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Rapastinel is an investigational, centrally active, intravenously administered amidated tetrapeptide developed as a rapid-acting antidepressant. It acts as a novel and selective positive allosteric modulator of the N-methyl-D-aspartate (NMDA) receptor, enhancing NMDA receptor-mediated signal transduction and synaptic plasticity. Unlike ketamine, it does not produce dissociative or psychotomimetic side effects. Rapastinel was originally developed by Naurex and later acquired by Allergan for adjunctive treatment of major depressive disorder (MDD), particularly in treatment-resistant cases. Despite promising early-phase results showing rapid onset of antidepressant effect within one day lasting up to seven days after a single injection, phase III trials failed to demonstrate efficacy over placebo[1][2][5][7].
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