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Deramciclane
Deramciclane (EGIS-3886) is a non-benzodiazepine-type anxiolytic drug to treat various types of anxiety disorders, which 40-80 million people in the world suffer from.〔Orion Pharma Inlicenses Deramciclane from Egis Pharmaceuticals. Phase 3 Program in Anxiety has Started, 2000 http://www.evaluategroup.com/Universal/View.aspx?type=Story&id=29979〕 Deramciclane is a unique alternative to current anxiolytics on the market because it has a novel chemical structure and target. It acts as an antagonist at the 5-HT2A receptor, as an inverse agonist at the 5-HT2C receptor, and as a GABA reuptake inhibitor. The two serotonin receptors are G protein-coupled receptors and are two of the main excitatory serotonin receptor types. Their excitation has been implicated in anxiety and mood. Deramciclane does not affect CYP3A4 activity in metabolizing other drugs, but it is a weak inhibitor of CYP2D6. Some studies also show the drug to have moderate affinity to dopamine D2 receptors and low affinity to dopamine receptor D1. Researchers are looking for alternatives to benzodiazepines for anxiolytic use because benzodiazepine drugs have sedative and muscle relaxant side effects.
==Commercial history==
Deramciclane was discovered by EGIS Pharmaceuticals Ltd in Budapest, Hungary. In 2000, EGIS signed over exclusive rights to Orion Pharma to further develop, register, and market deramciclane. Successful pre-clinical, Phase I, and Phase II trials looked promising to the company and its investors even up until the third quarter of 2002.〔Blow to Orion as deramciclane fails in Phase III anxiety studies, 2003 http://www.thepharmaletter.com/article/blow-to-orion-as-deramciclane-fails-in-phase-iii-anxiety-studies〕 Phase I studies show little to no side effects of deramciclane.〔 Phase II studies show little to no side effects and statistically significant improvement on the Hamilton Anxiety Rating Scale in response to daily 60 mg doses, but not in response to daily 10 or 30 mg doses.〔 Finally, in February, 2003, deramciclane development for use against general anxiety disorder (GAD) was discontinued during Phase III trials due to clinically insignificant results compared to placebo groups.〔
抄文引用元・出典: フリー百科事典『 ウィキペディア（Wikipedia）』
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