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Deramciclane is a non-benzodiazepine-type anxiolytic small molecule developed for the treatment of anxiety disorders. It acts primarily as an antagonist at the serotonin 5-HT2A receptor and as an inverse agonist at the serotonin 5-HT2C receptor. Additionally, it functions as a GABA reuptake inhibitor and has shown moderate affinity for dopamine D2 receptors with low affinity for dopamine D1 receptors. Deramciclane was discovered by Egis Pharmaceuticals and later licensed to Orion Pharma for further development. Although it showed promising results in preclinical and early clinical trials (Phase I/II), its development was discontinued during Phase III due to lack of significant efficacy compared to placebo in generalized anxiety disorder (GAD). The drug is well tolerated with mild side effects such as headache and dizziness, does not produce withdrawal effects after long-term use, and does not significantly affect CYP3A4 activity but is a weak inhibitor of CYP2D6[1][3][5][6].
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