | 1 | 0 | 1 | 2018 |
| Keele University | Academic/Hospital | 1 | 0 | 1 | 2018 |
| University of Copenhagen | Academic/Hospital | 1 | 0 | 1 | 2022 |