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paliperidone

✓ Approved

Torrent Pharmaceuticals Limited · DRD2 · Small Molecule

What is paliperidone?

paliperidone is a small molecule developed by Torrent Pharmaceuticals Limited. It is approved for therapeutic indications via oral (po).

Drug Profile

CompanyTorrent Pharmaceuticals Limited
Drug ClassSmall Molecule
Molecular TargetDRD2, HTR2A, HTR7
RouteOral (PO)
StatusApproved
Sources: ClinicalTrials.gov, Torrent Pharmaceuticals Limited

Mechanism of Action

Molecular Targets

paliperidone acts on 3 molecular targets:

DRD2dopamine receptor D2 (D2DR, D2R)
HTR2A5-hydroxytryptamine receptor 2A (5-HT2A, HTR2)
HTR75-hydroxytryptamine receptor 7 (5-HT7)
Want deeper analysis?Noah AI can explain complex mechanisms and compare to similar drugs.

Therapeutic Indications

paliperidone is developed for 1 unique indication across 1 therapeutic area.

Therapeutic AreaConditionPhase
Psychiatric disordersSchizophrenia✓ Approved

Related Research Articles

PubMedEuropean archives of psychiatry and clinical neuroscience2026-09-19

Peripheral immune-cell bioenergetics in acute and stable schizophrenia.

Debska-Vielhaber Grazyna G, Borucki Katrin K, Guest Paul C PC, Dudeck Leon L et al.

Immune and metabolic abnormalities are implicated in schizophrenia, but their functional integration remains unclear. We measured PBMC bioenergetics by Seahorse extracellular flux analysis in healthy controls, acutely ill antipsychotic-naive patients, and stable patients receiving olanzapine or risperidone/paliperidone. Acute schizophrenia showed increased glycolytic ATP production and an altered PBMC bioenergetic phenotype, without significant differences in composite mitochondrial integrity indices. Glycolytic measures were lower in stable treated patients, particularly under olanzapine, although treatment and illness-state effects cannot be separated. Neither plasma nor unstimulated PBMC culture-supernatant cytokines differed after FDR correction. PBMC bioenergetic profiling may provide a hypothesis-generating readout of acute-state-associated metabolic reprogramming.

PMID 42762238
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PubMedClinical neuropharmacology2026-09-18

Retrograde Ejaculation Associated With Paliperidone Palmitate: A Case Report.

Yavuzlar Civan Hazal H

Retrograde ejaculation is a rare but distressing adverse effect of antipsychotic treatment, primarily mediated by alpha-1 adrenergic receptor antagonism. While this complication has been widely reported with risperidone, reports associated with paliperidone palmitate are extremely limited. This report aims to present a case of paliperidone palmitate-induced retrograde ejaculation and to highlight its clinical implications. This report describes a 49-year-old male who developed retrograde ejaculation during treatment with paliperidone palmitate. Clinical evaluation, including urological assessment, was conducted to exclude organic causes. The temporal relationship between medication exposure, dose adjustment, and symptom progression was carefully assessed. Retrograde ejaculation emerged under paliperidone palmitate monotherapy, persisted despite dose reduction, and resolved only after discontinuation and switch to aripiprazole. No organic etiology was identified. Partial improvement was observed during cross-titration, with complete resolution following discontinuation. Paliperidone palmitate can induce retrograde ejaculation despite its lower alpha-1 adrenergic affinity compared with risperidone. This adverse effect may be underrecognized in clinical practice and can contribute to treatment nonadherence. Proactive assessment and appropriate treatment modification are essential to improve clinical outcomes.

PMID 42757639
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PubMedThe Journal of clinical psychiatry2026-09-17

Population Pharmacokinetics and Dosing Simulations for Paliperidone Palmitate 351 mg as Alternative Maintenance Doses in Patients With Schizophrenia or Schizoaffective Disorder.

Chen Yonglin Y, Hu Leijun L, Meyer Jonathan M JM, Citrome Leslie L et al.

Objective: Once-monthly paliperidone palmitate (PP1M) extended-release injectable suspension is approved for the treatment of adults with schizophrenia or schizoaffective disorder. A 351 mg dose of PP1M (LY03010 [brand name Erzofri]) became available in the US in April 2025 and is approved as a single initiation injection followed by recommended monthly maintenance doses up to 234 mg. The objective of this study was to investigate steady-state paliperidone exposure following administration of 351 mg as a maintenance dose at different dosing intervals using population pharmacokinetic (popPK) analysis. Methods: A popPK model was developed using Nonlinear Mixed Effects Modeling (NONMEM) based on the paliperidone concentration data from 2 phase 1 studies for LY03010. Plasma paliperidone exposures based on model simulations were summarized. Results: Simulated plasma concentration-time profiles demonstrated that LY03010 351 mg every 4 weeks (Q4W) produced steady-state paliperidone exposure comparable to 234 mg every 3 weeks (Q3W) based on analysis of Cmax,ss and Ctrough,ss. Simulated data indicated that administration of LY03010 351 mg every 6 weeks (Q6W) provided similar paliperidone exposure to 234 mg PP1M Q4W at steady state. Simulation of LY03010 351 mg every 8 weeks (Q8W) showed that Cmax,ss of paliperidone fell in-between that of 234 mg Q4W and 156 mg Q4W while Ctrough,ss was comparable to that of 117 mg Q4W. Conclusions: PopPK simulations suggest that LY03010 351 mg may provide alternative treatment options as a maintenance dose at different dosing intervals. Currently, there are no clinical data to support the alternative dosing regimens. Trial Registration: ClinicalTrials.gov identifiers: NCT04572685 and NCT04922593.

PMID 42752599
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PubMedThe British journal of psychiatry : the journal of mental science2026-09-14

Dopamine antagonists and dynamic symptom networks in schizophrenia.

Kenny Elizabeth A EA, Brand Bodyl A BA, Ebrahimi Omid V OV, McCutcheon Robert A RA

The symptoms of psychotic disorders do not exist in isolation, but interact with one another as part of a dynamic network. For example, hallucinations may worsen mood, which may exacerbate hallucinations, creating self-reinforcing cycles. These symptom interactions have been shown to lead to the onset and maintenance of disorders. Effective treatments should therefore not only reduce overall symptom severity, but also disrupt these pathological interactions. Although antipsychotics are known to reduce symptom burden, their effects on the dynamic architecture of symptom networks remain unclear. This study aims to characterise how 6 weeks of antipsychotic treatment alters the structure of temporal symptom networks in schizophrenia. Data were pooled from 8 randomised controlled trials evaluating the efficacy of paliperidone over 6 weeks, in 2508 participants with schizophrenia spectrum disorders. Twenty symptoms assessed across four time points were modelled using a panel graphical vector autoregression approach. Temporal networks were estimated for treatment and placebo groups. Network-level and symptom-level connectivity were compared using resampling-based permutation tests. Antipsychotic treatment was associated with significantly lower global symptom network connectivity than placebo treatment (18.92 v. 26.52; S = 7.60; p < 0.001). Specific inter-symptom connections were attenuated, most notably a reduced influence of 'lack of spontaneity' on other symptoms (0.97 v. 1.74; p < 0.001). Antipsychotic treatment not only decreases symptom severity, but also disrupts dynamic interdependencies among symptoms. These findings suggest that effective treatment weakens maladaptive symptom coupling, offering new insights into the mechanisms of clinical improvement and potential targets for intervention.

PMID 42734073
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PubMedJournal of psychiatric practice2026-09-14

Clozapine-Associated Serotonin Syndrome: A Case Report and Literature Review.

Zhan Chanel C, Zahrli Tyler T, Hoover Benjamin B

Serotonin syndrome (SS) is a rare but potentially life-threatening condition resulting from increased serotoninergic activity in the central nervous system, either from exposure to a serotonin agonist or from withdrawal of a serotonin antagonist. Clozapine withdrawal has been implicated in cases of serotonin syndrome; however, clozapine exerts both agonist and antagonist properties at the serotonin receptor. We present the case of a 37-year-old male with unspecified psychosis and a structural neurological deficit who developed SS according to the Hunter Criteria while on a regimen of clozapine, paliperidone, and prednisone taper. Within an hour of receiving 400 mg of clozapine, the patient developed fever, tachycardia, diaphoresis, tremor, hyperreflexia, and inducible clonus. His symptoms resolved with supportive care, including intravenous fluids, benzodiazepines, and acetaminophen. We speculate that clozapine exerted its serotoninergic properties to induce SS symptoms in our patient, although alternative considerations and etiologies are discussed. We also include a review of the literature on cases of serotonin syndrome associated with clozapine. Five case reports were identified, all of which described SS occurring in the context of clozapine withdrawal or discontinuation. To our knowledge, ours is the first case suggestive of clozapine-induced SS. This case highlights the importance of considering SS in patients receiving clozapine, especially when concomitant medications may amplify serotoninergic effects. In addition, clinicians should exercise caution when using clozapine in patients with complex neurological conditions or in those with atypical psychiatric presentations. Close monitoring is needed when clozapine dose adjustments are made.

PMID 42735280
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PubMedThe Australian and New Zealand journal of psychiatry2026-09-13

Employment trajectories following the diagnosis and after long-acting injectable antipsychotic treatment in patients with schizophrenia: A nationwide study.

Wu Chi-Shin CS, Wang Shi-Heng SH, Huang Wei-Lieh WL, Wu Ming-Shiang MS et al.

This study examined employment trajectories following the diagnosis and antipsychotic treatment of schizophrenia, with particular focus on transitions to long-acting injectable antipsychotic treatment. We conducted a nationwide matched cohort study using Taiwan's National Health Insurance Research Database (2001-2021). Individuals aged 18-64 years with newly diagnosed schizophrenia spectrum disorders were matched 1:1 with individuals without schizophrenia by birth year, sex, and index date. Employment trajectories were analyzed using controlled interrupted time-series models. To evaluate treatment-related transitions, individuals initiating long-acting injectable antipsychotics were compared with matched oral antipsychotic users. Subgroup analyses were conducted by illness duration and baseline medication adherence. The schizophrenia cohort (n = 93,041) showed substantially lower employment odds than matched comparisons (OR = 0.31), with a marked decline around diagnosis (OR = 0.90) and only modest recovery thereafter (post-diagnosis trend OR = 1.09 per year). In the treatment analysis (18,488 matched pairs), long-acting injectable users had lower baseline employment odds than oral antipsychotic users (OR = 0.85) and an immediate decline around long-acting injectable initiation (OR = 0.92), followed by a modestly more favorable post-initiation employment trend (OR = 1.03). More favorable post-initiation trends were observed among individuals with longer illness duration and lower baseline adherence. No meaningful differences in employment trajectories were observed across different long-acting injectable formulations, including flupentixol, risperidone, haloperidol, paliperidone, and fluphenazine. Employment outcomes in schizophrenia appear shaped by diagnostic and treatment-related transitions rather than static disease status. Stabilization after long-acting injectable initiation may be linked to incremental improvements in employment trajectories for some subgroups, but optimizing long-term vocational outcomes likely requires integrated psychosocial and vocational support.

PMID 42728847
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