Chemical Name: Apimostinel CAS Number: 1421866-48-9
Mechanism: NMDA receptor partial agonist
Status: Phase II (IV) and Phase I (oral) clinical trials
Developer: Allergan
Also known as NRX-1074, is a drug originally developed by Naurex for the treatment of depression - but currently being studied by both Naurex and Allergan (which acquired Naurex). The drug functions as a selective partial agonist on the NMDA receptor, specifically at the variant of the glycine binding site. While Apimostinel exhibits a similar mechanism of action to GLYX-13 (another drug being developed by Naurex), it differs from GLYX-13 by a more significant weight.
A comparative analysis showed that Apimostinel was thousands of times more potent than GLYX-13 by weight. I've previously discussed the potential benefits of using NRX-1074 to treat depression, mentioning that it works quickly, has no psychotomimetic effects and appears to be well-tolerated. Preliminary evidence suggests that depressive symptoms may disappear within 24 hours of taking Apimostinel.
Additionally, the mood-enhancing effects of Apimostinel appear to be dose-dependent, making the antidepressant effects more pronounced at higher doses. It is worth noting that in early trials, a single dose of Apimostinel provided more relief from depressive symptoms than SSRIs lasting several weeks.
