"Depression treatments for the past 40 years have involved medications affecting the level of monoamines in the brain — serotonin, dopamine, and norepinephrine. Rapastinel works on the glutamate system representing a completely different mechanistic approach. Our research found that rapastinel acts through a novel site within the NMDA receptor to enhance NMDA receptor function, providing a mechanism of action to explain both the rapid-acting antidepressant effects and a low propensity for dissociative and other psychotomimetic side effects," said
Glutamate is the most prominent excitatory neurotransmitter in the brain, research suggests that dysfunction of the glutamatergic system may play a role in the neurobiology of MDD. The NMDA receptor is one of the glutamatergic receptors in the brain, and plays a critical role in learning, memory, and the strength of synaptic communication. The current research suggests that rapastinel may help relieve depression by enhancing NMDA receptor function.
Please see the full publication here: https://academic.oup.com/ijnp/advance-article/doi/10.1093/ijnp/pyy101/5244644
About Rapastinel
Rapastinel is positive NMDA receptor modulator that demonstrated a rapid onset of antidepressant effect within one day that was sustained for an average of seven days after a single injection in a Phase 2 clinical study. Rapastinel is currently being evaluated as a once weekly, bolus intravenous (IV) injection in adjunctive and monotherapy MDD in Phase 3 clinical studies. Rapastinel is also being evaluated in MDD patients at imminent risk of suicide in a phase 2 proof of concept study.
About MDD
Approximately 16 million Americans are living with MDD, with 6.7 percent of U.S. adults reporting at least one MDD episode in the past year. MDD is the leading cause of disability in the U.S. for people between the ages of 15 and 44 and the primary reason why someone dies of suicide about every 12 minutes.
There remains a significant unmet need in treating MDD. Upwards of 70 percent of patients with MDD are partial or non-responders to first-line therapies, which include selective serotonin reuptake inhibitors (SSRIs) and serotonin-norepinephrine reuptake inhibitors (SNRIs). In addition, current antidepressants can take up to 6-8 weeks to produce a clinically-relevant response, with tolerability issues leading to early discontinuation for many patients. Patients with an inadequate response to current therapies may continue to experience significant depressive symptoms, which can include suicidal ideation in patients with severe, recurrent, or chronic depression. In the U.S. alone, treatment resistant depression costs
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