 | |
| Clinical data | |
|---|---|
| Other names | CP-101606; CP-98113 |
| ATC code |
|
| Identifiers | |
| |
| CAS Number |
|
| PubChemCID | |
| IUPHAR/BPS | |
| ChemSpider |
|
| UNII | |
| KEGG |
|
| ChEMBL | |
| CompTox Dashboard(EPA) | |
| ECHA InfoCard | 100.222.813 |
| Chemical and physical data | |
| Formula | C20H25NO3 |
| Molar mass | 327.424 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
| (verify) | |
Traxoprodil (developmental code nameCP-101606) is a drug developed byPfizer which acts as anNMDA antagonist, selective for theNR2B subunit.[1][2] It hasneuroprotective,[3]analgesic,[4] andanti-Parkinsonian effects in animal studies.[5][6] Traxoprodil has been researched in humans as a potential treatment to lessen the damage to the brain afterstroke,[7][8][9][10] but results fromclinical trials showed only modest benefit.[11] The drug was found to cause EKG abnormalities (QT prolongation) and its clinical development was stopped.[12] More recent animal studies have suggested traxoprodil may exhibit rapid-actingantidepressant effects similar to those ofketamine,[13] although there is some evidence for similar psychoactive side effects and abuse potential at higher doses,[14] which might limit clinical acceptance of traxoprodil for this application.
Traxoprodil showedketamine-like rapidly-actingantidepressant effects in a small clinical trial of 30 patients with depression who were non-responders to 6 weeks ofparoxetine treatment.[15] The response rate was 60%, relative to 20% forplacebo, and 33% of the participants met remission criteria by day five following a single administration.[15] After one week, 78% of responders still showed an antidepressant response, and after 15 days, 42% did so.[15] In the study, half of the participants had to have their dose lowered due to a high incidence of dissociative side effects at the higher doses.[15] Development was stopped due to incidence ofQTc prolongation.[15] Other NR2B subunit-selective antagonists of the NMDA receptor are still under development for depression, such asrislenemdaz (CERC-301, MK-0657).[15]
Chemically, traxoprodil is asubstituted phenethylamine andβ-hydroxyamphetaminederivative.[16]
