Drug intelligence / Profile preview

paliperidone palmitate

Development stage
Approved
Lead developer
Janssen Pharmaceutical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intramuscular
01

Overview

Paliperidone palmitate is a long-acting injectable atypical antipsychotic used primarily for the acute and maintenance treatment of schizophrenia in adults, and as monotherapy or adjunctive therapy for schizoaffective disorder. It is the long-chain fatty acid ester (palmitate) prodrug of paliperidone, which itself is the major active metabolite of risperidone. After intramuscular injection, it slowly hydrolyzes to release active paliperidone over weeks to months. The drug acts mainly by antagonizing dopamine D2 receptors and serotonin 5‑HT2A receptors in the brain, reducing psychotic symptoms through dual monoaminergic blockade[1][5][8]. It also exhibits antagonism at alpha1/alpha2 adrenergic and H1 histaminergic receptors.

Brand names
Invega SustennaXeplionInvega TrinzaInvega Hafyera
Other names
棕榈酸帕利哌酮Palmitate de palipéridonePalmitato de paliperidona
02

Targets

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

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