traxoprodil
Traxoprodil is a drug developed by Pfizer which acts as an NMDA antagonist, selective for the NR2B subunit. It has neuroprotective, analgesic, and anti-Parkinsonian effects in animal studies. Traxoprodil has been researched in humans as a potential treatment to lessen the damage to the brain after stroke, but results from clinical trials showed only modest benefit. The drug was found to cause EKG abnormalities and its clinical development was stopped. More recent animal studies have suggested traxoprodil may exhibit rapid-acting antidepressant effects similar to those of ketamine, although there is some evidence for similar psychoactive side effects and abuse potential at higher doses, which might limit clinical acceptance of traxoprodil for this application. — Wikipedia
Clinical trial activity
3 trials · 1 clinical orgs · 0 marketing orgs
Earliest trial started Sep 1, 2003 (NCT00073476)
Timeline
2000s
- Jan 1, 2003
Earliest Phase 2 Sponsor(trial)
Indications
Mechanism of action
- Glutamate NMDA receptor; GRIN1/GRIN2BANTAGONIST
Glutamate NMDA receptor; GRIN1/GRIN2B antagonist
Development discontinued due to QT prolongation.
Selective for the NR2B subunit.
Chemistry & pharmacology
SMILES
C[C@@H]([C@@H](O)c1ccc(O)cc1)N1CCC(O)(c2ccccc2)CC1- Mol. weight
- 327.42 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaTraxoprodil ↗
- ChEMBLCHEMBL17350 ↗
Also known as
- 1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidino)-1-propanol
- cp 101,606
- cp-101606
- cp-101606
- cp-101606
- cp-101,606
- cp-101,606
- cp-101,606
- traxoprodil
- traxoprodil
- traxoprodil
- traxoprodil mesylate
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00163085 | Phase 2 | May 1, 2005 | Pfizer |
| NCT00163059 | Phase 2 | May 1, 2004 | Pfizer |
| NCT00073476 | Phase 2 | Sep 1, 2003 | Pfizer |
Organizations
Research & Development (1)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Pfizer | For profit | 3 | 3 | 1 | 2003 |