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news.Naurex has has stated that GLYX-13, its clinical-stage candidate for the treatment of depression, shares key mechanistic features associated with the antidepressant efficacy of the NMDA receptor antagonist ketamine.
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Naurex said that Numerous studies have shown that ketamine has a markedly faster onset of action than other antidepressants (within hours, instead of weeks) and alleviates depression symptoms in a greater proportion of patients, but its clinical utility has been limited by the high incidence of addictive, dissociative and sedative side effects seen at dose levels close to the therapeutic dose.
GLYX-13 is Naurex’s glycine-site functional partial agonist (GFPA) selective modulator of the NMDA receptor (NMDAR).
Naurex said that in previous studies in preclinical models of depression, GLYX-13 demonstrated antidepressant-like effects consistent with those of ketamine.
In the preclinical studies presented at Neuroscience 2010, researchers found that three key features associated with the molecular mechanism underlying ketamine’s antidepressant efficacy are also seen with GLYX-13.
Reportedly, similar to ketamine, GLYX-13 appears to exert its antidepressant-like effects, at least in part, through AMPA receptor-dependent activity, shown by an increase in AMPA throughput and blocking of antidepressant effects when an AMPA antagonist is administered.
In these studies, antidepressant-like efficacy was demonstrated within minutes of administering a single dose of GLYX-13, and it lasted more than two weeks post-dosing.
Naurex founder, president and chief scientist Joseph Moskal said that the new preclinical data confirm that the efficacy mechanism of GLYX-13 is similar to that of ketamine.
Naurex said that the clean safety profile of GLYX-13 has been confirmed in a Phase I clinical trial in healthy volunteers, in which GLYX-13 has demonstrated the widest therapeutic ratio between efficacy and side effects of any known NMDAR modulator.
Naurex acting CEO Derek Small said that as envisioned by their founding scientists who discovered the GFPA modulators, it appears that the GFPA mechanism of GLYX-13 results in just right modulation of the NMDA receptor, achieving efficacy consistent with that of NMDAR blockers such as ketamine, but without the prohibitive side effects that plague those agents.
"We are eager to assess GLYX-13 in our upcoming Phase II trial in treatment-resistant depression, testing whether it can help patients and provide relief within hours, rather than weeks, of receiving a single dose," Small said.