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.
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Other names | CP-101606 |
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ECHA InfoCard | 100.222.813 |
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Formula | C20H25NO3 |
Molar mass | 327.424 g·mol−1 |
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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]