orvepitant
Orvepitant (GW823296) is a drug developed by GlaxoSmithKline which acts as a selective antagonist for the NK1 receptor. It was under development as a potential antidepressant drug, and early stage human clinical trials showed it to have some antidepressant effects, though not with sufficient efficacy to justify further development for this application. It was however considered a successful proof of concept for NK1 antagonists as potential antidepressants, and efforts are continuing to find more potent compounds which might be more effective. — Wikipedia
Clinical trial activity
11 trials · 6 clinical orgs · 0 marketing orgs
Earliest trial started Jun 1, 2007 (NCT00511654)
Timeline
Indications
Mechanism of action
- Neurokinin 1 receptorANTAGONIST
TACR1 antagonist
Phase 2 study terminated, isolated seizure events to be assessed (PMC3071576)
Chemistry & pharmacology
SMILES
Cc1cc(F)ccc1[C@H]1C[C@@H](N2CCN3C(=O)CC[C@H]3C2)CCN1C(=O)N(C)[C@H](C)c1cc(C(F)(F)F)cc(C(F)(F)F)c1- Mol. weight
- 628.63 g/mol
- Lipinski Ro5
- 2 violation(s)
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- ChEMBLCHEMBL2105667 ↗
- WikipediaOrvepitant ↗
- ChEMBLCHEMBL2105668 ↗
Also known as
- gw823296
- gw823296
- gw823296
- gw823296x
- gw823296x
- orvepitant
- orvepitant
- orvepitant
- orvepitant
- orvepitant maleate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT05185089 | Phase 2 | Aug 1, 2022 | NeRRe Therapeutics Ltd., Pharm-Olam International, University of London |
| NCT04387981 | Phase 1 | May 21, 2020 | NeRRe Therapeutics Ltd., Quotient |
| NCT03535662 | Phase 1 | Jun 8, 2018 | NeRRe Therapeutics Ltd., Parexel |
| NCT03464526 | Phase 2 | May 31, 2018 | NeRRe Therapeutics Ltd. |
| NCT02993822 | Phase 2 | May 10, 2017 | NeRRe Therapeutics Ltd. |
| NCT01000493 | Phase 2 | Nov 1, 2009 | GlaxoSmithKline |
| NCT00880399 | Phase 2 | Mar 1, 2009 | GlaxoSmithKline |
| NCT00880048 | Phase 2 | Mar 1, 2009 | GlaxoSmithKline |
| NCT00843011 | Phase 1 | Aug 1, 2008 | GlaxoSmithKline |
| NCT00675116 | Phase 1 | Apr 1, 2008 | GlaxoSmithKline |
| NCT00511654 | Phase 1 | Jun 1, 2007 | GlaxoSmithKline |
Organizations
Research & Development (6)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| GlaxoSmithKline | For profit | 6 | 6 | 2 | 2007 |
| NeRRe Therapeutics Ltd. | For profit | 5 | 5 | 2 | 2017 |
| Parexel | For profit | 1 | 0 | 1 | 2018 |
| Pharm-Olam International | For profit | 1 | 0 | 1 | 2022 |
| Quotient | For profit | 1 | 0 | 1 | 2020 |
| University of London | Academic/Hospital | 1 | 0 | 1 | 2022 |