Pimavanserin tartrate: a 5-HT2A inverse agonist with potential for treating various neuropsychiatric disorders.
BACKGROUND
Pimavanserin tartrate is the first 5-HT(2A) inverse agonist to enter clinical trials as a treatment for L-dopa-induced psychosis in Parkinson's disease and for augmentation of low-dose risperidone treatment in schizophrenia. Pimavanserin is also being evaluated as a possible anti-insomnia drug.


OBJECTIVE
To discuss the potential of pimavanserin to fill multiple therapeutic needs.


METHODS
The problems with currently approved antipsychotics and sleep agents are explored to highlight how pimavanserin might address some longstanding issues in the treatment of psychosis and insomnia.


CONCLUSIONS
In Phase II clinical trials, pimavanserin seemed to be safe, well-tolerated and efficacious in treating L-dopa-induced psychosis without worsening motor symptoms. Pimavanserin also potentiated the therapeutic effects of low-dose risperidone, reduced haloperidol-induced akathisia, and increased slow-wave sleep in older individuals.
Abbas
Atheir
A
Case Western Reserve University School of Medicine, Biochemistry, Cleveland, OH 44106, USA. aia4@case.edu
Roth
Bryan L
BL
D002986:Clinical Trials as Topic; D006801:Humans; D015394:Molecular Structure; D010300:Parkinson Disease / Q000188:drug therapy*; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D012559:Schizophrenia / Q000188:drug therapy*; D058826:Serotonin 5-HT2 Receptor Agonists; D016896:Treatment Outcome; D014508:Urea / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D010880:Piperidines; D058826:Serotonin 5-HT2 Receptor Agonists; D014508:Urea; C510793:pimavanserin