rapastinel
Rapastinel is a novel antidepressant that was under development by Allergan as an adjunctive therapy for the treatment of treatment-resistant depression. It is a centrally active, intravenously administered amidated tetrapeptide that acts as a novel and selective modulator of the NMDA receptor. The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to enhance NMDA receptor-mediated signal transduction and synaptic plasticity. — Wikipedia
Clinical trial activity
19 trials · 14 clinical orgs · 0 marketing orgs
Earliest trial started Nov 1, 2009 (NCT01014650)
Timeline
Indications
Mechanism of action
- Glutamate [NMDA] receptorPARTIAL AGONIST
Glutamate [NMDA] receptor partial agonist
NMDA glycin site partial-agonist, preferentially modulates NR2B-containing NMDAR receptor complexes
Partial agonist of the glycin-site on GRIN1-subunits, preferentially modulates NR2B-containing NMDAR
Partial agonist of the glycin-site on GRIN1-subunits.
- Glutamate receptor ionotropic, NMDA 1 (GRIN1) ↗
- Glutamate receptor ionotropic, NMDA 2A (GRIN2A) ↗
- Glutamate receptor ionotropic, NMDA 2B (GRIN2B) ↗
- Glutamate receptor ionotropic, NMDA 2D (GRIN2D) ↗
- Glutamate receptor ionotropic, NMDA 3B (GRIN3B) ↗
- Glutamate receptor ionotropic, NMDA 2C (GRIN2C) ↗
- Glutamate receptor ionotropic, NMDA 3A (GRIN3A) ↗
- Glutamate (NMDA) receptor subunit zeta 1
- Glutamate [NMDA] receptor subunit epsilon 1
- Glutamate [NMDA] receptor subunit epsilon 2
- Glutamate [NMDA] receptor subunit 3A
- Glutamate [NMDA] receptor subunit epsilon 4
- Glutamate [NMDA] receptor subunit epsilon 3
- Glutamate NMDA receptor; GRIN1/GRIN2B
- Glutamate NMDA receptor; GRIN1/GRIN2A
- Ionotropic glutamate receptor NMDA 1/2C
- Ionotropic glutamate receptor NMDA 1/2D
- Glutamate NMDA receptor; GRIN1/GRIN2A/GRIN2B
- Glutamate receptor ionotropic, NMDA 1/2C/3B
Chemistry & pharmacology
SMILES
C[C@@H](O)[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1CCC[C@H]1C(=O)N[C@H](C(N)=O)[C@@H](C)O- Mol. weight
- 413.48 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaRapastinel ↗
- ChEMBLCHEMBL3544917 ↗
Also known as
- glyx-13
- glyx-13
- glyx-13
- glyx-13 peptide
- rapastinel
- rapastinel
- rapastinel
- rapastinel
- rapastinel
- tppt-amide
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03855865 | Phase 3 | Jul 1, 2019 | Allergan |
| NCT03814733 | Phase 1 | Nov 14, 2018 | Allergan |
| NCT03799900 | Phase 1 | Nov 1, 2018 | Allergan |
| NCT03675776 | Phase 3 | Oct 1, 2018 | Allergan |
| NCT03668600 | Phase 3 | Aug 23, 2018 | Allergan |
| NCT03614156 | Phase 3 | Aug 7, 2018 | Allergan |
| NCT03560518 | Phase 3 | Jun 15, 2018 | Allergan |
| NCT03352453 | Phase 2 | Dec 5, 2017 | Allergan |
| NCT03002077 | Phase 3 | Feb 3, 2017 | Allergan |
| NCT02951988 | Phase 3 | Nov 13, 2016 | Allergan |
| NCT02943577 | Phase 3 | Nov 2, 2016 | Allergan |
| NCT02943564 | Phase 3 | Nov 1, 2016 | Allergan |
| NCT02932943 | Phase 3 | Oct 15, 2016 | Allergan |
| NCT02192099 | Phase 2 | Feb 1, 2015 | Allergan, Naurex |
| NCT02267629 | Phase 2 | Oct 1, 2014 | Columbia University, Stanford University |
| NCT01844726 | Phase 2 | May 1, 2013 | Northwestern University |
| NCT01684163 | Phase 2 | Nov 1, 2012 | Allergan, Naurex |
| NCT01234558 | Phase 2 | May 1, 2011 | Artemis Institute for Clinical Research, Claghorn-Lesem Research Clinic, Houston TX, Clinilabs, CNRI-LA, Pico Rivera CA, CRI-WW Lordes Hospital, Willingboro NJ, Lehigh Center for Clinical Research, Lynn Health Science Institute, Naurex, The University of Texas, Dallas |
| NCT01014650 | Phase 1 | Nov 1, 2009 | Lotus Clinical Research, Naurex |
Organizations
Research & Development (14)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Allergan | For profit | 15 | 13 | 3 | 2012 |
| Naurex | For profit | 4 | 4 | 2 | 2009 |
| Artemis Institute for Clinical Research | For profit | 1 | 0 | 1 | 2011 |
| Claghorn-Lesem Research Clinic, Houston TX | For profit | 1 | 0 | 1 | 2011 |
| Clinilabs | For profit | 1 | 0 | 1 | 2011 |
| CNRI-LA, Pico Rivera CA | For profit | 1 | 0 | 1 | 2011 |
| Columbia University | Academic/Hospital | 1 | 1 | 1 | 2014 |
| CRI-WW Lordes Hospital, Willingboro NJ | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Lehigh Center for Clinical Research | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Lotus Clinical Research | For profit | 1 | 0 | 1 | 2009 |
| Lynn Health Science Institute | Academic/Hospital | 1 | 0 | 1 | 2011 |
| Northwestern University | Academic/Hospital | 1 | 1 | 1 | 2013 |
| Stanford University | Academic/Hospital | 1 | 0 | 1 | 2014 |
| The University of Texas, Dallas | Academic/Hospital | 1 | 0 | 1 | 2011 |