ArticleFrontiers in pharmacology2024
SAL0114: a novel deuterated dextromethorphan-bupropion combination with improved antidepressant efficacy and safety profile.
Article in Frontiers in pharmacology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
Background: Esketamine, the first Food and Drug Administration-approved fast-acting antidepressant, has limited use because of its addictive properties. Although the combination of dextromethorphan and bupropion partially addresses the limitations of esketamine, concerns remain regarding neurologic side effects related to dextromethorphan metabolites, and seizure risks associated with high-dose bupropion. SAL0114, a novel formulation combining deuterated dextromethorphan (in which hydrogen atoms are replaced with deuterium) with bupropion, seeks to enhance dextromethorphan stability through deuteration of its metabolic sites. This approach is expected to increase antidepressant efficacy, reduce metabolite-induced safety issues, and allow for lower bupropion dosages. Methods: Radioligand competition binding assays were used to evaluate the impact of deuterium substitution on the Results: Deuterated dextromethorphan maintained the same Conclusion: Deuteration improved dextromethorphan metabolic stability without altering its
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