![]() | |
Clinical data | |
---|---|
Other names | CP-101606 |
ATC code |
|
Identifiers | |
| |
CAS Number |
|
PubChem CID | |
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) | |
| |
| |
![]() ![]() |
Traxoprodil (developmental code name CP-101606) is a drug developed by Pfizer which acts as an NMDA antagonist, selective for the NR2B subunit. [1] [2] It has neuroprotective, [3] analgesic, [4] and anti-Parkinsonian effects in animal studies. [5] [6] Traxoprodil has been researched in humans as a potential treatment to lessen the damage to the brain after stroke, [7] [8] [9] [10] but results from clinical 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-acting antidepressant effects similar to those of ketamine, [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 showed ketamine-like rapidly-acting antidepressant effects in a small clinical trial of 30 patients with depression who were non-responders to 6 weeks of paroxetine treatment. [15] The response rate was 60%, relative to 20% for placebo, 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 of QTc prolongation. [15] Other NR2B subunit-selective antagonists of the NMDA receptor are still under development for depression, such as rislenemdaz (CERC-301, MK-0657). [15]
![]() | |
Clinical data | |
---|---|
Other names | CP-101606 |
ATC code |
|
Identifiers | |
| |
CAS Number |
|
PubChem CID | |
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) | |
| |
| |
![]() ![]() |
Traxoprodil (developmental code name CP-101606) is a drug developed by Pfizer which acts as an NMDA antagonist, selective for the NR2B subunit. [1] [2] It has neuroprotective, [3] analgesic, [4] and anti-Parkinsonian effects in animal studies. [5] [6] Traxoprodil has been researched in humans as a potential treatment to lessen the damage to the brain after stroke, [7] [8] [9] [10] but results from clinical 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-acting antidepressant effects similar to those of ketamine, [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 showed ketamine-like rapidly-acting antidepressant effects in a small clinical trial of 30 patients with depression who were non-responders to 6 weeks of paroxetine treatment. [15] The response rate was 60%, relative to 20% for placebo, 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 of QTc prolongation. [15] Other NR2B subunit-selective antagonists of the NMDA receptor are still under development for depression, such as rislenemdaz (CERC-301, MK-0657). [15]