ACP-103 -: 5-HT2A receptor inverse agonist -: Treatment of psychosis -: Treatment of sleep disorders

The recent discovery that most available antipsychotics possess 5-HT2A receptor inverse agonist activity has spurred interest in developing more effective 5-HT2A inverse agonists for use in the treatment of schizophrenia and other neuropsychiatric disorders. ACP-103 is a potent and selective 5-HT2A inverse agonist shown to possess excellent oral bioavailability and antipsychotic-like effects, as well as to enhance the efficacy and reduce the side effects of antipsychotic agents in animal models. Pharmacokinetic studies indicated that ACP-103 had a long plasma half-life and occupied 5-HT2A receptors in human brain after oral administration. Clinical studies demonstrated that ACP-103 was safe and well tolerated and improved the efficacy of typical antipsychotic drugs such as haloperidol. Phase 11 studies of ACP-103 in the treatment of insomnia, schizophrenia and treatment-induced dysfunctions in Parkinson's disease have shown promising results, and further clinical studies are under way.