Multimodal Mechanism of Action of Maritupirdine and the Spectrum of Its Potential Clinical Effects
Abstract
Despite the wide range of available agents, a substantial proportion of patients with anxiety disorders fail to achieve remission or tolerate standard therapy poorly, which creates a need for new agents with anxiolytic activity and alternative mechanisms of action. In this context, maritupirdine, an original multi-target drug registered in Russia for the treatment of generalized anxiety disorder (GAD), is of particular interest. Pharmacologically, it acts predominantly as an antagonist of the 5-HT7 receptor (inhibition constant Ki = 153 pM), with additional antagonistic activity to serotonergic (5-HT2A, 5-HT2C, 5-HT6), adrenergic (α2A, α2B, α2C), and histamine H1 receptors. This review discusses the drug's probable mechanism of action through its receptor profile and the spectrum of its potential clinical effects. In experimental models and early-phase clinical studies, the drug has demonstrated anxiolytic, antidepressant, and procognitive properties with a low risk of adverse effects typical of selective serotonin reuptake inhibitors and selective serotonin-norepinephrine reuptake inhibitors, which are first-line agents in the treatment of anxiety and depressive disorders. At the same time, it should be emphasized that, except for the established anxiolytic effect in GAD, these considerations remain largely theoretical and debatable and require further confirmation in large clinical trials and direct comparative studies with other medications.
Keywords
maritupirdine, generalized anxiety disorder, 5-HT7 receptor, multi-target drug, mechanism of action
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