Drug intelligence / Profile preview

paliperidone

Development stage
Approved
Lead developer
Janssen Research & Development
Modality
Small Molecules
Administration
Oral, Intramuscular
01

Overview

Paliperidone is an atypical antipsychotic medication primarily used to treat schizophrenia and schizoaffective disorder. It is the primary active metabolite of risperidone. While its exact mechanism of action is not fully understood, it is believed to work through a combination of central dopamine D2 receptor and serotonin 5-HT2A receptor antagonism. Paliperidone also acts as an antagonist at alpha-1 adrenergic receptor and alpha-2 adrenergic receptor and histamine H1 receptor, which may explain some of its other effects. The FDA approved paliperidone for the treatment of schizophrenia on December 20, 2006. It is available in multiple formulations including extended-release tablets, once-monthly intramuscular injections, every-three-month intramuscular injections, and twice-yearly gluteal injections. Developed by Janssen.

Brand names
InvegaInvega SustennaInvega TrinzaInvega HafyeraErzofriXeplion
Other names
3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-4H,6H,7H,8H,9H-pyrido[1,2-a]pyrimidin-4-onepaliperidone7-hydroxyrisperidone147663-04-5CB9222359CB-9222359CB 9222359CHEMBL1621CHEMBL-1621CHEMBL 1621
02

Targets

HTR2A (Serotonin receptor 5-HT2A)HRH1 (Histamine H1 Receptor)ADRA2A (α2A)ADRA1A (α1A)DRD2 (Dopamine D2 Receptor)

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